LY364947 | 2646

LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC₅₀ value of 59 nM. LY364947 only weakly inhibits TGF-β RII (IC₅₀ = 400 nM), p38 MAPK (IC₅₀ = 740 nM), and mixed lineage kinase-7 (MLK-7; IC₅₀ = 1,400 nM).It inhibits TGF-β-induced cell growth (IC₅₀ = 89 nM) in NIH 3T3 mouse fibroblasts and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.

LY364947 is a selective inhibitor of TGF-β RI (TGFR-I, TβR-I, ALK-5), with an IC₅₀ value of 59 nM. LY364947 only weakly inhibits TGF-β RII (IC₅₀ = 400 nM), p38 MAPK (IC₅₀ = 740 nM), and mixed lineage kinase-7 (MLK-7; IC₅₀ = 1,400 nM).It inhibits TGF-β-induced cell growth (IC₅₀ = 89 nM) in NIH 3T3 mouse fibroblasts and TGF-β-directed Smad phosphorylation, synthesis of fibronectin, PAI-1 and uPA protein, and matrigel invasion in MDA-MB-231 cells.

2646 | LY364947 DataSheet

Alternate Name/Synonyms: 4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline; HTS 466284

Appearance: Off-white solid

Formulation: N/A

CAS Number: 396129-53-6

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₁₇H₁₂N₄

Molecular Weight: 272.31

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (~ 25 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A selective TGF-β RI (ALK-5) inhibitor

MDL Number: N/A

PubChem CID: 447966

SMILES: C1=CC=C2C(=C1)C(=CC=N2)C3=C(NN=C3)C4=CC=CC=N4

InChi: InChI=1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21)

InChi Key: IBCXZJCWDGCXQT-UHFFFAOYSA-N