CWHM-12

  Cat. No.:  DC9278   Featured
Chemical Structure
1564286-55-0
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Field of application
CWHM-12 a novel small molecule inhibitor of αV integrins with IC50s of 1.8/0.8/1.5/0.2 nM for αvβ1/αvβ3/αvβ8; less potency on αvβ5(IC50=61 nM) and on inhibition on αIIbβ3/α2β1/α10β1.
Cas No.: 1564286-55-0
Chemical Name: CWHM-12
Synonyms: CWHM12;CWHM-12;(3S)-3-(3-bromo-5-(tert-butyl)phenyl)-3-(2-(3-hydroxy-5-((5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino)benzamido)acetamido)propanoic acid;CWHM 12;GTPL10495;AOB2397;(3S)-3-(3-bromo-5-tert-butylphenyl)-3-[[2-[[3-hydroxy-5-[(5-hydroxy-1,4,5,6-tetrahydropyrimidin-2-yl)amino]benzoyl]amino]acetyl]amino]propanoic acid;BDBM50497716;(3S)-3-(3-bromo-5-tert-but
SMILES: BrC1=C([H])C(=C([H])C(=C1[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])[C@]([H])(C([H])([H])C(=O)O[H])N([H])C(C([H])([H])N([H])C(C1C([H])=C(C([H])=C(C=1[H])N([H])C1=NC([H])([H])C([H])(C([H])([H])N1[H])O[H])O[H])=O)=O
Formula: C26H32BrN5O6
M.Wt: 590.4662
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
In Vivo: Mice are treated with CCl4 for 3 weeks to establish fibrotic disease and then treated with CWHM-12 (CWHM 12) or vehicle for the final 3 weeks of CCl4. CWHM-12 significantly reduces liver fibrosis even after fibrotic disease have been established. Digital image quantitation demonstrates significantly reduced p-SMAD3 signaling in the livers of CWHM-12 treated mice compare to controls, demonstrating that the protection from CCl4-induced hepatic fibrosis observed in CWHM-12 treated mice is due at least in part to a reduction in TGF-β activation by αv integrins. Besides, administration of CWHM-12 significantly inhibited progression of pulmonary fibrosis[1].
In Vitro: CWHM-12 (CWHM 12) also less potently inhibits αvβ5 (IC50=61 nM) and αIIbβ3/α2β1/α10β1 (IC50>5000 nM). CWHM-12 demonstrates high potency against all of the five possible β subunit binding partners (αvβ1, αvβ3, αvβ5, αvβ6 and αvβ8) in in vitro ligand-binding assays, with somewhat less potency against αvβ5 than against the other αv integrins[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC9278 CWHM-12 CWHM-12 a novel small molecule inhibitor of αV integrins with IC50s of 1.8/0.8/1.5/0.2 nM for αvβ1/αvβ3/αvβ8; less potency on αvβ5(IC50=61 nM) and on inhibition on αIIbβ3/α2β1/α10β1.
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