BET PROTAC SIM1

Chemical Structure : BET PROTAC SIM1

CAS No.: 2719051-84-8

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货号: PC-23323Not For Human Use, Lab Use Only.

规格	价格	库存
5 mg	￥3280	In stock
10 mg	￥5280	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	1618.82
分子式	C79H98Cl2N14O13S3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
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)

参考文献

1. Satomi Imaide, et al. Nat Chem Biol. 2021 Nov;17(11):1157-1167.

BET PROTAC SIM1

生物&药学活性

物理化学性质&存储条件

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