ACBI1

製品コードS9612 バッチS961201

印刷

化学情報

Chemical Structure 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）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.250mg/ml (2.40mM) 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. This compound 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 this compound 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 this chemical 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

  • https://pubmed.ncbi.nlm.nih.gov/31178587/

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：

Mutation of SMARCA4 Induces Cancer Cell-Intrinsic Defects in the Enhancer Landscape and Resistance to Immunotherapy [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2054] PubMed: 40080526
HINT1 suppression protects against age-related cardiac dysfunction by enhancing mitochondrial biogenesis [ Mol Metab, 2025, 93:102107] PubMed: 39909188
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

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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