A01, Smurf1 E3 Ubiquitin Ligase Inhibitor

A01 is a potent and selective Smurf1 E3 ubiquitin ligase inhibitor with Kd ~3.7 nM. It attenuates Smurf1-mediated Smad 1/5 degradation and enhances BMP signaling. It also potentiates BMP-2-induced osteoblastic activity in C2C12 myoblasts and MC3T3-E1 osteoblast precursor cells.

Product information

CAS Number: 1007647-73-5

Molecular Weight: 512.93

Formula: C22H20ClF3N4O3S

Chemical Name: (4-((4-chloro-3-(trifluoromethyl)phenyl)sulfonyl)piperazin-1-yl)(4-(5-methyl-1H-pyrazol-1-yl)phenyl)methanone

Smiles: CC1=CC=NN1C1C=CC(=CC=1)C(=O)N1CCN(CC1)S(=O)(=O)C1=CC(=C(Cl)C=C1)C(F)(F)F

InChiKey: QFYLTUDRXBNZFQ-UHFFFAOYSA-N

InChi: InChI=1S/C22H20ClF3N4O3S/c1-15-8-9-27-30(15)17-4-2-16(3-5-17)21(31)28-10-12-29(13-11-28)34(32,33)18-6-7-20(23)19(14-18)22(24,25)26/h2-9,14H,10-13H2,1H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

A01 was used at 1-10 µM final concentration in various in vitro assays.

References:

1. Cao Y, et al. Selective small molecule compounds increase BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. (2014) Sci Rep. 4:4965.

Products are for research use only. Not for human use.