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
• Empirical Formula (Hill Notation): C₃₁H₃₀N₄O₅
• CAS Number: 1263131-92-5
• Molecular Weight: 538.59
• MDL number: MFCD25977098
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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

Description

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable