TPCA-1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
TPCA-1是一种新型有效的人IKK-2选择性抑制剂。
已证明，IκB激酶2（IKK-2）通过刺激肿瘤坏死因子（TNF-α）和细胞介素（IL-1），在核因子κB调节的促炎分子的产生中起关键作用，表明抑制IKK-2可能有益于类风湿性关节的治疗。
体外试验：测定TPCA-1对10种特定激酶，如COX-1和COX-2的活性，结果显示，与10种酶相比，该化合物对IKK-2约有550倍的选择性。TPCA-1抑制脂多糖诱导的人单核细胞对TNF-α、IL-6α和IL-8的生产，IC50值为170至320 nM[1]。
体内试验：TPCA-1以3、10或20 mg/kg的剂量预防性给药，导致小鼠胶原诱导性关节炎的严重程度剂量依赖性地降低。TPCA-1以10 mg/kg的剂量给药可以显著地降低该病的严重程度，并延迟发病，这可以和抗风湿药依那西普（etanercept）的疗效相媲美[1]。
临床试验：目前没有临床数据。
参考文献：
[1] Podolin PL, Callahan JF, Bolognese BJ, Li YH, Carlson K, Davis TG, Mellor GW, Evans C, Roshak AK. 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 proinflammatory cytokines and antigen-induced T cell Proliferation. J Pharmacol Exp Ther. 2005 Jan; 312(1): 373-81.
- 1. Yanhong Chen, Xu Zhou, et al. "The miR-26a-5p/IL-6 axis alleviates sepsis-induced acute kidney injury by inhibiting renal inflammation." Ren Fail. 2022 Dec;44(1):551-561. PMID: 35491874
- 2. Jingchun Du, Yougui Xiang, et al. "RIPK1 dephosphorylation and kinase activation by PPP1R3G/PP1γ promote apoptosis and necroptosis." Nat Commun. 2021 Dec 3;12(1):7067. PMID: 34862394
- 3. Varga Z, Molnár T, et al. "Differences in the sensitivity of classically and alternatively activated macrophages to TAK1 inhibitor-induced necroptosis." Cancer Immunol Immunother. 2020;10.1007/s00262-020-02623-7. PMID: 32472370
- 4. Robert J. Posont. "The Role of Inflammatory Pathways in Development, Growth, and Metabolism of Skeletal Muscle in IUGR Offspring; Blood Gene Expression of Inflammatory Factors as Novel Biomarkers for Assessing Stress and Wellbeing in Exotic Species." University of Nebraska-Lincoln. 2019.
- 5. Robeson AC, Lindblom KR, et al. "Dimer-specific immunoprecipitation of active caspase-2 identifies TRAF proteins as novel activators." EMBO J. 2018 Jun 6. pii: e97072. PMID: 29875129
- 6. Kwon Y, Choi SK, et al. "Involvement of inhibitor kappa B kinase 2 (IKK2) in the regulation of vascular tone." Lab Invest. 2018 May 21. PMID: 29785049
| Physical Appearance | A solid |
| Storage | Desiccate at -20°C |
| M.Wt | 279.29 |
| Cas No. | 507475-17-4 |
| Formula | C12H10FN3O2S |
| Solubility | insoluble in H2O; ≥13.95 mg/mL in DMSO; ≥2.53 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 2-(carbamoylamino)-5-(4-fluorophenyl)thiophene-3-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=CC=C1C2=CC(=C(S2)NC(=O)N)C(=O)N)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]: | |
|
细胞系 |
人类单核细胞 |
|
溶解方法 |
在DMSO中的溶解度>14mg/mL。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
0.1, 0.3, 1, 3和10 μM; 30 min |
|
应用 |
在人外周血单核细胞中，TPCA-1以浓度依赖性方式抑制由LPS诱导的TNF-α，IL-6和IL-8的产生，IC50值分别为170,290和320nM。 |
| 动物实验[1]: | |
|
动物模型 |
胶原免疫/增强的DBA/1小鼠 |
|
剂量 |
3, 10或20 mg/kg, 腹腔注射, 每日2次,从第1天到第48天 |
|
应用 |
在胶原免疫/增强的DBA / 1小鼠中，TPCA-1（20或10mg / kg）剂量依赖性地降低关节炎的严重性，导致平均临床评分显著降低并延迟发病时间。TPCA-1（10mg / kg，腹腔注射，每日2次）也抑制p65核定位和IL-1β、IL-6、TNF-α和IFN-γ的爪组织水平。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Podolin PL, Callahan JF, Bolognese BJ, Li YH, Carlson K, Davis TG, Mellor GW, Evans C, Roshak AK. 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 proinflammatory cytokines and antigen-induced T cell Proliferation. J Pharmacol Exp Ther. 2005 Jan;312(1):373-81. |
|
| Description | TPCA-1是一种IκB激酶-2的选择性抑制剂，对IKK-2和IKK-1的IC50值分别为17.9 nM和0.4 μM。 | |||||
| 靶点 | IKK-2 | IKK-1 | ||||
| IC50 | 17.9 nM | 0.4 μM | ||||
质量控制和MSDS
- 批次:
化学结构
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