SML3569

M4K2234

≥98% (HPLC)

• Synonym(s): 2-Fluoro-4-(5-(4-(4-isopropylpiperazin-1-yl)phenyl)-4-methylpyridin-3-yl)-6-methoxybenzamide
• Empirical Formula (Hill Notation): C₂₇H₃₁FN₄O₂
• CAS Number: 2421141-51-5
• Molecular Weight: 462.56
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: CC(C)N(CC1)CCN1C2=CC=C(C3=C(C)C(Cl)=CN=C3)C=C2
• 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

Description

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable