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。
| 生物活性 | TPCA-1 is a potent and selective inhibitor ofIKK-2withIC50of 17.9 nM. TPCA-1 is an effective inhibitor ofSTAT3phosphorylation, DNA binding, and transactivation. |
| IC50& Target[3] | |
体外研究
(In Vitro) | TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC50of 170 to 320 nM[1][2].
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[3].
TPCA-1 increased sensitivity to ZD1839 in both TKI sensitive cells and insensitive cells[3].
Cell Viability Assay[2] | Cell Line: | human peripheral blood monocytes stimulated with LPS. | | Concentration: | 0-10 μM. | | Incubation Time: | ~24 hours. | | Result: | TPCA-1 Inhibits LPS-Induced TNF-α, IL-6, and IL-8 production by human monocytes. |
Cell Viability Assay[3] | Cell Line: | HCC827 and H1975 cells. | | Concentration: | 0-10 μM. | | Incubation Time: | 0.5-2 hours. | | Result: | Suppressed proliferation of HCC827 and H1975 cells.
Led to a G2-M cell-cycle arrest in HCC827 but not A549. |
Western Blot Analysis[3] | Cell Line: | HEK-293T cell lines. | | Concentration: | 0-2 μM (before IL-2 or IFN-α treatment). | | Incubation Time: | 0.5-2 hours. | | Result: | Inhibited STAT3 phosphorylation and transactivation induced by cytokines and nonreceptor tyrosine kinase in dose- and time-dependent manner. |
|
体内研究
(In Vivo) | 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)[2].
TPCA-1(10 mg/kg, i.p. daily) inhibits growth of NSCLC with EGFR mutation and potentiates antitumor effect of ZD1839 in xenograft models[3].
| Animal Model: | 10-12 weeks old male DBA/1 OlaHsd mice[2]. | | Dosage: | 3, 10, or 20 mg/kg. | | Administration: | I.P., b.i.d, from days 1 to 47. | | Result: | Reduced the severity and delays the onset of CIA.
Attenuated ex vivo antigen-induced T cell proliferation in CIA. |
| Animal Model: | Six-week-old BALB/c female nude mice injected subcutaneously with HCC827 cells (5×106)[3]. | | Dosage: | 10 mg/kg. | | Administration: | Intraperitoneally daily. | | Result: | The tumor weight inhibition rate of TPCA-1, ZD1839, and their combination are 0.419(ETPCA-1), 0.680(EZD1839), and 0.837(Eobserved), respectively. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(358.05 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.5805 mL | 17.9025 mL | 35.8051 mL | | 5 mM | 0.7161 mL | 3.5805 mL | 7.1610 mL | | 10 mM | 0.3581 mL | 1.7903 mL | 3.5805 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution
此方案可获得 ≥ 7.5 mg/mL (26.85 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution
此方案可获得 ≥ 7.5 mg/mL (26.85 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution
此方案可获得 ≥ 7.5 mg/mL (26.85 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com