2. Metabolic Enzyme/Protease
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD)
  4. MTHFD2-IN-7

MTHFD2-IN-7 是一种口服有效、选择性的 MTHFD2 抑制剂，对人源 hMTHFD1 和 hMTHFD2 的 IC50 分别为 0.038 μM 和 7.44 μM。MTHFD2-IN-7 通过结合 MTHFD2 的底物结合位点并维持与 NAD+ 的相互作用来发挥作用。经 TSA 和 DARTS 实验验证，MTHFD2-IN-7 不仅能有效结合靶蛋白，还具备 Caco-2 渗透性及肝微粒体代谢稳定性。MTHFD2-IN-7 在小鼠中表现出良好的药代动力学特性。MTHFD2-IN-7 还能够显著抑制癌细胞增殖并缩小肿瘤体积，是急性髓系白血病研究中具有潜力的小分子工具。

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MTHFD2-IN-7

MTHFD2-IN-7 Chemical Structure

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MTHFD2-IN-7 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

MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research[1].

体外研究
(In Vitro)

MTHFD2-IN-7 (compound 31) 可抑制人白血病细胞系的增殖[1]。
MTHFD2-IN-7 (0.1-10 μM; 1 h+15 min) 可呈剂量依赖性结合并保护纯化的人源 MTHFD2 和 MTHFD1 免受链霉蛋白酶降解，在 0.1、1.0 和 10 μM 浓度下均有该作用，证实了其与靶点的直接结合[1]。

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

MTHFD2-IN-7 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Human leukemia cell lines: MOLM-13, THP-1, K562, NALM-6 and MOLT-4
Concentration: IC50
Incubation Time: 72 h
Result: Inhibited the proliferation of human leukemia cell lines, with IC50 values of 0.72 μM (MOLM-13), 0.25 μM (THP-1), 0.84 μM (K562), 2.45 μM (NALM-6) and 4.75 μM (MOLT-4).
体内研究
(In Vivo)

MTHFD2-IN-7 (compound 31) (100-300 mg/kg；口服；每日 1 次) 可在 MOLM-13 急性髓系白血病异种移植模型中诱导剂量依赖性的肿瘤生长抑制，且无显著毒性[1]。

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

Animal Model: BALB/c nude mice with Acute myeloid leukemia (female, 6−8 weeks old)[1]
Dosage: 100 mg/kg; 300 mg/kg
Administration: p.o.; once daily
Result: Achieved 37% tumor growth inhibition at 100 mg/kg.
Achieved 67% tumor growth inhibition at 300 mg/kg.
Showed no significant body weight loss, indicating well tolerated treatment.
分子量

623.64

Formula

C28H32F3N5O6S
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

MTHFD2-IN-7 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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The dilution calculator equation

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

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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:

MTHFD2-IN-7Methylenetetrahydrofolate Dehydrogenase (MTHFD)MTHFD2MOLM-13K562Caco-2acute myeloid leukemiacancer cell proliferationNAD+NALM-6THP-1MTHFD1Inhibitorinhibitorinhibit

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