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SIM1

PubChem编号: 156022820

有货

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库存信息

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货号 (SKU)	包装规格	是否现货	价格	数量
S613585-5mg	5mg	期货
S613585-25mg	25mg	期货

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bromodomain containing 2 Inhibitor

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基本描述

英文名称	SIM1
别名	compound 3
英文别名	compound 3

名称和标识符

IUPAC Name	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)
INCHI	InChI=1S/C79H98Cl2N14O13S3/c1-46-49(4)110-76-66(46)68(54-16-20-57(80)21-17-54)86-60(72-91-89-51(6)94(72)76)37-63(97)82-24-26-102-28-30-104-32-34-106-42-79(11,44-108-41-65(99)88-71(78(8,9)10)75(101)93-40-59(96)36-62(93)74(100)84-39-53-12-14-56(15-13-53)70-48(3)85-45-109-70)43-107-35-33-105-31-29-103-27-25-83-64(98)38-61-73-92-90-52(7)95(73)77-67(47(2)50(5)111-77)69(87-61)55-18-22-58(81)23-19-55/h12-23,45,59-62,71,96H,24-44H2,1-11H3,(H,82,97)(H,83,98)(H,84,100)(H,88,99)/t59-,60+,61+,62+,71-/m1/s1
InChi Key	RARNTROXRCXFHV-CMRSQZKGSA-N
Canonical SMILES	O[C@@H]1C[C@H](N(C1)C(=O)[C@H](C(C)(C)C)NC(=O)COCC(COCCOCCOCCNC(=O)C[C@H]1c2n(c3c(C(=N1)c1ccc(cc1)Cl)c(c(s3)C)C)c(nn2)C)(COCCOCCOCCNC(=O)C[C@H]1c2n(c3c(C(=N1)c1ccc(cc1)Cl)c(c(s3)C)C)c(nn2)C)C)C(=O)NCc1ccc(cc1)c1c(ncs1)C
PubChem CID	156022820

数据库链接

PubChem CID	156022820

关联配体

Ligand ID	11777
名称	SIM1
别名	compound 3 [PMID: 34675414]
类别	Synthetic organic
学名	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)
生物活性评价	SIM1 binds to immobilised VHL with a K_d of 624 nM . The binding affinity of SIM1/BRD2 complexes for VHL is higher at ~40 nM.In vitroSIM1 degrades BRD2 with a DC₅₀ value of 1.1 nM, and reduces viability of MV4;11 AML cells with an IC₅₀ of 1.1 nM.
评价	SIM1 is a first-in-class trivalent PROTAC molecule . It contains two bromo and extra terminal (BET) domain inhibitor ligand components and a von Hippel-Lindau (VHL) ligand domain which are tethered together by a branched linker. This approach increases the valency for target protein binding compared to earlier generation bivalent PROTAC molecules. SIM1 acts as a low picomolar BET degrader in vitro, and has favourable in vivo pharmacokinetics. BET inhibitors are being explored for anticancer activity.
配体家族	PROTACs, molecular glues and other degraders

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参考文献

1. Imaide S, Riching KM, Makukhin N, Vetma V, Whitworth C, Hughes SJ, Trainor N, Mahan SD, Murphy N, Cowan AD et al.. (2021) Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity.. Nat Chem Biol, 17 (11): (1157-1167). [PMID:34675414]

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