ACBI1

Catalog No.S9612 Batch:S961201

Technical Data

Formula

C₄₉H₅₈FN₉O₇S

Molecular Weight

936.10

CAS No.

2375564-55-7

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (106.82 mM)

Ethanol

2 mg/mL (2.13 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 Corn oil

2.25mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 45 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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>

Protocol (from reference)

Cell Assay:^{<sup><a class="sref" href="#s_ref">[1]</a></sup>}	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.

Cell Assay:^{<sup><a class="sref" href="#s_ref">[1]</a></sup>}

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.

References

[1] William Farnaby, et al. Nat Chem Biol. 2019 Jul;15(7):672-680.

Selleck's ACBI1 has been cited by 4 publications

Targeting SWI/SNF ATPases reduces neuroblastoma cell plasticity [ EMBO J, 2024, 10.1038/s44318-024-00206-1]	PubMed: 39174852
Enhancer reprogramming underlies therapeutic utility of a SMARCA2 degrader in SMARCA4 mutant cancer [ Cell Chem Biol, 2024, S2451-9456(24)00396-9]	PubMed: 39378885
Stepwise activities of mSWI/SNF family chromatin remodeling complexes direct T cell activation and exhaustion [ Mol Cell, 2023, 83(8):1216-1236.e12]	PubMed: 36944333
RNA Pol II preferentially regulates ribosomal protein expression by trapping disassociated subunits [ Molecular Cell, 2023, 8,-P1280-1297.E11]	PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.