ACBI1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ACBI1 是 BAF ATPase 亚基 SMARCA2 和 SMARCA4 的有效 PROTAC 降解剂，还可降解多溴相关 BAF (PBAF) 复合体成员 PBRM1，MV-4-中 SMARCA2、SMARCA4 和 PBRM1 的 DC50 分别为 6 nM、11 nM 和 32 nM分别为 11 个单元。

ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 can induce anti-proliferative effects and apoptosis.

ACBI1 (1-10000 nM； 3-7 days) shows anti-proliferative activity.ACBI1 (0.3 μM; 100 h) induces apoptosis in SK-MEL-5 cells.ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase von Hippel-Lindau. Cell Proliferation Assay Cell Line:MV-4-11, NCI-H1568 cells Concentration:0-1000 nM Incubation Time:3-7 days Result:Showed anti-proliferative activity with IC50 of 29, 68 nM for MV-4-11, NCI-H1568 cells, respectively.Apoptosis Analysis Cell Line:SK-MEL-5 cells Concentration:0.3 μM Incubation Time:100 hResult:Induced apoptosis in SK-MEL-5 cells.

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Apoptosis

Apoptosis

Apoptosis|Epigenetic Reader Domain|PROTAC

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2375564-55-7

936.1

C49H58FN9O7S

>98% (HPLC)

DMSO:100 mg/mL (106.83 mM)

CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(C4(CC4)F)=O)=O)=O)C(OCCOC5=CC=C(CN6CCN(C7=CC(C8=C(O)C=CC=C8)=NN=C7N)CC6)C=C5)=C2

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(-20℃)

With Ice Pack

≥ 2 years