Inhibitors
Cat.No. | Name | Information |
---|---|---|
M9910 | CDKI-73 | CDKI-73 is a potent and orally active CDK9 inhibitor with Ki of 4 nM. |
M9779 | THZ531 | THZ531 is a covalent CDK12 and CDK13 inhibitor with IC50 values of 158 nM and 69 nM, respectively. |
M9761 | AZD-5597 | AZD-5597 is potent CDK inhibitor with in vitro anti-proliferative effects against a range of cancer cell lines. |
M9755 | CYC065 | CYC065 (Fadraciclib) is an orally bioavailable inhibitor of cyclin dependent kinases 2 and 9 (CDK2/9) with IC50 values of 5 and 26 nM, respectively. |
M9622 | BAY-1143572 Racemate | BAY-1143572 Racemate (Atuveciclib Racemate) is the racemate mixture of Atuveciclib, Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM. |
M9558 | JSH-150 | JSH-150 is a potent CDK9 inhibitor with IC50 of 1 nM. |
M9553 | PF-06873600 | PF-06873600 is an orally bioavailable, cyclin-dependent kinase (CDK) inhibitor, with Ki values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. |
M9489 | SY-1365 | SY-1365 (Mevociclib) is a selective covalent CDK7 inhibitor. |
M9239 | BSJ-03-123 | BSJ-03-123 is a potent and novel CDK6-selective small-molecule degrader. |
M8995 | THZ2 | THZ2 (an analog of THZ1) is a potent and selective CDK7 inhibitor which overcomes the instability of THZ1 in vivo (IC50s: CDK7=13.9 nM; TNBC cells=10 nM). |
M8969 | LY-3177833 | LY-3177833 is a potent and selective inhibitor of CDC7 with IC50 of 3.3 nM. |
M8962 | Voruciclib | Voruciclib (P1446A-05) is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with IC50s of 90nM, 25nM, and 22nM for CDK4-CyclinD1, CDK1-Cyclin B, and CDK9-Cyclin T, respectively. |
M8902 | CVT-313 | CVT-313 is a potent and selective inhibitor of CDK2 that prevents neointimal proliferation, which has an IC50 of 0.5 microM in vitro. |
M8369 | PNU112455A hydrochloride | PNU112455A is an ATP site competetive inhibitor of CDK2 and CDK5. |
M8015 | Purvalanol A | Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor. |
M7557 | ON123300 | ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, with little inhibitory activity against CDKs 1,2,5 and 8. |
M6283 | SCH 900776 (CAS:891494-64-7) | MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. |
M6199 | MSC2530818 | MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable. |
M6167 | Palbociclib | Palbociclib is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases. |
M6147 | M2I-1 | M2I-1 a small Mad2 inhibitor-1. the first small molecule inhibitor targeting the binding of Mad2 to Cdc20, an essential proteinprotein interaction (PPI) within the SAC. |
M5332 | NU2058 | NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1. |
M5328 | LDC000067 | LDC000067 is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7. |
M5305 | RO-3306 | RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. |
M5263 | LDC4297 | LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs). |
M5228 | THZ1 | THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. |
M5029 | WHI-P180 | WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively. |
M4889 | LEE011 succinate | LEE011 succinate is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. |
M4617 | Cucurbitacin-E | Cucurbitacin-E is a natural compound which from the climbing stem of Cucumic melo L, which significantly suppresses the activity of the cyclin B1/CDC2 complex. |
M4393 | Wogonin | Wogonin is a cell-permeable and orally available flavonoid that displays anti-inflammatory and anticancer properties. |
M3890 | SU9516 | SU9516 is a selective CDK2 inhibtor with IC50 of 22 nM which is less potent for CDK1/CDK4(IC50=40/200 nM) and has no inhibition on PKC, EGFR, p38MAPK etc. |
M3774 | Kenpaullone | Kenpaullone is potent inhibitor of CDK1/cyclin B and GSK-3β with IC50 values of 0.4 and 0.23 μM respectively. |
M3729 | TAC-101 | TAC-101 is a retinobenzoic acid with potential antineoplastic activity. |
M3687 | AT7519 hydrochloride | AT7519 hydrochloride is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM and induces apoptosis in multiple myeloma via GSK-3β activation and RNA polymerase II inhibition. |
M3641 | XL413 | XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM. |
M3519 | PHA-848125 | 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. |
M3504 | BS-181 hydrochloride | BS-181 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. |
M3483 | Flavopiridol hydrochloride | Flavopiridol 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 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. |
M3475 | PHA-793887 | PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. |
M3062 | TG003 | TG003 is a potent and ATP-competitive Cdc2-like kinase (Clk) inhibitor with IC50 of 20 nM, 200 nM, and 15 nM for Clk1, Clk2, and Clk4, respectively. No inhibitory effect on Clk3, SRPK1, SRPK2, or PKC. |
M2913 | Palbociclib Isethionate | Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 2/3. |
M2911 | P276-00 | p276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. |
M2893 | NU6027 | 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 inhibitors. |
M2858 | ML167 | ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B. |
M2590 | Purvalanol B | Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. |
M2434 | BAY 1000394 | BAY 1000394 is an orally bioavailable pan-CDK inhibitor for CDK1/2/3/4/7/9 with IC50 of 5-25 nM. It also potently inhibits Aurora A, Clk2, ARK5, FGFR1, Flt3, and JAK2/3. Phase 1/2. |
M2323 | BMS-265246 | BMS265246 is a potent and selective CDK inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively. |
M2322 | PHA-767491 | PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively. |
M2239 | SB1317 | SB1317 (TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. |
M2218 | LEE011 | LEE011 is a novel, orally available, potent and selective CDK4/6 inhibitor. |
M2112 | LY2835219 mesylate | LY2835219 mesylate is an orally available inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM, respectively. |
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