2. Epigenetics Metabolic Enzyme/Protease
  3. Methionine Adenosyltransferase (MAT)
  4. ZS34

ZS34 是一种高效、口服有效、且选择性的 MAT2A 抑制剂，IC50 值为 13.7 nM，对 hERG 和 UGT1A1 的抑制作用极小。ZS34 通过抑制 SAM 合成、降低 SDMA 水平和诱导 DNA 损伤，选择性地抑制甲基硫代腺苷磷酸化酶 (MTAP) 缺陷型癌细胞的生长。ZS34 在 HCT116 MTAP-/- 异种移植小鼠模型中显示出抗肿瘤作用。ZS34 可用于 MTAP 缺陷型癌症的研究。

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ZS34

ZS34 Chemical Structure

CAS No. : 3106086-17-0

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ZS34 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZS34 is a potent, orally active, and selective MAT2A inhibitor with an IC50 of 13.7 nM, displaying minimal hERG and UGT1A1 liabilities. ZS34 selectively suppresses the growth of methylthioadenosine phosphorylase (MTAP)-deficient cancer cells by inhibiting SAM synthesis, reducing SDMA levels, and inducing DNA damage. ZS34 exhibits antitumor efficacy in a HCT116 MTAP-/- xenograft mouse model. ZS34 can be used for the research of MTAP-deficient cancer[1].

IC50 & Target[1]

MAT2A

13.7 nM (IC50)

体外研究
(In Vitro)

ZS34 (10 天) 抑制 MTAP 缺陷细胞 (NCI-H838、NCI-H1437、MCF-7、MDA-MB-231 和 MIA PaCa-2 细胞) 的增殖，IC50 分别为 1.70、386、38.1、37.2 和 115 nM，对 MTAP 功能正常的细胞 (A-375、AsPC-1、DU145、NCI-H460 和 NCI-H520) 表现出选择性，IC50 >10000 nM[1]。
ZS34 (10 天) 对 MTAP 缺失的 HCT116 细胞表现出强效的抗增殖作用 (IC50 = 124 nM)，但对 WT HCT116 细胞活性较弱(IC50 > 10000 nM)，表现出优异的选择性抑制作用，选择性指数 (SI) 超过 80.6[1]。
ZS34 (0-10 μM；96 小时) 通过抑制 MAT2A 选择性地诱导 MTAP 缺陷型 HCT116 细胞的 DNA 损伤[1]。
ZS34 与 MAT2A 二聚体的变构位点结合，与 Arg313 和配位水分子形成氢键，并与 Phe20、Trp274 和 Phe18 进行 π-π 堆积，同时其邻位甲基参与与 Phe333 的 CH-π 相互作用[1]。

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

ZS34 相关抗体:

Western Blot Analysis[1]

Cell Line: HCT116 (MTAP-/-) and HCT116 (WT)
Concentration: 0, 0.1, 1 μM
Incubation Time: 96 h
Result: Induced a dose-dependent decrease in the SDMA level, in HCT116 MTAP-/- cells, but not in HCT116 WT cells.
Induced a marked increase in γH2AX levels, a marker of DNA damage, in HCT116 MTAP-/- cells, but not in HCT116 WT cells.

Immunofluorescence[1]

Cell Line: HCT116 (MTAP-/-) and HCT116 (WT)
Concentration: 0.1, 1, 10 μM
Incubation Time: 96 h
Result: led to a marked increase in γH2AX levels in HCT116 MTAP-/-cells compared to the control, but not in HCT116 WT cells.
体内研究
(In Vivo)

ZS34 (10 和 30 mg/kg，口服，每日一次，持续 30 天) 在 HCT116 MTAP-/-异种移植模型中表现出强大的体内抗肿瘤功效和良好的安全性特征[1]。
ZS34（400 mg/kg，口服，单次剂量）对小鼠没有明显的毒性[1]。

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

Animal Model: Female ALB/c nude mice subcutaneously inoculated with HCT116 MTAP-/- cells[1]
Dosage: 10, 30 mg/kg
Administration: p.o., daily for 30 days
Result: Significantly suppressed tumor growth, with tumor growth inhibition (TGI) values of 57.3% and 89.0% at 10 and 30 mg/kg, respectively.
Showed a tendency to cause tumor regression at 30 mg/kg.
Reduced SAM levels in tumors.
Showed no significant body weight loss compared to control.
Animal Model: ICR mice[1]
Dosage: 400 mg/kg
Administration: p.o., single dose
Result: Was well tolerated at this high dose.
分子量

339.78

Formula

C18H14ClN3O2
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

ZS34 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

ZS343106086-17-0ZS 34ZS-34Methionine Adenosyltransferase (MAT)S-adenosylmethionine Synthetasemethylthioadenosine phosphorylase (MTAP)-deficient cancer cellsSAM synthesisSDMADNA damageHCT116 MTAP-/- xenograft mouse modelInhibitorinhibitorinhibit

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