About 31 results found for searched term "CDK4-IN-2" (0.095 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M41431 | CDK4-IN-2 | CDK |
| CDK4-IN-2 is a CDK4 inhibitor, with Ki and IC50 values of <10 nM. | ||
| M1806 | PD 0332991 HCL | CDK |
| Palbociclib HCl | ||
| PD-0332991 HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. | ||
| M2434 | BAY 1000394 | CDK |
| Roniciclib | ||
| 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. | ||
| M2911 | Riviciclib hydrochloride (P276-00) | CDK |
| Riviciclib hydrochloride | ||
| Riviciclib hydrochloride (P276-00) is an effective CDK inhibitor, inhibiting CDK9-CyclinT1, CDK4-cyclin D1, CDK1-Cyclinb with IC50 values of 20 nM, 63 nM, respectively. 79 nM. Riviciclib hydrochloride (P276-00) has anti-tumor activity against Cisplatin resistant cells. | ||
| M2913 | Palbociclib Isethionate | CDK |
| PD 0332991 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. | ||
| M6160 | Bohemine | CDK |
| Bohemine is A selective CDK inhibitor with IC50 of 4.6 μM, 83 μM and 2.7 μM against Cdk2/ Cyclin E, Cdk2/ Cyclin A and Cdk9/cyclin T1, respectively. Bohemine also inhibited ERK2, IC50 was 52 μM, and inhibited CDK1, CDK4 and CDK6. Bohemine is also a purine analogue and has a wide range of anticancer activities. | ||
| M7557 | ON123300 | CDK |
| Narazaciclib | ||
| 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. | ||
| M9910 | CDKI-73 | CDK |
| CDKI73; Asnuciclib; LS-007 | ||
| Cdki-73 (LS-007) is an orally active and highly effective CDK9 inhibitor with Ki values of 4 nM, 4 nM and 3 nM against CDK9, CDK1 and CDK2, respectively. Cdki-73 down-regulates phosphorylation of RNA polymerase II. Cdki-73 is also an inhibitor of Rab11. | ||
| M10347 | Abemaciclib (LY2835219) | CDK |
| LY2835219 free base | ||
| Abemaciclib (LY2835219) is a best-in-class, selective and effective dual inhibitor of CDK4 and CDK6, which inhibits CDK4/CDK6 activity with IC50 of 2 nM and 10 nM respectively. | ||
| M10705 | NVP-2 | CDK |
| NVP-2 is an effective and selective ATP competitive cyclin-dependent kinase 9 (CDK9) probe that inhibits CDK9/CycT activity.IC50 The value is 0.514 nM. NVP-2 has inhibitory effects on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases, which IC50 The values are 0.584 μM, 0.706 μM, and 0.605 μM, respectively. NVP-2 induces apoptosis. | ||
| M10734 | YKL-5-124 | CDK |
| YKL-5-124 is a potent, selective, irreversible COVALENT inhibitor of CDK7 and CDK7/Mat1/CycH IC50 53.5 nM and 9.7 nM, respectively. YKL-5-124 is more than 100 times more selective to CDK7 than CDK9 and CDK2 and is inactive to CDK12 and CDK13. YKL-5-124 induces intense cell cycle arrest and inhibits E2F-driven gene expression with little effect on RNA polymerase II phosphorylation status. | ||
| M10843 | KB-0742 dihydrochloride | CDK |
| KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor against CDK9/cyclin T1 IC50 is 6 nM. KB-0742 dihydrochloride is selective for CDK9/cyclin T1, which is more than 50 times more selective than other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity. | ||
| M10879 | RGB-286638 | CDK |
| RGB-286638 is a potent CDK inhibitor that inhibits cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 activity,IC50 1, 2, 3, 4, 5 and 5 nM, respectively, and can inhibit GSK-3β, TAK1, Jak2 and MEK1.IC50 The values are 3, 5, 50, and 54 nM, respectively. | ||
| M10886 | Samuraciclib hydrochloride | CDK |
| Samuraciclib (ICEC0942, CT7001) is a novel oral CDK7 inhibitor with an IC50 of 40 nM. It has IC50 values for other CDK proteins such as CDK1, CDK2, CDK5 and CDK9 as 45, 15, 230 and 30 times higher than that of CDK7 IC50, respectively. ICEC0942 (CT7001) promotes cell cycle blocking and apoptosis. | ||
| M10930 | Dalpiciclib | CDK |
| SHR-6390 | ||
| Dalpiciclib (SHR-6390) is a highly selective, oral bioavailable inhibitor of CDK4/6 that is used against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM) is equivalent. SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb protein and inducing G1 cell cycle blocking. | ||
| M11449 | AG-024322 | COX |
| CS-1092 | ||
| Ag-024322 is a potent ATP-competitive pan-CDK inhibitor that inhibits THE Ki values of CDK1, CDK2, and CDK4 in the 1-3 nM range. Ag-024322 showed broad spectrum antitumor activity and clear target regulation in vivo. Ag-024322 induced apoptosis. | ||
| M13398 | BSJ-03-204 | PROTAC |
| BSJ-03-204 is a Cereblon ligand linked to THE CDK ligand PROTAC, which is an effective, selective cdK4/6 dual inhibitor based on Palbociclib. The IC50 of CDK4/D1 and CDK6/D1 were 26.9 nM and 10.4 nM, respectively. | ||
| M13594 | Alsterpaullone | CDK |
| 9-Nitropaullone; NSC 705701 | ||
| Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. | ||
| M13605 | AUZ 454 | CDK |
| K03861 | ||
| AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins. | ||
| M13611 | RGB-286638 free base | CDK |
| RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM. | ||
| M14897 | AMG 925 HCl | FLT3 |
| AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively. | ||
| M20882 | G1T38 | CDK |
| Lerociclib | ||
| Lerociclib (G1T38) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively. | ||
| M21169 | PF-60873600 | Others |
| The CDK2/4/6 inhibitor PF-60873600 has oral bioactivity with low Ki values of 0.09 nM, 1.3 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. | ||
| M21409 | FN-1501 | CDK |
| FN-1501 is a potent inhibitor of Fms-like receptor tyrosine kinase 3 (FLT3) and cyclin-dependent kinase (CDK), and the IC50 for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3 with IC50s of 2.47, 0.85, 1.96 and 0.28 nM, respectively. | ||
| M27775 | BS-194 | CDK |
| BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer. | ||
| M28381 | NSC 625987 | CDK |
| NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2. | ||
| M28687 | CDK8-IN-4 | CDK |
| CDK8-IN-4 is an inhibitor of CDK8, with an IC50 of 0.2 nM. | ||
| M28894 | Samuraciclib | CDK |
| CT7001; ICEC0942 | ||
| Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib has anti-tumor effects. | ||
| M29171 | CDK2-IN-4 | CDK |
| CDK2-IN-4 is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC50=86 uM). | ||
| M29520 | BSJ-04-132 | PROTAC |
| BSJ-04-132 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity. | ||
| M29539 | FMF-04-159-2 | CDK |
| FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively. | ||
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