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Biochem/physiol Actions
ATP-competitive, highly potent and selective cyclin-dependent kinase CDK9 inhibitor.
NVP-2 is an ATP-competitive, highly potent and selective cyclin-dependent kinase CDK9 inhibitor (human Cdk9/CycT1 IC50 = 0.3 nM with 6 μM ATP; DYRK1B IC50 = 350 nM; CDK7 IC50 >10 ?M; 0-63% inhibition of 366 other kinases at 1 μM, including CDK2/3/4/5/8). NVP-2 inhibits RNA Pol II-mediated transcription by blocking Cdk9-dependent RNA Pol II CTD phosphorylation (250 nM for 1-24 hrs; MOLT4 cells), displaying higher apoptosis-inducing and antiproliferation efficacy than the CDK2/7/9 inhibitor SNS-032 (BMS-387032) in leukemia cultures (MOLT4 IC50 = 9 nM/NVP-2 vs. 173 nM/SNS-032).
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to brown |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | C[C@H](COC)N[C@@H]1CC[C@@H](NC2=NC=C(Cl)C(C3=NC(NCC4(CCOCC4)[N+]#[C-])=CC=C3)=C2)CC1 |
| InChI | 1S/C27H37ClN6O2/c1-19(17-35-3)32-20-7-9-21(10-8-20)33-26-15-22(23(28)16-30-26)24-5-4-6-25(34-24)31-18-27(29-2)11-13-36-14-12-27/h4-6,15-16,19-21,32H,7-14,17-18H2,1,3H3,(H,30,33)(H,31,34)/t19-,20-,21-/m1/s1 |
| InChI key | OPMDDHBKBFCAJY-NJDAHSKKSA-N |
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¥ 4164.19
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¥ 1683.78
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¥ 2013.69
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¥ 2068.25
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¥ 8293.41
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