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抑制剂/激活剂

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凋亡与自噬

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TPCA-1

TPCA-1 是一种有效，选择性的 IKK-2 抑制剂，IC50 值为 17.9 nM。TPCA-1 也是STAT3 磷酸化、DNA结合以及反式激活的有效抑制剂。

货号：
TK0320
规格：

1mg

2mg

5mg

10mg

100mg
价格：
￥0.00

产品参数

CAS No.	507475-17-4
生物活性	TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.
分子式	C12H10FN3O2S
分子量	279.29
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : ≥ 100 mg/mL (358.05 mM)
体内研究	TPCA-1 (3, 10, or 20 mg/kg, i.p.) results in a dose-dependent reduction in the severity of murine collagen-induced arthritis (CIA). TPCA-1(10 mg/kg, i.p. daily) inhibits growth of NSCLC with EGFR mutation and potentiates antitumor effect of ZD1839 in xenograft models.
体外研究	TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC50 of 170 to 320 nM. TPCA-1 (0-2 μM) inhibits STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner. TPCA-1 completely inhibits STAT3 phosphorylation without changing total STAT3 levels. TPCA-1 increased sensitivity to ZD1839 in both TKI sensitive cells and insensitive cells.
文献	•Signal Transduct Target Ther. 2021 Apr 24;6(1):167. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •ACS Nano. 2015 Dec 22;9(12):11800-11. •Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2996-3005. •Cell Death Dis. 2021 Oct 23;12(11):994. •Cell Death Dis. 2018 Apr 27;9(5):500. •Cell Death Dis. 2016 Dec 1;7(12):e2505. •Pharmacol Res. 2020 Jul;157:104800. •Cancer Cell Int. 2021 Jun 5;21(1):291. •Aging (Albany NY). 2021 Sep 8;13(17):21547-21570. •J Immunol. 2016 May 15;196(10):4322-30. •Exp Cell Res. 2021 Feb 15;399(2):112468. •J Sci Food Agric. 2019 Mar 30;99(5):2329-2339. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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