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Merck

616452

RepSox

≥95% (HPLC), solid, TGF-β RI kinase inhibitor, Calbiochem

Synonym(s):

TGF-β RI Kinase Inhibitor II, ALK5 Inhibitor II, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor II, 2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine

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About This Item

Empirical Formula (Hill Notation):
C17H13N5
CAS Number:
446859-33-2
Molecular Weight:
287.32
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
MFCD09037561

Key Documents

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Product Name

TGF-β RI Kinase Inhibitor II, TGF-β RI Kinase Inhibitor II, CAS 446859-33-2, is a cell-permeable, potent, reversible, ATP-competitive inhibitor of TGF-β R1 kinase (IC50 = 23 nM and 4 nM for ALK5 binding & auto-phosphorylation).

SMILES string

[nH]1ncc(c1c4nc(ccc4)C)c2nc3c(nccc3)cc2

InChI

1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)

InChI key

LBPKYPYHDKKRFS-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

potency

23 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 5 mg/mL
methanol: 5 mg/mL

shipped in

ambient

Quality Level

100

storage temp.

2-8°C

Biochem/physiol Actions

Cell permeable: yes
Primary Target
ALKS binding
Product competes with ATP.
Secondary Target
ALK 5 auto phosphorylation (IC₅₀ = 4 nM)

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable naphthyridinyl pyrazolo compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of TGF-β type I receptor (ALK5; IC50 = 23 nM, 4 nM and 18 nM for ALK5 binding, ALK5 auto-phosphorylation and TGF-β cellular assay in HepG2 cells, respectively). Minimally affects a panel of 9 closely related kinases including p38 MAPK at IC50 >16 µM. Also available as a 50 mM solution in DMSO (Cat. No. 508158).

Other Notes

Gellibert, F., et al. 2004. J. Med. Chem.47, 4494.
Ichida, J. K., et al. 2009. Cell Stem Cell 5, 491.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Xiao-Jun Li et al.
Science advances, 8(6), eabj7651-eabj7651 (2022-02-12)
Hair cell (HC) loss within the inner ear cochlea is a leading cause for deafness in humans. Before the onset of hearing, immature supporting cells (SCs) in neonatal mice have some limited capacity for HC regeneration. Here, we show that

Global Trade Item Number

SKUGTIN
616452-2MGCN04055977185829

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