T3Inh-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

T3Inh-1 

T3Inh-1 是一种有效且选择性的 ppGalNAc-T3 抑制剂(IC50=7 µM)。T3Inh-1 可降低组织细胞和小鼠体内的 FGF23 激素水平，且不会产生任何毒副作用。T3Inh-1 还可以预防乳腺癌细胞。ppGalNAc-T3 酶至少涉及两种重要的医学途径：癌症转移和FGF23的稳定 (调节血液中的磷酸盐水平)。

T3Inh-1

T3Inh-1 Chemical Structure

CAS No. : 50440-30-7

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生物活性

T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream)[1].

体外研究
(In Vitro)

T3Inh-1 (5 µM; 24-48 hours; 5 µM; MDA-MB231 cells) is strikingly effective, inhibiting migration by >80% and invasion by 98% while causing no discernable effect on cell proliferation[1].
T3Inh-1 exhibits no toxicity and did not affect HEK cell proliferation[1].
T3Inh-1 (HEK cells; 6 hours)increases cleavage of FGF23[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

T3Inh-1 (25 or 50 mg/kg; i.p.) blocks ppGalNAc-T3-mediated glycan-masking of FGF23 thereby increasing its cleavage[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wild-type C57BL/6 six to eight week old mice[1]
Dosage: 25 or 50 mg/kg
Administration: Intraperitoneal injection (Dissolved in DMSO at 25 and 50 mg/ml then further diluted with PEG400 to create 5 and 10 mg/ml stocks for injection)
Result: Caused a robust and statistically significant increase the ratio of cleaved/intact FGF23 at the tested 25 and 50 mg/kg concentrations.

分子量

476.49

Formula

C27H20N6O3
CAS 号

50440-30-7
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.
参考文献

  • [1]. Song L, et al. Inhibitor of ppGalNAc-T3-mediated O-glycosylation blocks cancer cell invasiveness and lowers FGF23 levels. Elife. 2017;6:e24051. Published 2017 Mar 31.

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