BLU0588 | PRKA inhibitor | Probechem Biochemicals

Chemical Structure : BLU0588

CAS No.: 2810747-78-3

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BLU0588 (BLU-0588)

货号: PC-26711Not For Human Use, Lab Use Only.

BLU0588 is a potent, selective and orally acitve protein kinase A (PKA) alpha catalytic subunit (PRKACA) inhibitor with IC50 of 1 nM and Kd of 4 nM.

规格	价格	库存
5 mg	￥1980	In stock
10 mg	￥2980	In stock
25 mg	￥4880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

BLU0588 is a potent, selective and orally acitve protein kinase A (PKA) alpha catalytic subunit (PRKACA) inhibitor with IC50 of 1 nM and Kd of 4 nM.
BLU0588 exhibits good to moderate selectivity against closely related AGC kinase family members and excellent overall kinome selectivity profiles.
BLU0588 exhibits cellular IC50 value of 25.0 nM for inhibition of VASP Ser157 phosphorylation in forskolin-stimulated Huh7 cells.
BLU0588 treatment led to a dose-dependent reduction in phosphorylated VASP in FLC PDX spheroid cultures.
BLU0588 at 30 mg/kg and 75 mg/kg once daily (QD) inhibits PRKACA in vivo, inhibits tumor growth in mice harboring FLC PDX tumors.

物理化学性质&存储条件

分子量	423.52
分子式	C26H25N5O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-((1R,2R)-2-(Pyrrolidin-1-yl)-2,3-dihydro-1H-inden-1-yl)-6-(1H-pyrrolo[2,3-b]pyridin-4-yl)nicotinamide

参考文献

1. Schalm SS, et al. Gastro Hep Adv. 2022 Nov 8;2(3):307-321.

2. Bruystens JGH, et al. Proc Natl Acad Sci U S A. 2026 May 12;123(19):e2536312123.

BLU0588 (BLU-0588)

生物&药学活性

物理化学性质&存储条件

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BLU0588 (BLU-0588)

生物&药学活性

物理化学性质&存储条件

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