1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. ST13

ST13 是一种邻羟基苯胺类化合物,是选择性、慢速且紧密结合的 HDAC1HDAC2 抑制剂,其 IC50 值分别为 23 nM 和 49 nM。ST13 对 HDAC3 (IC50 = 4.30 μM) 和 HDAC6 (IC50 > 10 μM) 的抑制作用较弱。ST13 的诱导契合机制通过两步过程进行:首先,酶和抑制剂快速形成碰撞复合物 (EI),然后缓慢转化为稳定的复合物 E*I。ST13 可诱导癌细胞凋亡 (apoptosis)。ST13 可用于黑色素瘤和三阴性乳腺癌的研究。

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ST13

ST13 Chemical Structure

CAS No. : 1013620-98-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ST13, an ortho-hydroxyanilide, is a selective, slow- and tight-binding HDAC1 and HDAC2 inhibitor with IC50s of 23 nM and 49 nM, respectively. ST13 shows a weak inhibition of HDAC3 (IC50 = 4.30 μM) and HDAC6 (IC50 > 10 μM). The induced fit mechanism of ST13 proceeds through a two-step process: first, the enzyme and inhibitor rapidly form a collision complex (EI), which then slowly transforms into the stable complex E*I. ST13 induces apoptosis in cancer cells. ST13 can be used for the study of melanoma and triple-negative breast[1].

IC50 & Target[1]

HDAC1

23 nM (IC50)

HDAC2

49 nM (IC50)

HDAC3

4300 nM (IC50)

HDAC6

>10 μM (IC50)

体外研究
(In Vitro)

ST13 (72-120 小时) 在癌细胞系中表现出时间依赖性的抗增殖活性,在 MV-3 细胞中,EC50 值从 2.77 µM (72 h) 降至 0.311 µM (120 h)。在 MDA-MB-231 中,EC50 值从 4.87 µM (72 小时) 降至 0.087 µM (120 小时)[1]
ST13 (10 µM;48 小时) 能显著诱导 MDA-MB-231 细胞凋亡[1]
ST13 (5 μM,24-72 h) 可显著增加 MV-3 细胞中乙酰化组蛋白 H3 的水平[1]
在 MV-3 细胞、MDA-MB-231 细胞、非肿瘤细胞系 HEK293 和血液癌细胞系 MM.1S 中,ST13 (18 h) 对 HDACs 表现出抑制作用,其 EC50 值分别为 0.311 μM、0.577 μM、0.333 μM 和 0.637 μM[1]
ST17 (0.040 µM, 0.072 µM; 10 分钟) 是 ST13 的光激活前药,在紫外照射下可有效抑制 HDAC1/HDAC2[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 10 µM
Incubation Time: 48 h
Result: Induced apoptosis in MDA-MB-231 cells.

Western Blot Analysis[1]

Cell Line: MV-3 cells
Concentration: 5 µM
Incubation Time: 24 h, 48 h, 72 h
Result: Only led to hyperacetylation of histone H3, indicating selectivity toward class I HDACs and the absence of HDAC6 inhibition in a cellular environment.
分子量

346.38

Formula

C21H18N2O3

CAS 号
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.

纯度 & 产品资料
参考文献
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