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dBET6

普罗塔克

规格或纯度: 98%

CAS编号: 1950634-92-0
分子式: C₄₂H₄₅ClN₈O₇S
分子量: 841.37
PubChem编号: 121427831

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货号 (SKU)	包装规格	是否现货	价格	数量
D414163-5mg	5mg	期货
D414163-10mg	10mg	现货
D414163-25mg	25mg	期货
D414163-50mg	50mg	现货

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bromodomain containing 4 Inhibitor

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基本描述

规格或纯度	98%
英文名称	dBET6
英文别名	6H-?Thieno[3,?2-?f]?[1,?2,?4]?triazolo[4,?3-?a]?[1,?4]?diazepine-?6-?acetamide,4-?(4-?chlorophenyl)?-?N-?[8-?[[2-?[[2-?(2,?6-?dioxo-?3-?piperidinyl)?-?2,?3-?dihydro-?1,?3-?dioxo-?1H-?isoindol-?4-?yl]?oxy]?acetyl]?amino]?octyl]?-?2,?3,?9-?trimethyl-?,(6S
生化机理	dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Information dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis . Targets BRD4 14 nM In vitro dBET6 is a highly cell-permeable degrader of BET bromodomains. It is potent in most cancer cell lines. dBET6 features highly increased cellular potency with evident degradation in the sub-nanomolar range. Treatment with 100 nM dBET6 leads to degradation of BRD4 after 1 hr, prompting subsequent downregulation of c-MYC and induction of apoptosis. dBET6 disrupts global productive transcription elongation. dBET6 treatment leads to a widespread decrease in steady-state mRNA levels, but observed an incommensurate impact on expression of members of the core regulatory circuitry of leukemogenic transcription factors. The collapse of the core transcriptional machinery prompted by BET degradation precedes a robust apoptotic response, of apparent translational significance. In vivo dBET6 is well tolerated. Upon dBET6 treatment, a significant reduction of leukemic burden is observed in a disseminated mouse model of T-ALL. Moreover, mice treated with dBET6 (7.5 mg/kg BID) exhibits a significant survival benefit compared to mice treated with vehicle control or JQ1 (20 mg/kg QD). Cell Research(from reference) Cell lines：MOLT4 cells deficient in CRBN expression? Concentrations：0.05, 0.1, 0.5, 1 μM? Incubation Time：3 hr?

产品属性

ALogP	4.8
HBD Count	3
Rotatable Bond	16

名称和标识符

IUPAC Name	2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]-N-[8-[[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetyl]amino]octyl]acetamide
INCHI	InChI=1S/C42H45ClN8O7S/c1-23-24(2)59-42-35(23)37(26-13-15-27(43)16-14-26)46-29(38-49-48-25(3)50(38)42)21-33(53)44-19-8-6-4-5-7-9-20-45-34(54)22-58-31-12-10-11-28-36(31)41(57)51(40(28)56)30-17-18-32(52)47-39(30)55/h10-16,29-30H,4-9,17-22H2,1-3H3,(H,44,53)(H,45,54)(H,47,52,55)/t29-,30?/m0/s1
InChi Key	JGQPZPLJOBHHBK-UFXYQILXSA-N
Canonical SMILES	CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCCCCCCCNC(=O)COC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O)C7=CC=C(C=C7)Cl)C
PubChem CID	121427831
分子量	841.37

数据库链接

PubChem CID	121427831
CAS Registry No.	1950634-92-0

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 100 mg/mL (118.85 mM); Ethanol: 50 mg/mL (59.42 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	100
DMSO(mM) Max Solubility	118.8537742016
Water(mg / mL) Max Solubility	＜1

安全和危险性（GHS）

象形图	Toxic Health Hazard
信号词	Danger
危险声明	H301: Toxic if swallowed H360: May damage fertility or the unborn child
预防措施声明	P280,P321,P405,P501,P264,P270,P330,P203,P301+P316,P318

关联配体

Ligand ID	10534
名称	dBET6
类别	Synthetic organic
学名	4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价	dBET6 has been used to show that BET bromodomain protein degradation promotes a collapse of global elongation that phenocopies CDK9 inhibition. It is suggested that BET bromodomain degraders could be developed as novel cancer therapeutics . dBET6 induces degradation of BRD4 in vivo, and inhibits tumour growth in T-ALL xenograft models.
评价	dBET6 is a BRD4-targeting, cereblon (CRBN)-engaging degrader (or PROTAC; proteolysis targeting chimera) .
配体家族	PROTACs, molecular glues and other degraders

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参考文献

1. Winter GE, Mayer A, Buckley DL, Erb MA, Roderick JE, Vittori S, Reyes JM, di Iulio J, Souza A, Ott CJ et al.. (2017) BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment.. Mol Cell, 67 (1): (5-18.e19). [PMID:28673542]

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