Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : BET PROTAC SIM1
CAS No.: 2719051-84-8
Catalog No.: PC-23323Not For Human Use, Lab Use Only.
BET PROTAC SIM1 is a highly potent, von Hippel-Lindau (VHL)-based BET trivalent PROTAC degrader with preference for BRD2 with DC50 of 1.1 nM, 3.3 nM and 0.7 nM for RD2, BRD3, BRD4 in HEK293 cells, potently inhibits cell viability of MV4;11 AML cell line with IC50 of 1.1 nM (48 h).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $328 | In stock | |
| 10 mg | $528 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
BET PROTAC SIM1 is a highly potent, von Hippel-Lindau (VHL)-based BET trivalent PROTAC degrader with preference for BRD2 with DC50 of 1.1 nM, 3.3 nM and 0.7 nM for RD2, BRD3, BRD4 in HEK293 cells, potently inhibits cell viability of MV4;11 AML cell line with IC50 of 1.1 nM (48 h).
SIM1 exhibits Dmax50 values of 60-400pM and BET family degradation preference of BRD2>BRD4>BRD3 on both λmax and Dmax50.
SIM1 shows more efficacious apoptosis-induced cytotoxicity in BET-sensitive cancer cell lines than bivalent PROTACs or inhibitors.
SIM1 simultaneously engages with high avidity both BET bromodomains in a cis intramolecular fashion and forms a 1:1:1 ternary complex with VHL, exhibiting positive cooperativity and high cellular stability with prolonged residence time.
| M.Wt | 1618.82 | |
| Formula | C79H98Cl2N14O13S3 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
N,N'-(11-((2-(((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)methyl)-11-methyl-3,6,9,13,16,19-hexaoxahenicosane-1,21-diyl)bis(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide) |
|
1. Satomi Imaide, et al. Nat Chem Biol. 2021 Nov;17(11):1157-1167.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
