TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.
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TPCA-1 Chemische Struktur
CAS. Nr. : 507475-17-4
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Based on 33 publication(s) in Google Scholar
TPCA-1 purchased from MedChemExpress. Usage Cited in:
Cell Death Dis. 2018 Apr 27;9(5):500.
[Abstract]
Western blotting analysis of lysates from 3×HA-IκBα-expressing HT-29 cells treated as indicated for 8 h.
TPCA-1 purchased from MedChemExpress. Usage Cited in:
J Immunol. 2016 May 15;196(10):4322-30.
[Abstract]
HEK293T (IRF3-BiLC) cells are pretreated with TPCA-1 for 1 h, stimulated with TNF-α for 12 h, and then transfected with poly(I:C) for 12 h, after which IRF3-BiLC luciferase activity is measured.
TPCA-1 purchased from MedChemExpress. Usage Cited in:
ACS Nano. 2015 Dec 22;9(12):11800-11.
[Abstract]
Neutrophil-mediated delivery of TPCA-1 mitigates acute lung inflammation/injury. Numbers of leukocytes and neutrophils, concentrations of IL-6 in BALF 20 h after iv injection of vehicle of TPCA-1 solution, 5% glucose, TPCA-1 solution or TPAC-1 BSA NPs in mice 4 h after LPS challenge (8 mg/kg).
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Alle IKK Isoform-spezifische Produkte anzeigen:
Alle Isoformen anzeigen
IKK-α IKK-β IKK IKKε TBK1
Alle STAT Isoform-spezifische Produkte anzeigen:
Alle Isoformen anzeigen
STAT3 STAT5 STAT6 STAT1
Beschreibung
TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.
IC50 & Target[3]
IKK-2
17.9 nM (IC50)
STAT3
In Vitro
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][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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TPCA-1 Related Antibodies
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.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
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.
Molekulargewicht
279.29
Formel
C12H10FN3O2S
CAS. Nr.
507475-17-4
Appearance
Solid
Color
White to gray
SMILES
O=C(C1=C(NC(N)=O)SC(C2=CC=C(F)C=C2)=C1)N
Versand
Room temperature in continental US; may vary elsewhere.
Speicherung
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 100 mg/mL (358.05 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (75.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Sachse F, et al. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro.Rhinology. 2011 Jun;49(2):168-73.
[Content Brief]
[2]. Podolin PL, et al. 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 proinflamm
[Content Brief]
[3]. Nan J, et al. TPCA-1 is a direct dual inhibitor of STAT3 and NF-κB and regresses mutant EGFR-associated human non-small cell lung cancers. Mol Cancer Ther. 2014 Mar;13(3):617-29.
[Content Brief]
[1]. Sachse F, et al. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro.Rhinology. 2011 Jun;49(2):168-73.
[2]. Podolin PL, et al. 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 proinflamm
[3]. Nan J, et al. TPCA-1 is a direct dual inhibitor of STAT3 and NF-κB and regresses mutant EGFR-associated human non-small cell lung cancers. Mol Cancer Ther. 2014 Mar;13(3):617-29.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
3.5805 mL
17.9025 mL
35.8051 mL
89.5127 mL
5 mM
0.7161 mL
3.5805 mL
7.1610 mL
17.9025 mL
10 mM
0.3581 mL
1.7903 mL
3.5805 mL
8.9513 mL
15 mM
0.2387 mL
1.1935 mL
2.3870 mL
5.9675 mL
20 mM
0.1790 mL
0.8951 mL
1.7903 mL
4.4756 mL
25 mM
0.1432 mL
0.7161 mL
1.4322 mL
3.5805 mL
30 mM
0.1194 mL
0.5968 mL
1.1935 mL
2.9838 mL
40 mM
0.0895 mL
0.4476 mL
0.8951 mL
2.2378 mL
50 mM
0.0716 mL
0.3581 mL
0.7161 mL
1.7903 mL
60 mM
0.0597 mL
0.2984 mL
0.5968 mL
1.4919 mL
80 mM
0.0448 mL
0.2238 mL
0.4476 mL
1.1189 mL
100 mM
0.0358 mL
0.1790 mL
0.3581 mL
0.8951 mL
TPCA-1 Related Classifications
NF-κBStem Cell/WntJAK/STAT SignalingApoptosis
IKKSTATApoptosis
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
TPCA-1507475-17-4TPCA1TPCA 1IKKSTATApoptosisIκB kinaseI kappa B kinase Inhibitorinhibitorinhibit
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