2. Metabolic Enzyme/Protease Anti-infection Apoptosis Cell Cycle/DNA Damage
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD) Parasite Apoptosis DNA/RNA Synthesis
  4. TH7299

TH7299 是一种具有抗寄生虫活性的 TbFolD 抑制剂。TH7299 可结合 MTHFD2 的四氢叶酸结合口袋，并抑制 MTHFD2L 以及 MTHFD1 的脱氢酶/环水解酶结构域。TH7299 可降低癌细胞活力，诱导 细胞凋亡 (apoptosis) 与 DNA 损伤。TH7299 可用于非洲锥虫病和急性髓系白血病的相关研究。

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TH7299

TH7299 Chemical Structure

CAS No. : 1415648-20-2

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TH7299 相关抗体

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TH7299 is a TbFolD inhibitor with antiparasitic activity. TH7299 binds the tetrahydrofolate-binding pocket of MTHFD2, and inhibits MTHFD2L and the dehydrogenase/cyclohydrolase domain of MTHFD1. TH7299 reduces cancer cells viability, induces apoptosis, DNA damage. TH7299 can be used for the researches of african trypanosomiasis and acute myeloid leukemia.[1][2]

体外研究
(In Vitro)

TH7299 (Compound 2) (0-100 μM; 5 minutes) 可抑制重组布氏锥虫 (Trypanosoma brucei) 的 FolD 脱氢酶活性，其 Ki 为 1.1 ± 0.8 μM，IC50 为 2.2 μM[1]。
TH7299 (72 h) 可在体外抑制血流型布氏锥虫布氏亚种 (Trypanosoma brucei brucei) 4的生长，其 IC50 为 49 ± 3.2 μM[1]。
TH7299 可强效抑制重组人源 MTHFD2 的酶活性，其 IC50 为 254 nM，同时能抑制 MTHFD2L (IC50 = 126 nM) 和 MTHFD1-(DC) (IC50 = 89 nM)[2]。
TH7299 (96 h) 可降低 HL-60 急性髓系白血病 (AML) 细胞的活力，其 EC50 为 1110 nM[2]。
TH7299 (30 μM; 2 h) 可在完整的 HL-60 急性髓系白血病 (AML) 细胞中结合并稳定 MTHFD2[2]。
TH7299 (10 μM; 24 h) 可使 THP-1 急性髓系白血病 (AML) 细胞的复制叉速度降低约 50%，而与 50 μM Thymidine (HY-N1150) 联合处理可完全逆转该效应[2]。
TH7299 (3 μM; 24-48 h) 主要在 S 期和 G2/M 期的 HL-60 急性髓系白血病细胞中诱导产生时间依赖性 DNA 损伤 (γH2AX 阳性)[2]。
TH7299 (10-8-10-5 M; 96 h) 可剂量依赖性地诱导 HL-60 急性髓系白血病 (AML) 细胞发生晚期凋亡，而在非致瘤性 LCL-889 细胞中仅诱导极少量凋亡[2]。
TH7299 (10-9-10-4 M; 96 h) 诱导的 HL-60 急性髓系白血病、THP-1 急性髓系白血病及 SW620 结直肠癌细胞活力丧失，可通过与 50 μM Thymidine 联合处理完全逆转[2] 。
TH7299 (10 μM; 24 h) 可增强 THP-1 急性髓系白血病 (AML) 细胞中复制起始点的激活[2]。
TH7299 (10 μM; 24 h) 可提高 THP-1 细胞中磷酸化 CHK1 蛋白与磷酸化 RPA32 蛋白的表达水平[2]。

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

TH7299 相关抗体:

Apoptosis Analysis[2]

Cell Line: HL-60 AML cells, LCL-889 nontumorigenic lymphoblastoid cells
Concentration: 10-8-10-5 M
Incubation Time: 96 h
Result: Induced late-stage apoptosis (annexin-V+/PI+) in ~60% of HL-60 cells at the highest concentration tested.
Induced late-stage apoptosis in <20% of LCL-889 cells at equivalent concentrations.

Cell Viability Assay[2]

Cell Line: HL-60 AML cells, THP-1 AML cells, SW620 colorectal cancer cells
Concentration: 10-9-10-4 M
Incubation Time: 96 h
Result: Reduced viability of HL-60, THP-1, and SW620 cells, and this viability reduction was completely rescued by co-treatment with 50 μM Thymidine.

Western Blot Analysis[2]

Cell Line: THP-1 cells
Concentration: 10 μM
Incubation Time: 6， 24， 48, 72 h
Result: Incresaed p-CHK1 and p-RPA32 levels at 24 h.
Increased p-CDK levels at 24 and 48 h.
Increased p21 levels at 48 and 72 h.
Increased γH2AX levels at 48 h.
分子量

433.38

Formula

C17H19N7O7
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

TH7299 相关分类

  • 摩尔计算器

  • 稀释计算器

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

TH72991415648-20-2TH 7299TH-7299Methylenetetrahydrofolate Dehydrogenase (MTHFD)ParasiteApoptosisDNA/RNA SynthesisHL-60 AML cellsMTHFD1MTHFD2TbFolDNADP+Trypanosoma bruceiTHP-1 AML cellsT-ALL cellsMTHFD2Lacute myeloid leukemiaInhibitorinhibitorinhibit

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