TPCA-1

Name: TPCA-1
Brand: MedChemExpress
SKU: HY-10074
Rating: 5.0 (34 reviews)

Cat. No.: HY-10074 Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

TPCA-1 Chemical Structure

CAS No. : 507475-17-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 111	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 111	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 121	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 352	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 539	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 34 publication(s) in Google Scholar

31 Publications Citing Use of MCE TPCA-1

Proliferation Assay

: 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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.

Animal Model:	Six-week-old BALB/c female nude mice injected subcutaneously with HCC827 cells (5×10⁶)^[3].
Dosage:	10 mg/kg.
Administration:	Intraperitoneally daily.
Result:	The tumor weight inhibition rate of TPCA-1, ZD1839, and their combination are 0.419(E_TPCA-1), 0.680(E_ZD1839), and 0.837(E_observed), respectively.

Molecular Weight

279.29

Formula

C₁₂H₁₀FN₃O₂S

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

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

Concentration Solvent Mass	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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO 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)
Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 7.5 mg/mL (26.85 mM); Clear solution

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 μL DMSO stock solution (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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.

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.

Purity & Documentation

Purity: 99.72%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (251 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

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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TPCA-1

Customer Review

TPCA-1 Related Antibodies

31 Publications Citing Use of MCE TPCA-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All IKK Isoform Specific Products:

View All STAT Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

TPCA-1 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

TPCA-1 Related Classifications

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