Description
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: ≥12 months 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:
- 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.
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