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Submit ReviewNVP 2 is a potent and selective ATP-competitive CDK9 inhibitor (IC50 = 0.5 nM). Exhibits selectivity for CDK9 over a panel of 468 kinases, but inhibits DYRK1B (IC50 = 350 nM), displays <90% binding to CDK7 (IC50 >10 μM) and CDK13. Inhibits proliferation of MOLT4 cells in vitro. Induces apoptosis.
M. Wt | 513.07 |
Formula | C27H37ClN6O2 |
Storage | Store at -20°C |
Purity | ≥97% (HPLC) |
CAS Number | 1263373-43-8 |
PubChem ID | 66937006 |
InChI Key | XWQVQSXLXAXOPJ-QNGMFEMESA-N |
Smiles | COC[C@H](N[C@H]1CC[C@H](NC2=CC(C3=NC(NCC4(C#N)CCOCC4)=CC=C3)=C(C=N2)Cl)CC1)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 51.31 | 100 | |
ethanol | 51.31 | 100 |
The following data is based on the product molecular weight 513.07. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.95 mL | 9.75 mL | 19.49 mL |
5 mM | 0.39 mL | 1.95 mL | 3.9 mL |
10 mM | 0.19 mL | 0.97 mL | 1.95 mL |
50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
References are publications that support the biological activity of the product.
Olson et al (2018) Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat.Chem.Biol. 14 163 PMID: 29251720
Winter et al (2017) BET bromodomain proteins function as master transcription elongation factors independent of CDK9 recruitment. Mol.Cell 67 5 PMID: 28673542
If you know of a relevant reference for NVP 2, please let us know.
Keywords: NVP 2, NVP 2 supplier, NVP2, Cyclin-dependent, protein, kinases, inhibitors, inhibits, Cdk9, potent, selective, Kinase, Transcriptional, CDKs, 6535, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for NVP 2 include:
Brian et al (2022) YAP1 maintains active chromatin state in head and neck squamous cell carcinomas that promotes tumorigenesis through cooperation with BRD4. Cell Rep 39 110970 PMID: 35705032
Jeffrey D et al (2022) Nuclear RNA binding regulates TDP-43 nuclear localization and passive nuclear export. Cell Rep 40 111106 PMID: 35858577
Bernhard et al (2020) Localized Inhibition of Protein Phosphatase 1 by NUAK1 Promotes Spliceosome Activity and Reveals a MYC-Sensitive Feedback Control of Transcription. Mol Cell 77 1322-1339.e11 PMID: 32006464
Ignacio et al (2020) CDK8 Fine-Tunes IL-6 Transcriptional Activities by Limiting STAT3 Resident Time at the Gene Loci. Cell Rep 33 108545 PMID: 33357429
Johannes et al (2021) Ubiquitylation of MYC couples transcription elongation with double-strand break repair at active promoters. Mol Cell 81 830-844.e13 PMID: 33453168
Do you know of a great paper that uses NVP 2 from Tocris? Please let us know.
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