507475-17-4
TPCA-1
CAS: 507475-17-4
Molecular Formula: C12H10FN3O2S
507475-17-4 - Names and Identifiers
507475-17-4 - Physico-chemical Properties
| Molecular Formula | C12H10FN3O2S |
| Molar Mass | 279.29 |
| Density | 1.490 |
| Melting Point | >217°C (dec.) |
| Boling Point | 442.6±45.0 °C(Predicted) |
| Solubility | DMSO: soluble5mg/mL, clear |
| Appearance | powder |
| Color | white to light brown |
| pKa | 13.12±0.50(Predicted) |
| Storage Condition | 2-8°C |
| 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. |
| In vitro study | In a time-resolved fluorescence energy resonance transfer assay, TPCA-1 inhibited human activity by IKK-2 with an IC50 of 17.9 nM. TPCA-1 was shown to be ATP competitive. Furthermore, TPCA-1 exhibited IC50 values of 400 nM and 3600 nM for IKK-1 and JNK3, respectively. TPCA-1 concentration-dependently inhibited TNF-α production by IL-6, and IL-8 with IC50 values of 170,290, and 320 nM, respectively. TPCA-1 inhibition of glioma cell proliferation, as well as TNF-induced RelA (p65) nuclear transport and NFκB-dependent IL8 gene expression. Importantly, TPCA-1 inhibited IFN-induced gene expression, completely inhibited MX1 and GBP1 gene expression, and had only a minor effect on ISG15 expression. |
| In vivo study | TPCA-1(3, 10, or 20 mg/kg, I. p., B. I. d.) prophylactic administration resulted in a dose-dependent decrease in the severity of collagen-induced arthritis (CIA) in mice. TPCA-1(10 mg/kg, I. p., B. I. d.) results in significantly reduced disease severity and delay in disease onset with an antirheumatic drug, etanercept(4 mg/kg, I. p.) the effect of prophylactic administration every other day was comparable. Nuclear localization of p65, as well as levels of IL-1β, TPCA-1, TNF-α, and interferon-γ were significantly reduced in IL-6-and etanercept-treated mouse paw tissue. In addition, TPCA-1 administration resulted in a significant reduction in collagen-induced T cell proliferation in vivo. TPCA-1 at 20 mg/kg instead of 3 or 10 mg/kg, I. p., B. I. d. Therapeutic administration significantly reduced the severity of CIA, etanercept at 12.5 mg/kg, I. p., administration every other day had the same effect. |
507475-17-4 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36 - Irritating to the eyes |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
507475-17-4 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.581 ml | 17.903 ml | 35.805 ml |
| 5 mM | 0.716 ml | 3.581 ml | 7.161 ml |
| 10 mM | 0.358 ml | 1.79 ml | 3.581 ml |
| 5 mM | 0.072 ml | 0.358 ml | 0.716 ml |
Last Update：2024-01-02 23:10:35
507475-17-4 - Reference Information
| biological activity | TPCA-1 (GW683965) is a IKK-2 inhibitor. IC50 is 17.9 nM in cell-free test, which inhibits NF-κB pathway and is 22 times more selective than acting on IKK-1. TPCA-1 is also an inhibitor of STAT3 and can promote apoptosis. |
| target | TargetValue NF-κB () STAT3 () IKK2 (Cell-free say) 17.9 nM |
| Target | Value |
| NF-κB () | |
| STAT3 () | |
| IKK2 (Cell-free assay) | 17.9 nM |
| in vitro study | in the time-resolved fluorescence energy resonance transfer test, TPCA-1 inhibited human IKK-2 activity, IC50 was 17.9 nM. TPCA-1 proved to be ATP competitive. In addition, TPCA-1 showed IC50 values of 400 nM and 3600 nM for IKK-1 and JNK3, respectively. TPCA-1 concentration-dependent inhibition of TNF-α,IL-6, and IL-8 production, IC50 values were 170,290, and 320 nM, respectively. TPCA-1 inhibits glioma cell proliferation, as well as TNF-induced RelA (p65) nuclear transport and NFκB-dependent IL8 gene expression. Importantly, TPCA-1 inhibition of IFN-induced gene expression, MX1 and GBP1 gene expression is completely inhibited, while it has only a small effect on ISG15 expression. |
| in vivo studies | preventive administration of TPCA-1(3, 10, or 20 mg/kg, I. p., B. I. d.) resulted in a dose-dependent decrease in the severity of collagen-induced arthritis (CIA) in mice. TPCA-1(10 mg/kg, I. p., B. I. d.) resulted in a significant reduction in disease severity and delay in disease onset, which is equivalent to the effect of antirheumatic drugs, etanercept(4 mg/kg, I. p.) administered prophylactically every other day. In TPCA-1-and etanercept-treated mouse claw tissues, the nuclear localization of p65 and the levels of IL-1β,IL-6,TNF-α, and interferon-γ were significantly reduced. In addition, TPCA-1 administration resulted in a significant reduction in collagen-induced T cell proliferation in vivo. Therapeutic administration of TPCA-1 at 20 mg/kg instead of 3 or 10 mg/kg, I. p., B. I. d. significantly reduced the severity of CIA, etanercept at 12.5 mg/kg, I. p., every other day had the same effect. |
Last Update：2024-04-10 22:29:15
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Featured ProductsSpot supply
Product Name: TPCA-1 Visit Supplier Webpage Request for quotationCAS: 507475-17-4
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Multiple SpecificationsSpot supply
Product Name: TPCA-1 Request for quotationCAS: 507475-17-4
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Multiple SpecificationsSpot supply
Product Name: TPCA-1 (Standard) Visit Supplier Webpage Request for quotationCAS: 507475-17-4
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: TPCA-1 Visit Supplier Webpage Request for quotationCAS: 507475-17-4
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: TPCA-1 Visit Supplier Webpage Request for quotationCAS: 507475-17-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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