SML3569
M4K2234
≥98% (HPLC)
别名:
2-Fluoro-4-(5-(4-(4-isopropylpiperazin-1-yl)phenyl)-4-methylpyridin-3-yl)-6-methoxybenzamide
InChI
1S/C19H24ClN3/c1-14(2)22-8-10-23(11-9-22)17-6-4-16(5-7-17)18-12-21-13-19(20)15(18)3/h4-7,12-14H,8-11H2,1-3H3
InChI key
UFAWMCANSWTKEG-UHFFFAOYSA-N
SMILES string
CC(C)N(CC1)CCN1C2=CC=C(C3=C(C)C(Cl)=CN=C3)C=C2
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
M4K2234 is a potent and selective TGF-β type I receptors ALK1/ACVRL1 & ALK2/ACVR1 inhibitor (IC50 = 7/14 nM, [ATP] = 10 mM) that inhibits TNIK and ALK6/BMPR1B only at higher concentrations (IC50 = 41 & 88 nM, respectively) with good kinome selectivity over >370 other kinases, including ALK3/BMPR1A, ALK4/ACVR1B, ALK5/TGFBR1 (IC50 = 0.165, 1.66, 1.95 μM, respectively). M4K2234 inhibits cellular phospho-SMAD1/5/8 induction by 10 ng/mL BMP-7 and phospho-SMAD2 induction by either 10 ng/mL activin A or 100 ng/mL TGF-β1 with good target selectivity by cellular NanoBRET assays (ALK1/2 IC50 = 83/13 nM).
Potent and selective TGF-β type I receptors ALK1/ACVRL1 & ALK2/ACVR1 inhibitor.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Deeba Ensan et al.
Journal of medicinal chemistry, 63(9), 4978-4996 (2020-05-06)
Diffuse intrinsic pontine glioma is an aggressive pediatric cancer for which no effective chemotherapeutic drugs exist. Analysis of the genomic landscape of this disease has led to the identification of the serine/threonine kinase ALK2 as a potential target for therapeutic
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