ACBI1

製品コードS9612 バッチS961201

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₄₉H₅₈FN₉O₇S

分子量

936.10

CAS No.

2375564-55-7

Solubility (25°C)*

体外

DMSO

100 mg/mL (106.82 mM)

Ethanol

2 mg/mL (2.13 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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>

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MV-4-11 cells
	濃度	0.1-1000 nM
	反応時間	18 h
	実験の流れ	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.

参考

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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