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NVP 2

Cat. No. 6535 5 Citations Submit a Review Datasheet / COA / SDS
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Description: Potent and selective ATP-competitive CDK9 inhibitor
Chemical Name: 4-[[[5'-Chloro-2'-[[trans-4-[[(1R)-2-methoxy-1-methylethyl]amino]cyclohexyl]amino][2,4'-bipyridin]-6-yl]amino]methyl]tetrahydro-2H-pyran-4-carbonitrile
Purity: ≥97% (HPLC)
Datasheet
Citations (5)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for NVP 2

NVP 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.

Technical Data for NVP 2

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.

Solubility Data for NVP 2

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.31 100
ethanol 51.31 100

Preparing Stock Solutions for NVP 2

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for NVP 2

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.

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5 Citations for NVP 2

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

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

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

Do you know of a great paper that uses NVP 2 from Tocris? Please let us know.

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