TPCA-1
- CAS No.
- 507475-17-4
- Chemical Name:
- TPCA-1
- Synonyms
- TPCA-1;CS-991;GW683965;GW683965A;TPCA-1(TPCA 1);TPCA-1 USP/EP/BP;TPCA-1 (GW-683965;TPCA-1 IKK-2 Inhibitor IV;IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem;5-(4-Fluorophenyl)-2-ureidothiophene-3-carboxamide
- CBNumber:
- CB41073580
- Molecular Formula:
- C12H10FN3O2S
- Molecular Weight:
- 279.29
- MDL Number:
- MFCD09037541
- MOL File:
- 507475-17-4.mol
- MSDS File:
- SDS
| Melting point | >217°C (dec.) |
|---|---|
| Boiling point | 442.6±45.0 °C(Predicted) |
| Density | 1.490 |
| storage temp. | 2-8°C |
| solubility | DMSO: soluble5mg/mL, clear |
| pka | 13.12±0.50(Predicted) |
| form | powder |
| color | white to light brown |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| FDA UNII | 9M632G86CC |
TPCA-1 price More Price(37)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | T1452 | TPCA-1 ≥95% (HPLC) | 507475-17-4 | 1mg | $174 | 2024-03-01 | Buy |
| Sigma-Aldrich | 401481 | IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem | 507475-17-4 | 500μg | $144 | 2024-03-01 | Buy |
| Cayman Chemical | 15115 | TPCA-1 ≥98% | 507475-17-4 | 500μg | $68 | 2024-03-01 | Buy |
| Cayman Chemical | 15115 | TPCA-1 ≥98% | 507475-17-4 | 1mg | $95 | 2024-03-01 | Buy |
| Sigma-Aldrich | T1452 | TPCA-1 ≥95% (HPLC) | 507475-17-4 | 5mg | $697 | 2024-03-01 | Buy |
TPCA-1 Chemical Properties,Uses,Production
Description
TPCA-1 (507475-17-4) selective inhibitor of IκB kinase 2 (IKK2) (IC50 = 17.9 nM).1 Inhibits production of pro-inflammatory cytokines in arthritis and other animal models of inflammation.1,2 Also attenuates NLRP3 inflammasome activation in THP-1 myeloid cells, and suppresses IL1β-induced proliferation, migration, and invasion of HeLa cells.3,4 Continuous exposure to TPCA-1 promotes expansion of hematopoietic stem/progenitor cells (HSPCs) via improved glycolysis and limited ROS production.5
Uses
TPCA-1 is a direct dual inhibitor for both IKKβ (IKK-2) and STAT3. It inhibits STAT3 phosphorylation, DNA binding, and transactivation in vivo. Synergistic treatment of TPCA-1 with tyrosine kinase inhibitors (TKIs) can potentially be a more effective method for treating cancers.
Definition
ChEBI: 2-(carbamoylamino)-5-(4-fluorophenyl)-3-thiophenecarboxamide is a member of thiophenes and an aromatic amide.
Biological Activity
Potent, selective inhibitor of I κ B kinase-2 (IKK-2) (IC 50 = 17.9 nM) that displays > 22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes. Inhibits production of pro-inflammatory cytokines in vitro and in vivo and inhibits NF- κ B nuclear localisation. Reduces the severity and onset of collagen-induced arthritis; anti-inflammatory.
Biochem/physiol Actions
TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC50 = 17.9 nM for IKK-2 compared to 400nm for IKK-1. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation.
in vitro
determination of the activity of tpca-1 against ten selected kinases, cox-1 and cox-2, showed the compound to be ~550-fold selective for ikk-2 versus ten of these enzymes. tpca-1 inhibits lipopolysaccharide-induced human monocyte production of tnf-α, il-6, and il-8 with an ic50 of 170 to 320 nm [1].
in vivo
prophylactic administration of tpca-1 at 3, 10, or 20 mg/kg resulted in a dose dependent reduction in the severity of murine collagen-induced arthritis. the significantly reduced disease severity and delay of disease onset resulting from administration of tpca-1 at 10 mg/kg were comparable to the effects of the antirheumatic drug, etanercept [1].
storage
Store at -20°C
References
Podolin et al. (2005), Attenuation of murine collagen-induced arthritis by a novel, 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; Pharmacol. Exp. Ther., 312 373 Wang et al. (2021), TPCA-1 negatively regulates inflammation mediated by NF-kB pathway in mouse chronic periodontitis model; Oral Microbiol., 36 192 Unterreiner et al. (2021), Pharmacological inhibition of IKKb dampens NLRP3 inflammasome activation after priming in the human myeloid cell line THP-1; Biophys. Res. Commun., 545 177 Tao et al. (2021), IL-1b promotes cervical cancer though activating NF-κB/CCL-2; J. Exp. Pathol., 14 426 Sun et al. (2021), Continuous NF-κB pathway inhibition promotes expansion of human phenotypical hematopoietic stem/progenitor cells through metabolism regulation; Cell Res., 399 112468
TPCA-1 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29220 | 58 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9923 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
