[CAS NO. 1467093-03-3]  Adavivint (SM04690)

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PRODUCTS SPECIFICATIONS [1467093-03-3]

Catalog
SLK-S8761
Brand
Selleck
CAS
1467093-03-3

DESCRIPTION [1467093-03-3]

Overview

MDLMFCD30489411
Molecular Weight505.55
Molecular FormulaC29H24FN7O
SMILESCC(C)CC(NC1=CC(C2=CC3=C(NN=C3C(N4)=NC5=C4C=NC=C5C6=CC=CC(F)=C6)C=C2)=CN=C1)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.9780 mL9.8902 mL19.7804 mL
5 mM0.3956 mL1.9780 mL3.9561 mL
10 mM0.1978 mL0.9890 mL1.9780 mL
50 mM0.0396 mL0.1978 mL0.3956 mL

Description

Adavivint (SM04690,Lorecivivint) is a potent and specific inhibitor of with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.

Targets

Wnt [1]

In vitro

Bone-marrow-derived hMSCs (CD29+, CD44+ CD166+ CD105+ CD45-), treated with SM04690, show a dose-dependent decrease in the expression of Wnt pathway genes (ASCL1, LEF1, TCF7L2, TCF7, C-262 MYC and AXIN2). M04690 also inhibits the expression of AXIN2, TCF7 and LEF1 in hMSCs and AXIN2 and LGR5 in IEC6 (intestinal stem cells sensitive to Wnt activation) when the Wnt pathway is selectively activated using either Wnt3a or a GSK3β inhibitor, CHIR-99021. SM04690 has minimal effects on the non-canonical Wnt pathway and the BMP pathway. SM04690 protects chondrocytes from catabolic breakdown in vitro.