TPCA-1
- Product Name
- 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
- Formula Weight
- 279.29
- MOL File
- 507475-17-4.mol
TPCA-1 Property
- 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
- form
- powder
- pka
- 13.12±0.50(Predicted)
- 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.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H319Causes serious eye irritation
- Precautionary statements
-
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- T1452
- Product name
- TPCA-1
- Purity
- ≥95% (HPLC)
- Packaging
- 1mg
- Price
- $174
- Updated
- 2024/03/01
- Product number
- 401481
- Product name
- IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem
- Packaging
- 500μg
- Price
- $144
- Updated
- 2024/03/01
- Product number
- 15115
- Product name
- TPCA-1
- Purity
- ≥98%
- Packaging
- 500μg
- Price
- $68
- Updated
- 2024/03/01
- Product number
- 15115
- Product name
- TPCA-1
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $95
- Updated
- 2024/03/01
- Product number
- T1452
- Product name
- TPCA-1
- Purity
- ≥95% (HPLC)
- Packaging
- 5mg
- Price
- $697
- Updated
- 2024/03/01
TPCA-1 Chemical Properties,Usage,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
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View Lastest Price from TPCA-1 manufacturers
- Product
- TPCA-1 507475-17-4
- Price
- US $1.00/g
- Min. Order
- 100g
- Purity
- 99%
- Supply Ability
- G/KG/T
- Release date
- 2019-12-20