2. Metabolic Enzyme/Protease
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD)
  4. MTHFD1/2-IN-1

MTHFD1/2-IN-1 是一种口服有效、双重 MTHFD1/MTHFD2 抑制剂，对人源 MTHFD1 和 MTHFD2 的 IC50 分别为 0.26 μM 和 0.031 μM。MTHFD1/2-IN-1 通过抑制 MTHFD1 的脱氢酶活性以及 MTHFD2 的脱氢酶和环水解酶活性，阻断一碳代谢，进而破坏癌细胞内的核苷酸生物合成与氧化还原稳态。MTHFD1/2-IN-1 具备良好的 Caco-2 通透性及肝微粒体代谢稳定性。MTHFD1/2-IN-1 表现出显著的抗白血病活性，不仅能降低多种白血病细胞活力，还能在小鼠模型中抑制急性髓系白血病 (AML) 的肿瘤生长。

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MTHFD1/2-IN-1

MTHFD1/2-IN-1 Chemical Structure

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MTHFD1/2-IN-1 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

MTHFD1/2-IN-1 is an oraly active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models[1].

体外研究
(In Vitro)

MTHFD1/2-IN-1 (compound 34) 可强效抑制人急性髓系白血病 (AML) 细胞系 MOLM-13 (IC50=0.25 μM) 和 THP-1 (IC50=0.06 μM) 的增殖，对 K562、NALM-6 和 MOLT-4 细胞仅表现出中等活性[1]。
MTHFD1/2-IN-1 (0.1-10 μM; 1 h+15 min) 可直接与人类 MTHFD1 和 MTHFD2 蛋白相互作用，这一点可通过其对蛋白水解降解的剂量依赖性保护作用得到证实[1]。

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

MTHFD1/2-IN-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: human AML cell lines MOLM-13, THP-1; human CML cell line K562; human ALL cell lines NALM-6, MOLT-4
Concentration: Serial dilutions
Incubation Time: 72 h
Result: Inhibited proliferation of MOLM-13 cells with an IC50 of 0.25 μM.
Inhibited proliferation of THP-1 cells with an IC50 of 0.06 μM.
Inhibited proliferation of K562 cells with an IC50 of 0.40 μM.
Inhibited proliferation of NALM-6 cells with an IC50 of 1.26 μM.
Inhibited proliferation of MOLT-4 cells with an IC50 of 1.78 μM.
体内研究
(In Vivo)

MTHFD1/2-IN-1 (compound 34) (100-300 mg/kg；口服；每日 1 次) 在 AML 异种移植模型中可诱导剂量依赖性的肿瘤生长抑制，且毒性极低[1]。

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

Animal Model: BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft model)[1]
Dosage: 100 mg/kg; 300 mg/kg
Administration: p.o.; once daily
Result: Induced tumor growth inhibition at 100 mg/kg.
Induced 79% tumor growth inhibition (TGI) at 300 mg/kg.
Maintained stable body weight across treatment period, indicating no significant treatment-related toxicity.
分子量

651.70

Formula

C30H36F3N5O6S
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

MTHFD1/2-IN-1 相关分类

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  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

MTHFD1/2-IN-1Methylenetetrahydrofolate Dehydrogenase (MTHFD)nucleotide biosynthesismouse liver microsomesone-carbon metabolismacute myeloid leukemiaMTHFD2Caco-2MTHFD1human liver microsomeschronic myeloid leukemiaredox homeostasisInhibitorinhibitorinhibit

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