BRD4-degrader-AT1 _BRD4 Degrader - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBRD4 degrader AT1Cat. No.: HY-111433CAS No.: 2098836-45-2分式: CHClNOS分量: 972.68作靶点: Epigenetic Reader Domain; PROTAC作通路: Epigenetics; PROTAC储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (1

2、02.81 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.0281 mL 5.1404 mL 10.2809 mL5 mM 0.2056 mL 1.0281 mL 2.0562 mL10 mM 0.1028 mL 0.5140 mL 1.0281 mL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，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使

3、；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.17 mg/mL (1.20 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.17 mg/mL (1.20 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 1.17

4、 mg/mL (1.20 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 BRD4 degrader AT1于 PROTAC 技术的种度选择性的 Brd4 降解剂，在细胞中对 Brd4BD2 的 Kd 值为44 nM。IC50 & Target Kd: 44 nM (Brd4BD2, cell assay), 38.8 nM (Brd4BD2 QVK, cell assay), 111 nM (Brd2BD1, cell assay), 94 nM(Brd2BD

5、2, cell assay), 35 nM (Brd3BD1, cell assay), 39 nM (Brd3BD2, cell assay), 75 nM (Brd4BD1, cellassay), 35 nM (Brd2BD1 KEA, cell assay) 1体外研究 BRD4 degrader AT1 is a highly selective Brd4 degrader, with a Kd of 44 nM, for Brd4BD2 in cells. BRD4degrader AT1 also shows Kds of 38.8 nM for a mutant Brd4BD2

6、 (QVK), 111 14 nM for Brd2BD1, 94 9 nMfor Brd2BD2, 35 3 nM for Brd3BD1, 39 8 nM for Brd3BD2, 75 23 nM for Brd4BD1 and 35 4 nM for aBrd2BD1 mutant (KEA). BRD4 degrader AT1 (1-3 M) causes remarkable Brd4-selective depletion and hasno or little activity against Brd2 and Brd3 1.REFERENCES1. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017May;13(5):514-521.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.T