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Merck

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:
1263131-92-5
Molecular Weight:
538.59
MDL number:
MFCD25977098
UNSPSC Code:
12352200

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

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 Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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