2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. IACS-4619

IACS-4619 (compound 4) 是高选择性、2-氨基嘧啶类 MTH1 (MutT 同源物 1) 抑制剂 (IC50=0.2 nM)。IACS-4619 通过抑制 MTH1 水解 8-oxo-dGTP 等氧化嘌呤核苷酸，进而阻断 MTH1 对氧化核苷酸掺入 DNA 的抑制作用。IACS-4619 在 MTH1 过表达 U2OS 细胞中可显著抑制内源性 MTH1 活性，但对多种人类癌症及正常细胞系无明显抗增殖或细胞毒性。IACS-4619 可用于肿瘤学领域中 MTH1 靶点相关研究。

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IACS-4619

IACS-4619 Chemical Structure

CAS No. : 1884209-98-6

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IACS-4619 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

IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC50=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target[1].

体外研究
(In Vitro)

IACS-4619 表现出良好的 MDCK 细胞渗透性、较高的人血浆蛋白结合率、较高的肝微粒体代谢周转率，以及在大鼠和人类中的良好血浆稳定性 [1]。
在人类癌症细胞系（U2OS、SaOS2 等）和正常细胞系（WI38、BJ 等）中，IACS-4619 (最高浓度达 50 μM) 未表现出显著的抗增殖表型 [1]。

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

IACS-4619 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Human cancer cell lines (U2OS, SaOS2, SW480, HCT116, MDAMB231, HeLa, UOK262, 293T, A549, H460, H358) and normal cell lines (WI38, BJ, hMEC, MRC5)
Concentration: 0-50 μM
Incubation Time: /
Result: Did not exhibit significant antiproliferative effects or cytotoxicity in any tested cell lines, even with prolonged treatment, and cell lines with high intrinsic ROS levels tolerated the compound well.
分子量

195.27

Formula

C10H17N3O
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

IACS-4619 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IACS-46191884209-98-6IACS4619IACS 4619DNA/RNA Synthesisliver microsomal turnoverhuman plasma protein bindingintact cellsMTH1recombinant MTH1plasma stabilitynormal cell linesMTH1-overexpressing cell lysateshuman cancer cell linesMDCK cell permeabilityInhibitorinhibitorinhibit

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