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NVP-2

Catalog No. T16363   CAS 1263373-43-8

NVP-2 is an effective and selective ATP-competitive cyclin-dependent kinase 9 (CDK9) probe. NVP-2 induces cell apoptosis. NVP-2 inhibits CDK9/CycT activity (IC50: 0.514 nM). NVP-2 shows inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases (IC50: 0.584 μM, 0.706 μM, and 0.605 μM, respectively).

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NVP-2 Chemical Structure
NVP-2, CAS 1263373-43-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 50.00
2 mg In stock $ 72.00
5 mg In stock $ 122.00
10 mg In stock $ 213.00
25 mg In stock $ 463.00
50 mg In stock $ 683.00
100 mg In stock $ 973.00
1 mL * 10 mM (in DMSO) In stock $ 137.00
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Purity: 99.76%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NVP-2 is an effective and selective ATP-competitive cyclin-dependent kinase 9 (CDK9) probe. NVP-2 induces cell apoptosis. NVP-2 inhibits CDK9/CycT activity (IC50: 0.514 nM). NVP-2 shows inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases (IC50: 0.584 μM, 0.706 μM, and 0.605 μM, respectively).
Targets&IC50 CDK9:0.5 nM (IC50)
In vitro NVP-2 has an anti-proliferation of leukemia cells, suppresses KOPT-K1, Jurkat, P12-ICHIKAWA, DU.528, MOLT 16, HSB-2, PF-382, SKW-3, SUP-T11, DND-41 and HPB-ALL cells with IC50 values of 0.1688 μM, 0.1233 μM,0.5736 μM,0.1575 μM, 0.1620 μM,0.1585 μM, 0.1808 μM, 0.2589 μM, 0.0918 μM and 0.3023 μM, respectively. NVP-2 (0-10 nM; 72 hours) shows CRBN-dependent anti-proliferative and pro-apoptotic effects in MOLT4 cells (IC50: 9 nM). NVP-2 (250 nM; 24 hours) causes cell apoptosis in MOLT4 cells, upregulates caspase-3 and γH2A.X expression. However, while the compound washout significantly reduces the degree of apoptosis induced by NVP-2. NVP-2 (250 nM-1 μM; 6 hours) engages CDK9 in wildtype and CRBN?/? MOLT4 cells at all concentrations, while CDK2 and CDK7 are unaffected.
Molecular Weight 513.07
Formula C27H37ClN6O2
CAS No. 1263373-43-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (194.91 mM)

TargetMolReferences and Literature

1. Winter GE, et al. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment.Mol Cell. 2017 Jul 6;67(1):5-18.e19.

TargetMolCitations

1. Shan X, Jiang R, Gou D, et al.Identification of a diketopiperazine‐based O‐GlcNAc transferase inhibitor sensitizing hepatocellular carcinoma to CDK9 inhibition.The FEBS Journal.2023 2. Wang J, Wen Y, Zhang Y, et al.An interpretable artificial intelligence framework for designing synthetic lethality-based anti-cancer combination therapies.Journal of Advanced Research.2023

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Cell Cycle Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Anti-Pancreatic Cancer Compound Library Covalent Inhibitor Library Apoptosis Compound Library

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Keywords

NVP-2 1263373-43-8 Apoptosis Cell Cycle/Checkpoint CDK inhibit Cyclin dependent kinase NVP2 Inhibitor CRBN CDK9 Leukemia NVP 2 inhibitor

 

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