373278
Hh Signaling Antagonist XII, MRT-83
The Hh Signaling Antagonist XII, MRT-83 controls the biological activity of Hh pathway. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
Hh Signaling Antagonist XII, MRT-83, N-(2-Methyl-5-(3-(3,4,5-trimethoxybenzoyl)guanidino)phenyl)-(1,1ʹ-biphenyl)-4-carboxamide
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About This Item
Empirical Formula (Hill Notation):
C31H30N4O5
CAS Number:
Molecular Weight:
538.59
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow-white
solubility
DMSO: 100 mg/mL
shipped in
wet ice
storage temp.
2-8°C
SMILES string
O=C(NC(NC1=CC(NC(C2=CC=C(C3=CC=CC=C3)C=C2)=O)=C(C)C=C1)=N)C4=CC(OC)=C(C(OC)=C4)OC
General description
A cell-permeable acylguanidine compound that is shown to block Hh signaling and act as a potent, reversible and high-affinity Smo (Smoothened) antagonist. Displays 20-60 -fold greater potency than Cyclopamine (Cat. No. 239803 ) and competitively inhibits bodipy-cyclopamine binding to Smo (IC50 = 4.6 and 14 nM in HEK293-hSMO and HEK293-mSMO cells, respectively). Represses ShhN (N-myristoylated Shh) signaling (IC50 = 15 nM for Gli-dependent luciferase activity in Shh-light2 cells) and SAG-(Cat. Nos. 566660 & 566661) induced C3H10T1/2 cell differentiation (IC50 = 10 nM in an alkaline phosphatase activity assay). Inhibits ShhN (3 nM) and SAG (10 nM)-mediated proliferation of rat cerebellar granule cell precursors (IC50 ~ 3 and 6 nM, respectively).
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.
Other Notes
Roudaut, H., et al. 2011. Mol. Pharmacol.79, 453.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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