1. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  2. JAK
  3. NVP-BSK805 trihydrochloride

NVP-BSK805 trihydrochloride 是一种 ATP 竞争性的 JAK2 抑制剂,对 JAK2 JH1 (JAK 同源 1),JAK1 JH1,JAK3 JH1,和 TYK2 JH1 的 IC50 值分别为 0.48 nM,31.63 nM,18.68 nM 和 10.76 nM。

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NVP-BSK805 trihydrochloride Chemical Structure

NVP-BSK805 trihydrochloride Chemical Structure

CAS No. : 2320258-95-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively[1].

IC50 & Target[1]

JAK2 JH1

0.48 nM (IC50)

JAK2(V617F)

0.56 nM (IC50)

FL JAK2 wt

0.58 nM (IC50)

TYK2 JH1

18.68 nM (IC50)

JAK1 JH1

31.68 nM (IC50)

体外研究
(In Vitro)

NVP-BSK805 trihydrochloride (BSK 805) is a JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. NVP-BSK805 trihydrochloride inhibits the full-length wild-type JAK2 (FL JAK2 wt) and FL JAK2 V617F activity, with IC50s of 0.58 ± 0.03 and 0.56 ± 0.04 nM. NVP-BSK805 trihydrochloride is ATP-competitive, with aclculated Ki of 0.43 ± 0.02 nM. NVP-BSK805 trihydrochloride suppresses the growth of JAK2V617F-bearing acute myeloid leukemia cell lines with GI50 of <100 nM. NVP-BSK805 trihydrochloride blocks the STAT5 phosphorylation at ≥100 nM concentrations, and shows a bias for JAK2 over JAK1 and JAK3 inhibition in the JAK2V617F-mutant cell lines[1].
NVP-BSK805 trihydrochloride (5 μM) improves P-gp inhibitory activity. NVP-BSK805 trihydrochloride increases sensitization of drug-resistant KBV20C cancer cells to VIC treatment at 10 μM, and such an effect is more effective than a 5 μM dose[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NVP-BSK805 trihydrochloride (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-driven mouse model[1].
NVP-BSK805 trihydrochloride (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

599.93

Formula

C27H31Cl3F2N6O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NVP-BSK805 trihydrochloride
目录号:
HY-14722C
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