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ACBI1

ACBI1 is a potent and cooperative PROTAC degrader of SMARCA2, SMARCA4 and PBRM1 with DC50 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 induces anti-proliferative effects and apoptosis.

ACBI1 Chemical Structure

ACBI1 Chemical Structure

CAS: 2375564-55-7

Selleck's ACBI1 has been cited by 2 publications

Purity & Quality Control

Batch: S961201 DMSO] 100 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false Purity: 98.85%
98.85

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Biological Activity

Description ACBI1 is a potent and cooperative PROTAC degrader of SMARCA2, SMARCA4 and PBRM1 with DC50 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 induces anti-proliferative effects and apoptosis.
Targets
SMARCA2 [1]
(in MV-4-11 cells)		 SMARCA4 [1]
(in MV-4-11 cells)		 PBRM1 [1]
(in MV-4-11 cells)
6 nM(DC50) 11 nM(DC50) 32 nM(DC50)
In vitro
In vitro

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 can induce anti-proliferative effects and apoptosis.<sup><a class="sref" href="#s_ref">[1]</a></sup>
Cell Research Cell lines MV-4-11 cells
Concentrations 0.1-1000 nM
Incubation Time 18 h
Method

ACBI1 is diluted from a 10 mM DMSO stock solution to 20 μM in buffer consisting of 20 mM 1,3-bis[tris(hydroxymethyl)methylamino] propane (BIS-TRIS) propane, 150 mM NaCl, 1 mM TCEP, pH 7.4 and a final DMSO concentration of 0.2%. Two sets of sequential titrations aer performed; first, a titration of SMARCA2BD (200 μM, in the syringe) into the PROTAC solution (20 μM, in the cell), followed by a titration of VCB complex solution (168 μM in the syringe) into the PROTAC–SMARCA2BD complex solution retained in the cell. Binary experiments consisted of an analogous initial single injection of buffer (syringe) into the PROTAC solution (20 μM, in the cell), followed by a titration of VCB complex solution (168 μM in the syringe) into the diluted PROTAC solution retained in the cells.

Chemical Information & Solubility

Molecular Weight 936.10 Formula

C49H58FN9O7S
CAS No. 2375564-55-7 SDF --
Smiles CC1=C(SC=N1)C2=CC(=C(CNC(=O)C3CC(O)CN3C(=O)C(NC(=O)C4(F)CC4)C(C)(C)C)C=C2)OCCOC5=CC=C(CN6CCN(CC6)C7=C(N)N=NC(=C7)C8=C(O)C=CC=C8)C=C5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (106.82 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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