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Merck

204001

BX-795 hydrochloride

BX-795, also referenced under CAS 702675-74-9, modulates the biological activity of multiple kinases. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

別名:

BX-795, AMPK Related Kinase 5 Inhibitor I, ARK5 Inhibitor I, NUAK Kinase Inhibitor I, NUAK1 Inhibitor I, SnF1 Like Kinase-1 Inhibitor I, N-(3-((5-Iodo-4-((3-(2-thienylcarbonyl)amino)propyl)amino)-2-pyrimidinyl)amino)phenyl)-1-pyrrolidinecarboxamide, Aurora Kinase, N-(3-((5-Iodo-4-((3-(2-thienylcarbonyl)amino)propyl)amino)-2-pyrimidinyl)amino)phenyl)-1-pyrrolidinecarboxamide, AMPK Related Kinase 5 Inhibitor I, ARK5 Inhibitor I, NUAK Kinase Inhibitor I, NUAK1 Inhibitor I, SnF1 Like Kinase-1 Inhibitor I, Aurora Kinase Inhibitor VIII

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実隓匏ヒル衚蚘法:
C23H26IN7O2S
CAS番号:
分子量:
591.47
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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補品名

BX-795, BX-795, also referenced under CAS 702675-74-9, modulates the biological activity of multiple kinases. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Quality Segment

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

pale yellow

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

Ic1c(nc(nc1)Nc3cc(ccc3)NC(=O)N4CCCC4)NCCCNC(=O)c2[s]ccc2

InChI

1S/C23H26IN7O2S/c24-18-15-27-22(30-20(18)25-9-5-10-26-21(32)19-8-4-13-34-19)28-16-6-3-7-17(14-16)29-23(33)31-11-1-2-12-31/h3-4,6-8,13-15H,1-2,5,9-12H2,(H,26,32)(H,29,33)(H2,25,27,28,30)

InChI key

VAVXGGRQQJZYBL-UHFFFAOYSA-N

General description

A cell-permeable aminopyrimidine compound that acts as a potent, ATP-competitive and reversible multi-kinase inhibitor (IC50 = 11 nM for PDK1 at ≀ 10 µM of ATP; IC50 = 5 , 6, 19, 31, 41 and 111 nM for NUAK1, TBK1, MARK4, Aurora B, IKKε and PDK1 at 100 µM of ATP, respectively) and displays 50-fold greater selectivity over Cdk2/E, EGFR, GSK-3β, IR, c-Kit, PKA, PKC, TAK1 and VEGFR. Shown to block PDK1/Akt signaling, induce growth arrest and apoptosis in PC-3 and MDA-468 cells (IC50 = 0.25 and 0.75 µM, respectively); further, inhibit phosphorylation (pSer396), nuclear translocation and transcriptional activity of IRF3 and reduce IFN-β production in stimulated macrophages.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Clark, K., et al. 2009. J. Biol. Chem.284, 14136.
Tamgumcy, T., et al. 2008. Exp. Cell Res.314, 2299.
Feldman, R.I., et al. 2005. J. Biol. Chem.280, 19867.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)


保管分類

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


適甚法什

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Substances Subject to be Indicated Names

ishl_indicated

Substances Subject to be Notified Names

ishl_notified



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