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Merck
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SML3069

Sigma-Aldrich

NVP-2

≥98% (HPLC)

同義詞:

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, NVP2

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About This Item

經驗公式（希爾表示法）:
C27H37ClN6O2
CAS號碼:
1263373-43-8
分子量：:
513.07
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

white to brown

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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

生化／生理作用

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).

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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分析證明 (COA)

Lot/Batch Number

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Phillip Wright et al.
Archives of toxicology, 93(3), 659-671 (2019-01-09)
Cyclin-dependent kinases (CDKs) are a family of kinases associated predominantly with cell cycle control, making CDK inhibitors interesting candidates for anti-cancer therapeutics. However, retinal toxicity (loss of photoreceptors) has been associated with CDK inhibitors, including the pan-CDK inhibitor AG-012896. The
Georg E Winter et al.
Molecular cell, 67(1), 5-18 (2017-07-05)
Processive elongation of RNA Polymerase II from a proximal promoter paused state is a rate-limiting event in human gene control. A small number of regulatory factors influence transcription elongation on a global scale. Prior research using small-molecule BET bromodomain inhibitors
Calla M Olson et al.
Nature chemical biology, 14(2), 163-170 (2017-12-19)
Cyclin-dependent kinase 9 (CDK9), an important regulator of transcriptional elongation, is a promising target for cancer therapy, particularly for cancers driven by transcriptional dysregulation. We characterized NVP-2, a selective ATP-competitive CDK9 inhibitor, and THAL-SNS-032, a selective CDK9 degrader consisting of

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