产品说明书

TPCA-1

Print
Chemical Structure| 507475-17-4 同义名 : IKK2 Inhibitor IV;GW683965
CAS号 : 507475-17-4
货号 : A377370
分子式 : C12H10FN3O2S
纯度 : 99%+
分子量 : 279.29
MDL号 : MFCD09037541
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(375.95 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 TPCA-1 effectively suppresses the production of TNF-α, IL-6, and IL-8 in human monocytes triggered by lipopolysaccharide, with an IC50 ranging from 170 to 320 nM[1][2]. TPCA-1, at concentrations ranging from 0 to 2 μM, dose-dependently and over time, impedes the phosphorylation and transactivation of STAT3 caused by cytokines and nonreceptor tyrosine kinases. It fully halts the phosphorylation of STAT3 while maintaining the overall levels of STAT3 unchanged[3] TPCA-1 enhances the responsiveness to ZD1839 across cell lines that are either sensitive or resistant to tyrosine kinase inhibitors. In human peripheral blood monocytes activated with LPS, TPCA-1, at concentrations from 0 to 10 μM over approximately 24 hours, curtails the production of TNF-α, IL-6, and IL-8. This inhibition of LPS-induced cytokine production confirms the compound's effectiveness in cell viability assays. In cancer cell lines HCC827 and H1975, TPCA-1, administered in the same concentration range for 0.5 to 2 hours, inhibits cell proliferation and induces a G2-M phase cell-cycle arrest in HCC827 cells, but not in A549 cells[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
C57BL/6 mouse BMDM cells Cytotoxicity assay 24 h Cytotoxicity against C57BL/6 mouse BMDM cells assessed as LDH release after 24 hrs 22533790
C57BL/6 mouse BMDM cells 0.5 μM Function assay 1 h Antiinflammatory activity in C57BL/6 mouse BMDM cells assessed as inhibition of LPS-stimulated TNFalpha production at 0.5 uM pretreated for 1 hr before LPS challenge after 8 to 24 hrs by immunoassay 22533790
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.90mL

3.58mL

1.79mL

35.81mL

7.16mL

3.58mL
参考文献

[1]Sachse F, et al. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro.Rhinology. 2011 Jun;49(2):168-73.

[2]Podolin PL, et al. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflamm

[3]Nan J, et al. TPCA-1 is a direct dual inhibitor of STAT3 and NF-κB and regresses mutant EGFR-associated human non-small cell lung cancers. Mol Cancer Ther. 2014 Mar;13(3):617-29.