||AT 7519 hydrochloride salt
||AT7519 hydrochloride is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9.
||Palbociclib is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4)
||BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, t
||BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.
||ZCL278 is a selective Cdc42 GTPase inhibitor.
||Dinaciclib is a new-type and effective CDK inhibitor for CDK2/5/1/9 (IC50: 1 nM/1 nM/3 nM/4 nM) with potential antineoplastic activity.
||BIO is a specific inhibitor of GSK-3.
||BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1/2/4/5/6/9.
||NG 52 is a cell-permeable, reversible, and ATP-compatible inhibitor of the cell cycle-regulating kinase Cdc28p and the related Pho85p kinase.
||Bohemine is a cyclin-dependent kinase inhibitor.
||WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
||Purvalanol A is an effective and cell-permeable CDK inhibitor with IC50 of 70/4/35/850 nM for cdk2-cyclin A/B/E, and cdk4-cyclin D1, respectively.
||CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectiv
||Roscovitine is a potent inhibitor of Cdk2/cyclin E (IC50: 0.1 μM). It also inhibits Cdk7/cyclin H, Cdk5/p35, and Cdc2/cyclin B (IC50s: 0.49/0.16/0.65 μM).
||PHA-793887 has been used in trials studying the treatment of Advanced/Metastatic Solid Tumors.
||SC-514 is a selective, orally active, ATP-competitive IKK-2 inhibitor (IC50=11.2±4.7 μM), obstructs NF-κB-dependent gene expression.
||1NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.
||2-Chloropyrazine is used in chemical industry.
||LRRK2-IN-1 is an effective and selective LRRK2 inhibitor.
||Kenpaullone, a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged
||RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.
||RGB-286638 free base
||RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectiv
||LY2835219 is an effective and specific CDK4/6 inhibitor (IC50: 2/10 nM).
||IC261 is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.
||ML141 is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).
||PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).
||AZD5438 is an effective inhibitor of CDK, for CDK1(IC50=16 nM),CDK2(IC50=6 nM),CDK9(IC50=20 nM).
||CHK1 Inhibitor MK-8776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.
||Alvocidib Hydrochloride is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by prevent
||ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor.
||BMS-265246 is a potent and selective CDK1/2 inhibitor.
||TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2).
||TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
||LY2835219 is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).
||VX-11e is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
||NU2058 is a guanine-based CDK inhibitor, also inhibits DNA topoisomerase II ATPase activity.
||CVT-313(NG-26) is a potent, selective, reversible, and ATP-competitive inhibitor.
||Briciclib is a small molecule that suppresses cyclin D1 accumulation in Y cells.
||XL-413 is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. XL-413 binds to and inhibits the activity of CDC7, wh
||NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.
||NSC23005 sodium is a p18INK inhibitor with potently promoted hematopoietic stem cell (HSC) expansion (ED50: 5.21 nM).
||THZ1 is a novel selective and potent covalent CDK7 inhibitor.
||SCH900776 (S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM) and cyclin-dependen
||SB1317 hydrochloride (1204918-72-8(free base))
||SB1317 is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
||SNS-032 is a selective inhibitor of CDK2 (IC50: 48 nM ) and is 10- and 20-fold selective over CDK1/CDK4. It is also sensitive to CDK7/9 (IC50: 62 nM/4 nM), and no effect on CDK6.
||GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.
||URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
||Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.
||JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2.
||A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
||SU11274(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.
||BS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
||SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also has inhibitory effects on CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.
||Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 uM and 0.6 uM.
||PF-562271 (besylate) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other p
||LEE011 is an orally available, and highly specific CDK4/6 inhibitor (IC50：10/39 nM).
||AT7519 is a CDK1/2/4/6/9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.
||PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.
||U0126-EtOH is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM).
||Palbociclib (PD-0332991) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.
||Palbociclib (PD-0332991) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.
||Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), respectively.
||R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.
||CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB
||LDC000067 is a highly specific and selective CDK9 inhibitor with an IC50 value of 44±10 nM.
||NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibit
||XL-413 is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. CDC7 kinase inhibitor BMS-863233 binds to and inhibit
||AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively.
||BI-9564, a specific cell-permeable BRD9 BD inhibitor. The Kd for BRD9 is 5.9 nM, and IC50 for BET family is > 100 μM.
||Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Fl
||K03861 is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely.
||ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11nM).
||PHA-767491 is an effective ATP-competitive dual Cdc7/CDK9 inhibitor (IC50: 10/34 nM). It has ~20-fold selectivity against GSK3-β and CDK1/2, 50-fold selectivity against CDK5 and M
||THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).
||LDC-4297 HCl (1453834-21-3(free base))
||LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.
||Indisulam is a carbonic anhydrase inibitor and Antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting
||A-674563 HCl (552325-73-2(free base))
||A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) . It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16/46 nM) bu
||CC-671 is a dual TTK protein kinase (IC50: 0.005 μM) /CLK2 (IC50: 0.006 μM) inhibitor.
||Indirubin-3’-oxime is a potent inhibitor of GSK3β (IC50: 22 nM) and also inhibits CDKs ( (IC50s: 100/180/250 nM for Cdk5/p35, Cdk1/cyclin B, Cdk2/cyclin E).
||BI-1347 is a potent, selective inhibitor of CDK8/cyclinC (IC50: 1 nM). It shows tumor growth inhibition in an in vivo xenograft model.
||BSJ-03-123 is a potent and novel CDK6-selective small-molecule degrader (PROTAC).
||MC180295 is a novel potent, highly selective CDK9 inhibitor (IC50: 5 nM), displays >22-fold selectivity over other CDKs.
||Senexin A is an effective and selective CDK8 inhibitor that also inhibits CDK19 with Kd values of 0.83 microns and 0.31 microns, respectively.
||Rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer. Rafoxanide is a salicylanilide used as an anthelmintic. It is used to treat fluke, hookworm and other infest
||THZ2, an analog of THZ1, is a potent and selective CDK7 inhibitor(IC50:13.9 nM),with the potential to treat Triple-negative breast cancer (TNBC).
||Purvalanol B is a CDK inhibitor that inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdk2/cyclin B (IC50s = 6, 9, 6, and 6 nM, respectively)
||BS194 is as a potent cyclin-dependent protein kinases (CDKs) inhibitor.
||Alsterpaullone is a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells Through Apoptosis-Inducing Effec
||CYC065 is an orally available, second-generation ATP-competitive inhibitor of CDK2/CDK9 kinases (IC50s: 5/26 nM).
||LY2857785 is a type I competitive and reversible ATP kinase inhibitor against CDK7/CDK8/CDK9 (IC50s: 246 nM/16 nM/11 nM).
||NVP-LCQ195 (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).
||CDK inhibitor II
||CDK-IN-2 is a potent and specific CDK9 inhibitor (IC50: <8 nM).
||MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM).
||LY-3177833 is an Cdc7 kinase inhibitor (IC50 : 3.3 nM)
||CASIN is a specific inhibitor of GTPase Cdc42 (IC50: 2 uM).
||Longdaysin is an inhibitor of CK1α and CK1δ (IC50s: 5.6/8.8 μM). It also can inhibit ERK2 (IC50: 52 μM).
||PNU 112455A is an ATP site competetive inhibitor of CDK2 and CDK5,binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively.
||SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13(CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM), which disables triple-negative breast cancer (TNBC) cells
||Tamarixetin has vasodilator effects in rat isolated vessels. Tamarixetin has cytotoxic against leukemia cells and in particular P-glycoprotein- overexpressing K562/ADR cells, it in
||23-epi-26-Deoxyactein has anti-inflammatory activity, it inhibits nitric oxide production by reducing iNOS expression without affecting activity of the enzyme. It also has anti-can
||Furanodiene has anti-inflammatory and antioxidant activities, it is active against gram-positive bacteria and Candida albicans.
||Hellebrigenin has anti-hepatoma activities, it induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells through inhibition of Akt. Hellebrigenin exhibi
||Ganoderic acid DM
||Ganoderic acid DM is an antiandrogenic osteoclastogenesis inhibitor, it especially suppresses the expression of c-Fos and nuclear factor of activated T cells c1 (NFATc1), this supp
||Pinoresinol has antiinflammatory, hepatoprotective, and fungicidal activities, it can protect pial microcirculation from I-reperfusion injury, to increase nitric oxide release and
||Ganoderic acid H
||Ganoderic acid H is a potent antitumour agent, it mediates its biological effects through the inhibition of transcription factors AP-1 and NF-kappaB, resulting in the down-regulati
||Palbociclib D8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active inhibitor of CDK4 and CDK6 (IC50s of 11 and 16 nM, respectively).
||PROTAC CDK2/9 Degrader-1
||PROTAC CDK2/9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).
||(2S,3R)-Voruciclib is the (2S,3R)-enantiomer of Voruciclib. It is an orally active CDK inhibitor.
||Abemaciclib Metabolites M2
||Abemaciclib Metabolites M2 is a metabolite of abemaciclib, acts as a potent CDK4 and CDK6 inhibitor (IC50s: 1-3 nM) with anti-cancer activity.
||Samuraciclib hydrochloride (CT7001 hydrochloride; ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity
||Senexin B is a potent and selective inhibitor of CDK8/19(CDK8 and CDK19 with Kds of 140 nM and 80 nM).
||PF-06873600 is a selective and orally bioavailable cyclin-dependent kinase (CDK) inhibitor(CDK2, CDK4 and CDK6 with Ki of 0.09 nM, 0.13 nM and 0.16 nM, respectively), has potential
||AG-024322 is a potent ATP-competitive inhibitor of pan-CDK against cell cycle kinases CDK1, CDK2, and CDK4(Ki values in the 1-3 nM range)
||AZ1495 is an oral active Interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor(IC50 of 5 nM and 23 nM for IRAK4 and IRAK1, respectively).
||Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM. Atuveciclib Racemate (BAY-1143572 Racemate) is the racema
||(R)-CR8 trihydrochloride is a potent inhibitor CDK1/2/5/7/9.
||AS2863619 free base
||AS2863619 free base enables the conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor
||Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb/CDK9 inhibitor. It inhibits CDK9/CycT1 (IC50: 13 nM).
||Atuveciclib (BAY-1143572) S-enantiomer is a potent and selective CDK9 inhibitor (IC50: 16 nM for CDK9/CycT1).
||AZD4573 is an effective and selective CDK9 inhibitor (IC50: <4 nM). It enables transient target engagement for the treatment of hematologic malignancies.
||BRD6989, an analog of the natural product cortistatin A (dCA), inhibits CDK8 and upregulates IL-10. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes. It
||BRD7389 is an inducer of insulin expression in pancreatic α-cells and a specific inhibitor of RSK family kinase (IC50s: 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3).
||Cdk1/2 Inhibitor III
||Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor (IC50: 2.1 μM for CDK1/cyclin B).
||CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and non-covalent CDK9 inhibitor while avoiding ABC transporter-mediated efflux. It has a weak binding ability to CDK7
||CDK2-IN-4 is a potent and selective CDK2 inhibitor (IC50: 44 nM for CDK2/cyclin A). It shows 2,000-fold selectivity over CDK1/cyclin B (IC50: 86 uM).
||CDK9-IN-2 is a special CDK9 inhibitor extracted from patent WO/2012131594A1 (compound CDKI(8)) and has an IC50 of 5 nM and 7 nM in A2058 skin cell line (72 hours) and H929 multiple
||CDKI-73 is a potent CDK9 inhibitor (Ki: 4 nM). It shows selective toxicity to CLL cells (LD50: 80 nM) versus normal B cell and normal CD34+ cell (LD50>20 μM).
||CLK-IN-T3 is a potent inhibitor of CDC-like kinase (CLK) (IC50s: 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases) with anti-cancer activity.
||CDK12-IN-3 is a selective CDK12 inhibitor (IC50: 491 nM in an enzymatic assay).
||EHT 5372 is a strong DYRK’s family kinases of inhibitor (IC50s: 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively).
||FN-1501 is a potent FLT3 and CDK inhibitor (IC50s: 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively). FN-1501 also has antica
||SEL120-34A HCl is a selective, orally available and ATP-competitive inhibitor of CDK8(CDK8/CycC and CDK19/CycC with IC50s of 4.4 nM and 10.4 nM , respectively), with antitumor acti
||SEL120-34A monohydrochloride is an ATP-competitive and selective inhibitor of CDK8(CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3
||SY-1365 is a highly selective covalent CDK7 inhibitor. SY-1365 possesses therapeutic potential in both hematological and solid tumors.
||T025 is a highly potent and orally available inhibitor of Cdc2-like kinase (CLK)(Kds of 4.8, 0.096, 6.5, and 0.61 nM for CLK1, CLK2, CLK3, and CLK4, respectively).
||THZ1-R displays diminished activity for CDK7 inhibition(Kd:142 nM).
||FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively. FMF-04-159-2 is a covalent CDK14 inhibitor.
|| FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader . FN-1501-propionic acid is a CDK2/9 ligand for PROTAC.
||Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 2nM, 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively.
||Lerociclib dihydrochloride is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 2 nM and 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively.
||bio-THZ1 is a biotinylated version of THZ1. THZ1 is a selective and irreversibly covalent CDK7 inhibitor (IC50: 3.2 nM).
||Bisindolylmaleimide X hydrochloride
||Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective PKC inhibitor. It is also a potent CDK2 antagonist (IC50: 200 nM).
||Cdc7-IN-1 is a highly selective and ATP competitive inhibitor of Cdc7 kinase (IC50: 0.6 nM at 1 mM ATP). It potently inhibits Cdc7 activity in cancer cells and effectively induces
||IIIM-290 is a oral and potent CDK inhibitor with IC50s of 90 and 94 nM for CDK2/A and CDK9/T1.
||Trilaciclib hydrochloride is an inhibitor of CDK4/6 (IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively).
||Voruciclib hydrochloride is an orally active and selective inhibitor of CDK(Ki of 0.626 nM-9.1 nM).
||CDK4/6/1 Inhibitor is a CDK4/6 inhibitor (IC50s: 3 and 1 nM).
||CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor (IC50s: 2.7 and 16 nM) extracted from patent US20180000819A1 (Compound 1).
||CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM) used for the treatment of glioblastoma. It inhibits CDK1 with a Ki of 110 nM.
||CDK4/6-IN-4 is a selective CDK4/6 inhibitor and the active metabolite of Abemaciclib.
||CDK8/19-IN-1 is a selective and oral bioavailable CDK8/19 dual inhibitor (IC50s: 0.46 nM, 0.99 nM, and 270 nM for CDK8, CDK19, and CDK9).
||CDK8-IN-1 is a selective CDK8 inhibitor (IC50: 3 nM).
||CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection (IC50: 39 nM for CDK9/CycT1).
||CDK9-IN-10 is a potent CDK9 inhibitor and the ligand for the PROTAC CDK9 degrader-2.
||CDK9-IN-11 is a potent CDK9 inhibitor and the ligand for the PROTAC CDK9 degrader-1.
||CDK9-IN-7 is a highly selective and orally active CDK9/cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD: 148 nM; CDK6/cyclinD: 145 nM).
||CDK9-IN-8 is a highly potent and selective CDK9 inhibitor (IC50: 12 nM).
||CDK9-IN-9 is a potent and selective CDK9 inhibitor (IC50: 1.8 nM) with anti-cancer activity. It inhibits CDK2 (IC50: 155 nM).
||CLK1-IN-1 is a potent and selective inhibitor of the Cdc2-like kinase 1 (CLK1; IC50: 2 nM).
||Ribociclib hydrochloride is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It is over 1,000-fold less potent against the cyclin B/CDK1 complex.
||Ribociclib succinate hydrate
||Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50 values of 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1
||Ribociclib succinate is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.
||JSH-150 is a highly selective CDK9 inhibitor(IC50 : 1 nM).
||CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myelo
||YM-46303 is an antagonist of mAChR
||(1S,3R,5R)-PIM447 (dihydrochloride) an inhibitor of PIM(IC50 of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3).
||Indomethacin-D4 is a deuterium labeled Indomethacin. Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2,
||Indoramin D5 is a piperidine antiadrenergic agent. Indoramin D5 is deuterium labeled Indoramin.
||JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflamm
||Men 10376 is a selective antagonist of tachykinin NK-2 receptor. It has a Ki of 4.4 μM for rat small intestine NK-2 receptor.
||NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM
||(R)-CR8 is a potent and selective CDK inhibitor.
||SEL120-34A is a selective, orally available, and ATP-competitive CDK8 inhibitor (IC50s: 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC) with antitumor activity.
||ON-013100 is an antineoplastic drug. It also acts as a mitotic inhibitor that could inhibit Cyclin D1 expression.
||Roniciclib is an inhibitor of pan-cyclin dependent kinase (IC50s: 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7, and CDK9).
||Simurosertib is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <0.3 nM).
||THAL-SNS-032 is a selective CDK9 degrader PROTAC.
||Trilaciclib is an inhibitor of CDK4/6 (IC50s: 1 nM and 4 nM for CDK4 and CDK6, respectively).
||CDK8-IN-4 is an inhibitor of CDK8 (IC50: 0.2 nM).
||CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor (IC50: 2.3 nM).
||NVP-2 is an effective and selective ATP-competitive cyclin-dependent kinase 9 (CDK9) probe. NVP-2 induces cell apoptosis. NVP-2 inhibits CDK9/CycT activity (IC50: 0.514 nM). NVP-2
||Aristolactam AIIIa is a new type of Plk1 inhibitors, targeting the Polo Box domain (PBD), it has anti-tumor activity. Aristolactam IIIa shows inhibition of platelet aggregation ind
||7-O-Prenylscopoletin and cedrelopsin show high antiproliferative activities against cancer cell lines.
||Clausine Z exhibits inhibitory activity against cyclin-dependent kinase 5 (CDK5) and shows protective effects on cerebellar granule neurons in vitro.
||Cristacarpin exhibits moderate but selective activity towards DNA repair-deficient yeast mutants. It promotes endoplasmic reticulum (ER) stress, leading to sub-lethal reactive oxyg
||Dehydrodiconiferyl alcohol shows anti-adipogenic and anti-lipogenic effects in 3T3-L1 cells and primary mouse embryonic fibroblasts. Dehydrodiconiferyl alcohol can modulate the dif
||Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Foxo3a activity by inh
||Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation by targeting PI3K,
||Kobophenol A has antimicrobial, and anti-inflammatory activities, it might be a candidate for treatment of inflammatory bone diseases relevant to osteoblast cell death. Kobophenol
||1. Lappaol F has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade. <br/> 2. Lappaol F has potentia
||AS2863619 is an orally active inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19 (IC50s of 0.61 nM and 4.28 nM, respectively).