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BX-795 is a multi-kinase inhibitor that is an ATP-competitive inhibitor of 3-phosphoinositide-dependent protein kinase 1 (PDK1) and TANK-binding kinase 1 (TBK1, IC50s = 6 and 11 nM, respectively). It also inhibits the CAMK family kinases AMPK-related kinase 5 (NUAK1, IC50 = 5 nM) and microtubule affinity-regulating kinase 1 (MARK1), MARK2, MARK3, and MARK4 (IC50s = 55, 53, 81, and 19 nM, respectively), as well as the MAP3K kinases mixed-lineages kinase 1 (MLK1), MLK2, and MLK3 (IC50s = 50, 46, and 42 nM, respectively). BX-795 is selective for these kinases over five additional kinases (IC50s = >1,100 nM) but does inhibit the receptor tyrosine kinase VEGFR, as well as IkappaB kinase epsilon (I??epsilon) and Aurora B kinase (IC50s = 41 and 31 nM, respectively). It inhibits phosphorylation of Akt at Thr308 and p70 ribosomal S6 kinase 1 (p70S6K1) at Thr389 in PC3 prostate cancer cells (IC50 = 300 nM). BX-795 (1 µM) also inhibits the secretion of IFN-beta induced by LPS or poly(I:C) in RAW 264.7 macrophages. It inhibits the proliferation of PC3 prostate and MDA-MB-468 breast cancer cells (IC50s = 250 and 720 nM, respectively). BX-795 (5 µM) inhibits the proliferation of PDK1-/- murine embryonic stem cells expressing either wild-type PDK1 or PDK1 with an alanine-to-glycine (L159G) mutation.Formal Name: N-[3-[[5-iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide. CAS Number: 702675-74-9. Molecular Formula: C23H26IN7O2S. Formula Weight: 591.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 12.5 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 11.1 mg/ml. lambdamax: 247 nm. SMILES: [H]N(CCCN(C(C1=CC=CS1)=O)[H])C2=C(I)C=NC(N([H])C3=CC(N(C(N4CCCC4)=O)[H])=CC=C3)=N2. InChi Code: 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.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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