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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.
分子量 | 513.07 |
公式 | C27H37ClN6O2 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 51.31 | 100 | |
ethanol | 51.31 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: NVP 2, NVP 2 supplier, NVP2, Cyclin-dependent, protein, kinases, inhibitors, inhibits, Cdk9, potent, selective, Kinase, Transcriptional, CDKs, 6535, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NVP 2 的部分引用包括:
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
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