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PROTAC BET Degrader-1 Sale

目录号 : GC33109

PROTACBETDegrader-1是基于PROTAC技术的BET降解剂,能够在低浓度下降低BRD2,BRD3和BRD4的蛋白水平。

PROTAC BET Degrader-1 Chemical Structure

Cas No.:2093386-22-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥7,275.00
现货
5mg
¥4,909.00
现货
10mg
¥7,586.00
现货
25mg
¥16,511.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

PROTAC BET Degrader-1 (Compound 9) is a potent BET degrader based on PROTAC, decreases the level of BRD2, BRD3, and BRD4 proteins in RS4;11 cells at 3-10 nM, and inhibits the growth of this cell line with an IC50 of 4.3 nM, and 45.5 nM for MOLM-13 cells[1].

[1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.

Chemical Properties

Cas No. 2093386-22-0 SDF
Canonical SMILES CCN1C(NC2=C3C4=CC(OC)=C(C(C(C)=NO5)=C5C)C=C4NC3=NC(C(NCCCCNC(COC6=C(C(N7C(CCC8=O)C(N8)=O)=O)C(C7=O)=CC=C6)=O)=O)=N2)=CC(C9CC9)=N1
分子式 C44H45N11O9 分子量 871.9
溶解度 DMSO : ≥ 50 mg/mL (57.35 mM) 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.1469 mL 5.7346 mL 11.4692 mL
5 mM 0.2294 mL 1.1469 mL 2.2938 mL
10 mM 0.1147 mL 0.5735 mL 1.1469 mL
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Research Update

General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex

ACS Pharmacol Transl Sci 2021 Feb 26;4(2):941-952.PMID:33860212DOI:PMC8033776

Proteolysis-targeting chimeras (PROTACs) degrade target proteins by engaging the ubiquitin-proteasome system. Assays detecting target-PROTAC-E3 ligase ternary complexes are critical for PROTAC development. Both time-resolved fluorescence energy transfer (TR-FRET) assays and amplified luminescent proximity homogeneous assays can characterize ternary complexes and assess PROTAC efficacy; stepwise optimization protocols for these assays are lacking. To identify assay conditions that can be applied to various targets and PROTACs, we used a stepwise approach to optimize a TR-FRET assay of BRD2(BD1)/PROTACs/CRBN ternary complexes. This assay is sensitive and specific and responds to the bivalent PROTACs dBET1, PROTAC BET Degrader-1, and PROTAC BET Degrader-2 but not to non-PROTAC ligands of BRD2(BD1) or CRBN. The activity rank order of dBET1, PROTAC BET Degrader-1, and PROTAC BET Degrader-2 in the TR-FRET assay corresponded with previously reported cell growth inhibition assays, indicating the effectiveness of our assay for predicting PROTAC cellular activity. The TR-FRET ternary complex formation assay for BRD2(BD1)/PROTAC/CRBN can be configured to characterize the binding activities of BRD2(BD1) and CRBN ligands with the same compound activity rank order as that of previously reported binary binding assays for individual targets but with the advantage of simultaneously assessing the ligand activities for both targets. Our assay is modular in nature, as BRD2(BD1) can be replaced with other BRDs and successfully detect ternary complexes without modifying other assay conditions. Therefore, the TR-FRET ternary complex assay for BRDs provides a general assay protocol for establishing assays for other targets and bivalent molecules.