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Merck

616452

RepSox

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

Synonyme(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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A propos de cet article

Formule empirique (notation de Hill) :
C17H13N5
Numéro CAS:
446859-33-2
Poids moléculaire :
287.32
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
MFCD09037561

Principaux documents

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Nom du produit

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

Catégories apparentées

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificats d'analyse (COA)

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The Journal of pathology, 244(3), 367-379 (2017-12-14)
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Cancer cell international, 22(1), 358-358 (2022-11-16)
Tumor suppressor CYLD dysfunction by loss of its expression, triggers malignant transformation, especially drug resistance and tumor invasion/metastasis. Although loss of CYLD expression is significantly associated with poor prognosis in a large variety of tumors, no clinically-effective treatment for CYLD-negative
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Growing evidence suggests an association between epithelial-mesenchymal transition (EMT), a hallmark of tumor malignancy, and chemoresistance to a number of anti-cancer drugs. However, the mechanism of EMT induction in the process of acquiring anti-cancer drug resistance remains unclear. To address
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Stem cell reports, 19(7), 973-992 (2024-06-29)
Genetic differences between pluripotent stem cell lines cause variable activity of extracellular signaling pathways, limiting reproducibility of directed differentiation protocols. Here we used human embryonic stem cells (hESCs) to interrogate how exogenous factors modulate endogenous signaling events during specification of
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Cell metabolism, 35(5), 887-905 (2023-04-20)
Cellular exposure to free fatty acids (FFAs) is implicated in the pathogenesis of obesity-associated diseases. However, there are no scalable approaches to comprehensively assess the diverse FFAs circulating in human plasma. Furthermore, assessing how FFA-mediated processes interact with genetic risk
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