GLPBio

TPCA-1

Catalog No.: GC17621Purity:>98.00%
COASDSData Sheet
TPCA-1 is an orally active IKK-2 inhibitor with an IC50 of 17.9nM.

Products are for research use only. Not for human use. We do not sell to patients.

TPCA-1
Cas No.: 507475-17-4
10mM (in 1mL DMSO)In Stock
$50.00
1
1mgIn Stock
$23.00
1
2mgIn Stock
$32.00
1
5mgIn Stock
$51.00
1
10mgIn Stock
$85.00
1
25mgIn Stock
$156.00
1
50mgIn Stock
$227.00
1
100mgIn Stock
$327.00
1
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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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Description

TPCA-1 is an orally active IKK-2 inhibitor with an IC50 of 17.9nM. TPCA-1 blocks IκBα phosphorylation by inhibiting IKK-2, thereby suppressing NF-κB nuclear translocation. TPCA-1 inhibits STAT3 phosphorylation and activation to suppress inflammation and tumor-related signaling. TPCA-1 can be used in studies of inflammatory diseases and tumors[1-4].

In vitro, treatment of HPAF-II cells with 8μM TPCA-1 for 48 hours reduced the protein expression of antiviral genes MxA and OAS. Treatment of HPAF-II, Hs766T, CFPAC-1, and HPAC cells with 8μM TPCA-1 for 48 hours followed by infection with VSV-ΔM51-GFP enhanced virus-mediated cell death[5]. Treatment of TNF-α-induced U87 cells with 2-16μM TPCA-1 for 2 hours inhibited RelA nuclear translocation. Pretreatment of U87 cells with 2-16μM TPCA-1 for 2 hours followed by treatment with 1000U/mL IFN-α for 48 hours attenuated the protective effect of cells against vesicular stomatitis virus-induced cytopathy and promoted viral replication[6]. Treatment of KYSE-150, KYSE-180, KYSE-450, and Het-1A cells with 0.5-4μM TPCA-1 for 2 days to 2 weeks induced apoptosis, inhibited IKKβ phosphorylation, stabilized IκBα, suppressed NF-κB signaling pathway, inhibited cell viability, and suppressed colony formation ability[7].

In vivo, a single intravenous injection of 200μg/kg TPCA-1 was given to chronic periodontitis model C57BL/6 mice. The treatment reduced mRNA levels of IL-6, TNF, and IL-1b in gingival tissue. A single intravenous injection of 200μg/kg TPCA-1 was given to wild-type chronic periodontitis model C57BL/6 mice. TPCA-1 reduced cementum-enamel junction to alveolar bone crest (CEJ-ABC) distance and decreased the expression of inflammatory factors in gingival tissue[8]. C57BL/6J mice were given 30-50mg/kg TPCA-1 by oral gavage once daily for 10 days. TPCA-1 reduced ethanol intake and preference[9]. C57BL/6 mice were given intraperitoneal injections of 10mg/kg TPCA-1 once daily for 30 days. TPCA-1 significantly increased the number of active young cells and significantly decreased the number of early senescent and late senescent cells in mammary CD49fhighEpCAMlow cells. TPCA-1 restored Bcl11b activity scores and inhibited senescence-related pathways including NF-kB, Jak-Stat, MAPK, and PI3K-Akt[10].

References:

[1] Bhatti FUR, Hasty KA, Cho H. Anti-inflammatory role of TPCA-1 encapsulated nanosomes in porcine chondrocytes against TNF-α stimulation. Inflammopharmacology. 2019 Oct;27(5):1011-1019.

[2] Wu B, Wang Z, Liu J, et al. Dual rectification of metabolism abnormality in pancreatic cancer by a programmed nanomedicine. Nat Commun. 2024 Dec 3;15:10526.

[3] Zhang C, Lin W, Gao J, et al. pH-Responsive Nanoparticles Targeted to Lungs for Improved Therapy of Acute Lung Inflammation/Injury. ACS Appl Mater Interfaces. 2019 May 08;11(18):16380-16390.

[4] Wang Z, Yang J, Yang Y, et al. Targeted and Combined TPCA-1-Gold Nanocage Therapy for In Vivo Treatment of Inflammatory Arthritis. AAPS PharmSciTech. 2020;21:298.

[5] Cataldi M, Shah NR, Feltz S, et al. Breaking Resistance of Pancreatic Cancer Cells to an Attenuated Vesicular Stomatitis Virus Through a Novel Activity of IKK inhibitor TPCA-1. Virology. 2015 Nov;485:340-54.

[6] Du Z, Whitt MA, Baumann J, et al. Inhibition of Type I Interferon-Mediated Antiviral Action in Human Glioma Cells by the IKK Inhibitors BMS-345541 and TPCA-1. J Interferon Cytokine Res. 2012 Aug;32(8):368-77.

[7] Li Z, Zou L, Xiao Z, et al. Transcriptome-based drug repositioning identifies TPCA-1 as a potential selective inhibitor of esophagus squamous carcinoma cell viability. Int J Mol Med. 2022;49(6):75.

[8] Wang B, Bai S, Wang J, et al. TPCA-1 negatively regulates inflammation mediated by NF-kB pathway in mouse chronic periodontitis model. Mol Oral Microbiol. 2021;00:1-10.

[9] Truitt JM, Blednov YA, Benavidez JM, et al. Inhibition of IKKβ Reduces Ethanol Consumption in C57BL/6J Mice. eNeuro. 2016 Sep/Oct;3(5):e0256-16.2016.

[10] Bai H, Liu X, Lin M, et al. Progressive senescence programs induce intrinsic vulnerability to aging-related female breast cancer. Nat Commun. 2024 Jun 17;15:5154.

Protocol

Cell experiment [1]:

Cell lines

 HPAF-II, Hs766T, CFPAC-1, HPAC, AsPC-1, Mia PaCa-2 (human pancreatic ductal adenocarcinoma cell lines), BHK-21 (baby hamster kidney fibroblasts), Vero (African green monkey kidney cells)

Preparation Method

 HPAF-II and other PDAC cells were maintained in appropriate media with 10% FBS at 37°C, 5% CO2. Cells were treated with TPCA-1 at 2-16μM for 48h prior to infection with VSV-ΔM51-GFP or SeV-GFP-Fmut, with treatment maintained post-infection; lysates were analyzed by Western blot, GFP fluorescence, MTT, flow cytometry, real-time PCR, EMSA and JAK1 kinase assay.

Reaction Conditions

 2-16μM; 48h pretreatment

Applications

 TPCA-1 decreased MxA and OAS expression, inhibited STAT1 and STAT2 phosphorylation, blocked ISRE binding, directly inhibited JAK1 kinase activity, enhanced VSV-ΔM51-GFP and SeV-GFP-Fmut replication, increased GFP-positive cell percentage, and reduced cell viability in VSV-infected HPAF-II cells.
Animal experiment [2]:

Animal models

 C57BL/6J mice

Preparation Method

Mice were orally administered TPCA-1 freshly prepared as suspension in saline with Tween-80 (30mg/kg or 50mg/kg) 30min prior to ethanol presentation in continuous 24h two-bottle choice test or limited-access 3h drinking-in-the-dark two-bottle choice test; ethanol intake, preference and total fluid intake were measured at 6h/24h or end of 3h drinking period.

Dosage form

30-50mg/kg; p.o.; daily for 10 days

Applications

TPCA-1 at 50mg/kg reduced ethanol intake and preference in both continuous 24h two-bottle choice and 3h drinking-in-the-dark two-bottle choice tests, while 30mg/kg showed no significant change in continuous 24h test, and neither dose altered total fluid intake.

References:

[1] Cataldi M, Shah NR, Feltz SA, et al. Breaking Resistance of Pancreatic Cancer Cells to an Attenuated Vesicular Stomatitis Virus Through a Novel Activity of IKK inhibitor TPCA-1. Virology. 2015 Nov;485:340-354.

[2] Truitt JM, Blednov YA, Benavidez JM, et al. Inhibition of IKKβ Reduces Ethanol Consumption in C57BL/6J Mice. eNeuro. 2016 Oct 19;3(5):e0256-16.2016.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
507475-17-4
Chemical Name
2-(carbamoylamino)-5-(4-fluorophenyl)thiophene-3-carboxamide
SMILES
C1=CC(=CC=C1C2=CC(=C(S2)NC(=O)N)C(=O)N)F
Molecular Formula
C12H10FN3O2S
Molecular Weight
279.29
Solubility
≥ 13.95mg/mL in DMSO, ≥ 2.53 mg/mL in EtOH with ultrasonic and warming
Storage
Desiccate at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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