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AB222042

SB-525334, TGFBR1 inhibitor.

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MW 343.4 Da, Purity >98%. Cell permeable, potent, selective transforming growth factor beta 1 receptor (ALK5) (IC50 = 14.3 nM) and ALK4 (IC50 = 58.5 nM) inhibitor, with no activity at ALK2, 3 and 6 (IC50 > 10 μM). Blocks fibrosis and renal injury markers in a puromycin-induced nephritis model. Causes significant attenuation in Smad2/3 nuclear translocation and a decrease in CTGF-expressing cells, myofibroblast proliferation and type 1 collagen deposition resulting in an overall attenuation in bleomycin-induced pulmonary fibrosis.
1 Images
Chemical Structure - SB-525334, TGFBR1 inhibitor. (AB222042)
  • Chemical Structure

Lab

Chemical Structure - SB-525334, TGFBR1 inhibitor. (AB222042)

2D chemical structure image of ab222042, SB-525334, TGFBR1 inhibitor.

Key facts

CAS number

356559-20-1

Purity

>98%

Form

Solid

form

Molecular weight

343.4 Da

Molecular formula

C<sub>2</sub><sub>1</sub>H<sub>2</sub><sub>1</sub>N<sub>5</sub>

PubChem

9967941

Nature

Synthetic

Solubility

Soluble in DMSO to 85 mM

Biochemical name

6-(2-(tert-Butyl)-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl)quinoxaline

Biological description

Cell permeable, potent, selective transforming growth factor beta 1 receptor (ALK5) (IC50 = 14.3 nM) and ALK4 (IC50 = 58.5 nM) inhibitor, with no activity at ALK2, 3 and 6 (IC50 > 10 μM). Blocks fibrosis and renal injury markers in a puromycin-induced nephritis model. Causes significant attenuation in Smad2/3 nuclear translocation and a decrease in CTGF-expressing cells, myofibroblast proliferation and type 1 collagen deposition resulting in an overall attenuation in bleomycin-induced pulmonary fibrosis.

Canonical smiles

CC1=NC(=CC=C1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=NC=CN=C4C=C3

InChi

InChI=1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)

InChiKey

DKPQHFZUICCZHF-UHFFFAOYSA-N

IUPAC Name

6-[2-tert-butyl-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl]quinoxaline

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions
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Product protocols

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