VY-3-135

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

VY-3-135 

VY-3-135 是一种具有口服活性的，选择性乙酰辅酶 A 合成酶 2 (ACSS2) 抑制剂，IC50 值为 44 nM。VY-3-135 对重组人 ACSS1 或 ACSS3 没有抑制活性。VY-3-135 有效抑制 ACSS2 依赖性脂肪酸代谢，但对肿瘤中的基因表达没有影响。VY-3-135 可以抑制小鼠 ACSS2high 肿瘤模型中三阴性乳腺癌 (TNBC) 肿瘤生长，对 ACSS2low 肿瘤模型不影响。

VY-3-135

VY-3-135 Chemical Structure

CAS No. : 1824637-41-3

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生物活性

VY-3-135 is an orally active, selective acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC50 value of 44 nM. VY-3-135 displayes no inhibitory activity towards recombinant human ACSS1 or ACSS3. VY-3-135 potently inhibits ACSS2 dependent fatty acid metabolism but has no effect on gene expression in tumors. VY-3-135 inhibits triple negative breast cancer (TNBC) tumor growth in mouse ACSS2high but not ACSS2low tumors models[1].

体外研究
(In Vitro)

VY-3-135 (0.1, 1 μM; for 24 hours) blocks acetate dependent labeling of palmitate by 13C2-acetate in ACSS2low A7C11 and ACSS2high Brpkp110 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

VY-3-135 (100 mg/kg/day; PO; 30 days) represses MDA-MB-468 (ACSS2high) tumor growth but is mostly ineffective at blocking WHIM12 (ACSS2low) growth[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

429.51

Formula

C26H27N3O3
CAS 号

1824637-41-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vivo:
  • 1.

    10% DMSO, 20% solutol, 70% water containing 0.5% Tween20
参考文献

  • [1]. Katelyn D Miller, et al. Targeting ACSS2 with a Transition-State Mimetic Inhibits Triple-Negative Breast Cancer Growth. Cancer Res. 2021 Mar 1;81(5):1252-1264.

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