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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).
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