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Enzymes for Research, Diagnostic and Industrial Use

Vismodegib (GDC-0449)

Cat No.
CEI-0201
Description
Vismodegib (GDC-0449) can inhibit hedgehog and p-gp with 3 nM and 3 uM.
CAS No.
879085-55-9
Molecular Weight
421.3
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
Hedgehog, p-gp
Molecular Formula
C19H14Cl2N2O3S
Chemical Name
2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide
Solubility
DMSO 84 mg/mL Water
In vitro
GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide) is a potent inhibitor of the hedgehog pathway.Treating with GDC-0449 can lead to rapid (although transient) regression of the tumor and reduction of symptoms in metastatic medulloblastoma. GDC-0499 inhibited cell viability and induced apoptosis in three pancreatic cancer cell lines and pancreatic CSCs. This inhibitor also suppressed cell viability, Gli-DNA binding and transcriptional activities, and induced apoptosis through caspase-3 activation and PARP cleavage in pancreatic CSCs. GDC-0449-induced apoptosis in CSCs showed increased Fas expression and decreased expression of PDGFRalpha. And Bcl-2 was down-regulated whereas TRAIL-R1/DR4 and TRAIL-R2/DR5 expression was increased following the treatment of CSCs with GDC-0449.
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