| T2412 |
SRT1720 |
SRT 1720 is a selective activator of SIRT1 (EC1.5: 0.16 μM) and shows less potent activities on SIRT2/SIRT3 (EC1.5s: 37 μM/300 μM). |
| T1859 |
AZD8055 |
AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms. |
| T2259 |
Silmitasertib |
CX-4945 is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki: 0.38 nM). |
| T2241 |
Alisertib |
Alisertib (MLN8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib is >200-fold higher for Aurora A than Aurora B. |
| T1952 |
MK-2206 dihydrochloride |
MK-2206 is a highly specific inhibitor of Akt1/2/3 (IC50: 8/12/65 nM in cell-free assays) and no effect on the activities of 250 other protein kinases. |
| T1791 |
LDK378 |
Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM). |
| T1948 |
AZD4547 |
AZD4547, a new-type specific FGFR inhibitor, targets for FGFR1/2/3 (IC50: 0.2/2.5/1.8 nM in cell-free assays). |
| T6269 |
Bemcentinib |
R428 is a selective inhibitor of Axl (IC50: 14 nM) and has been investigated for the treatment of NSCLC. |
| T2144 |
Tacrolimus |
Tacrolimus can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase. |
| T1935 |
LDN-193189 |
LDN193189 (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8/0.8/5.3/16.7 nM for ALK1/2/3/6). |
| T2414 |
Torkinib |
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM). |
| T0740 |
Metformin hydrochloride |
Metformin HCl, a widely used anti-diabetic drug, has a potential function as an anti-Y medicine. It inhibits the proliferation of a variety of Y cells including colon, prostate, |
| T1920 |
Capivasertib |
Capivasertib (AZD5363) is a new-type orally available inhibitor of the serine/threonine protein kinase AKT (IC50s: 3/7/7 nM for Akt1/2/3). |
| T1034 |
Docetaxel |
Docetaxel is a microtubule inhibitor that inhibits microtubule disassembly (IC50: 0.2 μM). |
| T6223 |
U0126-EtOH |
U0126-EtOH is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM). |
| T1903 |
Dabrafenib |
Dabrafenib is a selective inhibitor of mutated forms of BRAF kinase (IC50s: 0.7/5 nM for B-Raf (V600E)/C-Raf). |
| T6253 |
Talazoparib |
Talazoparib is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM). |
| T1921 |
Alpelisib |
Alpelisib is an orally bioavailable PI3Kα inhibitor (IC50: 5 nM in a cell-free assay) with potential antineoplastic activity and minimal effect on PI3Kβ/γ/δ. |
| T6146 |
Dorsomorphin dihydrochloride |
Dorsomorphin is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases. |
| T6069 |
Gemcitabine HCl |
Gemcitabine is a DNA synthesis inhibitor (IC50s: 12, 18, 40, 92.7, 89.3 in Capan2, BxPC-3, Mia Paca-2, PANC-1, and PL-45 cells, respectively). |
| T2155 |
Thiazovivin |
Thiazovivin, a ROCK inhibitor (IC50: 0.5 μM), increases the survival rate of hESC. |
| T3032 |
VE-821 |
VE-821 is a selective ATP competitive inhibitor of ATR( Ki/IC50: 13/26 nM in cell-free assays). |
| T2119 |
ABT-199 |
ABT-199 is a selective inhibitor of Bcl-2 (Ki < 0.010 nM), binding over 3 orders of magnitude less avidly to Bcl-xL, and Bcl-W (Kis = 48 and 245 nM, respectively). |
| T2110 |
(+)-JQ-1 |
(+)-JQ1 is a BET bromodomain inhibitor (IC50: 77 nM/33 nM for BRD4 (1/2)). |
| T2146 |
Fulvestrant |
Fulvestrant is a potent Estrogen Receptor antagonist (IC50: 9.4 nM). |
| T3109 |
Pyrazolanthrone |
SP600125 is a JNK1/2/3 inhibitor (IC50: 40/40/90 nM) and 10-fold higher selectivity than MKK4, 25-fold higher selectivity than MKK3, MKK6, PKCα, and PKB. |
| T1725 |
Y-27632 dihydrochloride |
Y-27632 is a selective inhibitor of ROCKs including p160ROCK (Ki: 140 nM) and ROCK2 (IC50: 800 nM). |
| T6250 |
H 89 2HCl |
H 89 is a potent inhibitor of protein kinase A (PKA; IC50: 0.14 ?M, Ki: 48 nM). |
| T2154 |
MG-132 |
MG-132 is a potent cell-permeable 20S proteasome inhibitor (IC50: 100 nM). It also inhibits calpain (IC50: 1.2 μM). |
| T1762 |
RGFP 966 |
RGFP966 is an HDAC3 inhibitor (IC50: 0.08 μM) and does not affect other HDACs at concentrations up to 15 ?M. |
| T2696 |
PRT062607 hydrochloride |
PRT062607 (BIIB-057) is a selective inhibitor of Syk (IC50: 1 nM). It displays at least 80-fold selectivity for Syk over other kinases. |
| T1637 |
Deferoxamine Mesylate |
Deferoxamine is an iron-chelating agent that binds free iron in a stable complex. It also is an inhibitor of ferroptosis. |
| T3634 |
Osimertinib mesylate |
Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)). |
| T1583 |
Vorinostat |
Vorinostat is a pan-inhibitor of Histone Deacetylase with antineoplastic activity (IC50: ~10 nM). |
| T2301 |
SB202190 |
SB 202190 is a selective and cell-permeable inhibitor of p38 MAPK (IC50s: 50/100 nM for p38α/p38β). |
| T1764 |
SB203580 |
SB 203580 is a p38 MAPK inhibitor (IC50: 0.3-0.5 μM). It shows more than 100-fold selectivity over PKB, LCK, and GSK-3β. |
| T6230 |
Imatinib |
matinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit (IC50: 600/100/100 nM). |
| T2008 |
LY294002 |
LY294002 is an inhibitor of PI3K (IC50s: 0.5/0.57/0.97 μM for PI3Kα/δ/β in cell-free assays). It also blocks autophagosome formation. |
| T1564 |
Cisplatin |
Cisplatin, a DNA-crosslinking agent, is able to suppress DNA synthesis by conforming DNA adducts in cancer cells. |
| T1784 |
Everolimus |
Everolimus is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors. |
| T2539 |
Fingolimod hydrochloride |
Fingolimod, a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells). |
| T2145 |
Temsirolimus |
Temsirolimus is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer. |
| T2623 |
PD 98059 |
PD98059 is a non-ATP competitive MEK inhibitor (IC50: 2/50 μM for MEK1/MEK2). |
| T2399 |
Bortezomib |
Bortezomib (PS-341) is a potent 20S proteasome inhibitor (Ki: 0.6 nM, in a cell-free assay). |
| T0373L |
Erlotinib hydrochloride |
Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer. |
| T0373 |
Erlotinib |
Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer. |
| T1181 |
Gefitinib |
Gefitinib is an EGFR tyrosine kinase inhibitor and can inhibit Tyr1173, Tyr992, Tyr1173 and Tyr992 (IC50s: 37/37/26/57 nM). |
| T2095 |
Roscovitine |
Roscovitine is a potent inhibitor of Cdk2/cyclin E (IC50: 0.1 ?M). It also inhibits Cdk7/cyclin H, Cdk5/p35, and Cdc2/cyclin B (IC50s: 0.49/0.16/0.65 ?M). |
| T6013 |
Z-VAD(OMe)-FMK |
Z-VAD(OMe)-FMK is a cell-permeable and irreversible pan-caspase inhibitor. It inhibits cleavage of PARP, preventing apoptosis when used at 10-50 ?M. |
| T2384 |
Pomalidomide |
Pomalidomide inhibits TNF-α release in LPS stimulated human PBMCs (IC50: 13 nM). It is an anti-angiogenic agent and an immunomodulator. |
| T1642 |
Lenalidomide |
Lenalidomide is a potent inhibitor of TNF-α that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines. |
| T6308 |
Stattic |
Stattic is a small molecule inhibitor of STAT3. It selectively inhibits STAT3 activation, dimerization, and nuclear translocation (IC50: 5.1 μM). |
| T1270 |
Vincristine sulfate |
Vincristine binds irreversibly to microtubules (Ki: 85 nM) and spindle proteins in S phase of the cell cycle and interferes with the formation of the mitotic spindle. |
| T6202 |
DAPT |
DAPT is a novel γ-secretase inhibitor which reduces the Aβ production (IC50: 20 nM in HEK 293 cells) and Aβ42 levels (IC50: 200 nM). |
| T6233 |
Entinostat |
Entinostat (MS-275) is an inhibitor of HDACs that inhibits HDAC1 and HDAC3 (IC50s: 0.18/0.74 μM). |
| T2443 |
CI-1040 |
CI-1040 (PD184352) is an ATP non-competitive MEK1/2 inhibitor (IC50: 17 nM). |
| T1038 |
Fludarabine |
Fludarabine is a nucleic acid synthesis Inhibitor and a STAT1 activation inhibitor. |
| T1621 |
Imatinib Mesylate |
Imatinib mesylate is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively). |
| T0078 |
Lapatinib |
Lapatinib is a dual inhibitor of Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor |
| T1508 |
Decitabine |
Decitabine is a DNA methyltransferase inhibitor that incorporates into DNA resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. |
| T2310 |
CHIR-99021 |
CHIR-99021 (CT99021) is a GSK-3α/β inhibitor (IC50: 10/6.7 nM). |
| T1020 |
Doxorubicin hydrochloride |
Doxorubicin intercalation between base pairs in the DNA helix, thereby preventing DNA replication. It also inhibits topoisomerase II. |
| T3695 |
Pepstatin |
Pepstatin is a specific aspartic proteases inhibitor produced by actinomycetes, and inhibits the aspartic proteases cathepsin D, pepsin and renin. |
| T1878 |
XAV-939 |
XAV-939 shows the selective inhibition against Wnt/β-catenin-mediated transcription by tankyrase1/2 inhibition (IC50: 11/4 nM in cell-free assays). |
| T0093L |
Sorafenib |
Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-4/B-Raf). |
| T6277 |
Doramapimod |
Doramapimod is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70. |
| T1713 |
IBMX |
IBMX is a pan-phosphodiesterase (PDE) inhibitor (IC50s: 6.5/26.3/31.7 μM for PDE3/PDE4/PDE5). |
| T1726 |
SB 431542 |
SB-431542 is a potent and selective inhibitor of ALK5 (IC50: 94 nM) and is also an inhibitor of ALK4 (IC50: 140 nM) and ALK7. |
| T1448 |
Dasatinib |
Dasatinib is a potent inhibitor of the Bcr-Abl and Src family (IC50s: 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit, and c-KitD816V, respectively). |
| T1452 |
Axitinib |
Axitinib is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respectively. |
| T0968 |
Paclitaxel |
Paclitaxel is a cyclodecane isolated from the bark of the Pacific yew tree, TAXUS BREVIFOLIA. It stabilizes MICROTUBULES in their polymerized form leading to cell death. |
| T0132 |
Etoposide |
Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50: 60.3 μM). |
| T0374 |
Sunitinib Malate |
Sunitinib is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit. |
| T6500 |
Ferrostatin-1 |
Ferrostatin-1 is a potent ferroptosis inhibitor (EC50: 60 nM). |
| T1763 |
SB525334 |
SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM). |
| T6143 |
PI-103 |
PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK). |
| T6078 |
Saracatinib |
Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes. |
| T0152 |
Bosutinib |
Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases. |
| T6235 |
Lapatinib Ditosylate |
Lapatinib is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2). |
| T6189 |
PD0325901 |
PD0325901 is a specific and non-ATP-competitive MEK inhibitor (IC50: 0.33 nM). |
| T2383 |
Panobinostat |
Panobinostat is a potent inhibitor of all HDACs (Kis: 0.6-31 nM for HDAC1-11). |
| T6278 |
Sotrastaurin |
Sotrastaurin is a potent pan-PKC inhibitor (Kis: 0.95/0.64/2.1/3.2/1.8/0.22 nM for PKCα/βI/δ/ε/η/θ). |
| T1847 |
Necrostatin-1 |
Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-α-induced necroptosis (EC50: 490 nM in Jurkat cells). |
| T2303 |
Afatinib |
Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, respectively. |
| T1656 |
Vandetanib |
Vandetanib is a potent inhibitor of VEGFR2 (IC50: 40 nM). It also inhibits VEGFR3 and EGFR. |
| T2825 |
Cyclopamine |
Cyclopamine, a Smoothened (Smo) antagonist (IC50: 46 nM in TM3Hh12 cells), belongs to the group of steroidal jerveratrum alkaloids. |
| T6127 |
Rucaparib Phosphate |
Rucaparib is an inhibitor of PARP (Ki: 1.4 nM for PARP1) that is used in clinical therapy to sensitize cancer cells to chemotherapy. |
| T0093 |
Sorafenib tosylate |
Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf). |
| T6111 |
Selisistat |
EX 527 is an effective and specific SIRT1 inhibitor (IC50: 38 nM) and shows >200-fold selectivity against SIRT2/3. |
| T1076 |
Dexamethasone (DHAP) |
Dexamethasone is a glucocorticoid receptor agonist and an IL receptor modulator. |
| T1558 |
Resveratrol |
Resveratrol is a polyphenolic phytoalexin with antioxidant and chemopreventive activities. It has a wide spectrum of targets including COX, SIRT, LOC, etc. |
| T6171 |
BI-D1870 |
BI-D1870 is a cell-permeable, ATP-competitive inhibitor of ribosomal S6 kinases (RSKs; IC50s: 31/24/18/15 nM for RSK1/2/3/4). |
| T2505 |
S3I-201 |
S3I-201 is a selective Stat3 inhibitor (IC50: 86±33 μM) and low effect towards STAT1/5. |
| T6276 |
NU7441 |
NU7441 (KU-57788) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM). |
| T0194 |
Chloroquine diphosphate |
Chloroquine is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs). |
| T0984 |
Fluorouracil |
Fluorouracil interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. |
| T1056 |
Isoprenaline hydrochloride |
Isoproterenol is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties. |
| T1879 |
3-Methyladenine |
3-Methyladenine (3-MA) is a selective PI3KV inhibitor, and the IC50s against ps34 and PI3Kγ were 25/60 μM in HeLa cells, respectively. |
| T1537 |
Rapamycin |
Rapamycin, a macrolide compound obtained from Streptomyces hygroscopicus, is a potent and specific mTOR inhibitor (IC50: 0.1 nM in HEK293 cells). |
| T2398 |
Tofacitinib Citrate |
Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM). |
| T1765 |
Erastin |
Erastin is a ferroptosis activator acting on mitochondrial VDAC. It induces ferroptotic cell death in vitro. |
| T6218 |
Selumetinib |
Selumetinib (AZD6244) is an effective, specific inhibitor of MEK1 and ERK1/2 phosphorylation (IC50: 14/10 nM). |
| T2509 |
Tozasertib |
MK-0457 is a pan-Aurora kinase inhibitor (Kis: 0.6/18/4.6 nM for Aurora A/Aurora B/Aurora C). It shows selectivity against more than 190 different kinases. |
| T1524 |
Nilotinib |
Nilotinib is a second-generation Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. |
| T0320 |
Colchicine |
Colchicine is a tubulin inhibitor (IC50: 3 nM) and blocks polymerization of microtubules by binding to tubulin. |
| T1777 |
Nintedanib |
Nintedanib is an inhibitor of the receptor tyrosine kinases VEGFR/FGFR/PDGFR (IC50s: 13-34/37-610/59/65 nM for VEGFR1-3, FGFR1-4, and PDGFRα/β, respectively). |
| T2939 |
Forskolin |
Forskolin, a potent activator of the adenylate cyclase (EC50: 0.5 μM), can increase the cAMP level. It is extracted from the plant Coleus forskohlii. |
| T2677 |
Crenolanib |
Crenolanib is an orally bioavailable type III tyrosine kinases inhibitor of PDGFRα/β and FLT3 (IC50s: 11, 3.2, and 4 nM). |
| T2325 |
Neratinib |
Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively. |
| T2123 |
LY2109761 |
LY2157299 is a selective inhibitor of the TGF-β receptor I/II kinases (Ki: 38/300 nM). |
| T2510 |
Galunisertib |
Galunisertib is an orally available antagonist of TβRI (IC50: 56 nM) with potential antineoplastic activity. |
| T2602 |
Barasertib |
Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor (IC50: 0.37 nM) and demonstrates ~3,700-fold greater selectivity than Aurora A. |
| T2512 |
Mocetinostat |
Mocetinostat is an orally available HDAC inhibitor with most potency for HDAC1 (IC50: 0.15 μM), 2- to 10- fold selectivity against HDAC2/3/11. |
| T1989 |
Luminespib |
AUY922 (NVP-AUY922) is a new-type inhibitor of HSP90 (IC50s: 7.8/21 nM for HSP90α/β in cell free assay). |
| T1792 |
Regorafenib |
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor (IC50s: 1.5/2.5/4.2/7/13/22 nM for RET/C-RAF/VEGFR2/c-Kit/VEGFR1/PDGFRβ). |
| T6173 |
BI 2536 |
BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3. |
| T6019 |
Volasertib |
Volasertib (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM). |
| T6290 |
Tanespimycin |
Tanespimycin (17-AAG) is an inhibitor of Hsp90 that selectively inhibits BT474 tumor cell Hsp90 (IC50: 5 nM). |
| T3015 |
Olaparib |
Olaparib is a small molecule inhibitor of PARP1/PARP2 (IC50: 5/1 nM) but is less effective against the PARP tankyrase-1 (IC50: 1.5 ?M). |
| T1912 |
Dinaciclib |
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. |
| T6275 |
Obatoclax Mesylate |
Obatoclax is a Bcl-2 antagonist (Ki: 0.22 μM) and can induce apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3. |
| T6239 |
Palbociclib hydrochloride |
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. |
| T6240 |
Palbociclib Isethionate |
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. |
| T6174 |
R406 |
R406 is an effective Syk inhibitor (IC50: 41 nM) and shows no effects on Lyn. |
| T6274 |
RO4929097 |
RO4929097, a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM). |
| T3113 |
Foretinib |
Foretinib is a broad-spectrum tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR. |
| T2586 |
Cabozantinib |
Cabozantinib (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50s: 0.035, 1.3, 4.6, 7 and 11.3 nM). |
| T2099 |
ABT-737 |
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w (EC50s: 78.7/30.3/197.8 nM). |
| T1178 |
Temozolomide |
Temozolomide is a DNA alkylating agent interfering with DNA replication. |
| T1894 |
Idelalisib |
Idelalisib is a small molecule inhibitor of the PI3K catalytic subunit p110δ (IC50: 2.5 nM). The selectivity for p110δ is 40- to 300-fold than p110α/β/γ. |
| T2125 |
Trametinib |
Trametinib is an ATP-noncompetitive inhibitor of MEK 1/2 (IC50s: 0.7/0.9 nM). It shows low inhibition for more than 180 kinases, including B-Raf, c-Raf, and MEK5. |
| T1975 |
Infigratinib |
Infigratinib (BGJ398) is an orally bioavailable pan FGFR inhibitor (IC50: 0.9/1.4/1 nM for FGFR1/2/3), >40-fold selective for FGFR versus FGFR4 and VEGFR2. |
| T2588 |
Ivacaftor |
Ivacaftor (VX-770) is a potentiator of CFTR targeting G551D-CFTR (EC50: 100 nM) and F508del-CFTR (EC50: 25 nM) in Fisher rat thyroid cells, respectively. |
| T1661 |
Crizotinib |
Crizotinib is an ATP-competitive small-molecule tyrosine kinases inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptor. |
| T2590 |
Vismodegib |
Vismodegib is a hedgehog pathway inhibitor (IC50: 3 nM). It also inhibits P-gp (IC50: 3.0 μM), ABCG2 (IC50: 1.4 μM). |
| T2591 |
Veliparib |
Veliparib (ABT-888) is an orally bioavailable inhibitor of PARP (Kis: 5.2/2.9 nM for PARP1/2). It enhances apoptosis and autophagy. |
| T2235 |
Dactolisib |
Dactolisib is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR). |
| T6002 |
Enzalutamide |
Enzalutamide (MDV 3100) is a non-steroidal androgen receptor (AR) antagonist (IC50: 36 nM in LNCaP prostate cells). |
| T2382 |
Vemurafenib |
Vemurafenib (PLX4032) is a novel and potent B-Raf (V600E) inhibitor (IC50: 31 nM). |
| T2473 |
PLX4720 |
PLX-4720 is a potent and selective inhibitor of B-Raf (V600E) (IC50: 13 nM), equally potent to c-Raf-1(Y340D and Y341D mutations). |
| T2101 |
Navitoclax |
Navitoclax (ABT-263) is a potent, orally bioavailable Bcl-2 family protein inhibitor that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki < 1 nM for all three proteins). |
| T2474 |
KU-60019 |
Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50: 6.3 nM). It is much less effective or without effect against a panel of 229 other kinases. |
| T1995 |
Fedratinib |
Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3. |
| T1835 |
Ibrutinib |
Ibrutinib is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation. |
| T2595 |
Lumacaftor |
VX-809 is a CFTR modulator that corrects the folding and trafficking of CFTR protein. It enhances F508del-CFTR protein maturation in FRT cells (EC50: 100 nM). |
| T1829 |
(R)-Ruxolitinib |
Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC50: 3.3/2.8 nM) and is relatively less selective for JAK3 (IC50: 322 nM). |
| T6066 |
SCH772984 |
SCH 772984 is a potent inhibitor of ERK1/ERK2 (IC50: 4/1 nM) and has only weak inhibitory for other 300 tested kinases. |
| T2372 |
Ponatinib |
Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively). |
| T1827 |
Buparlisib |
Buparlisib is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110α, p110β, and p110δ). |
| T0251 |
Gemcitabine |
Gemcitabine is a DNA synthesis inhibitor that can inhibit the growth of MIAPaCa2, BxPC3 and Capan2 cells (IC50s: 40/18/12 nM). It can also induce autophagy. |
| T2066 |
Quizartinib |
Quizartinib is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases. |
| T2077 |
Adavosertib |
MK-1775 is a small molecule inhibitor of the checkpoint kinase WEE1 (IC50: 5.2 nM). It hinders the G2 DNA damage checkpoint. |
| T1994 |
Pictilisib |
Pictilisib (GDC-0941) is a potent pan inhibitor of class I catalytic subunits of PI3K (IC50s: 3/33/3/75 nM for p110α/β/δ/γ). |
