TPCA-1
TPCA-1 structure
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Common Name | TPCA-1 | ||
|---|---|---|---|---|
| CAS Number | 507475-17-4 | Molecular Weight | 279.290 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 442.6±45.0 °C at 760 mmHg | |
| Molecular Formula | C12H10FN3O2S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 221.5±28.7 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
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IKK2 inhibition using TPCA-1-loaded PLGA microparticles attenuates laser-induced choroidal neovascularization and macrophage recruitment.
PLoS ONE 10 , e0121185, (2015) The inhibition of NF-κB by genetic deletion or pharmacological inhibition of IKK2 significantly reduces laser-induced choroid neovascularization (CNV). To achieve a sustained and controlled intraocular release of a selective and potent IKK2 inhibitor, 2-[(ami... |
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Breaking resistance of pancreatic cancer cells to an attenuated vesicular stomatitis virus through a novel activity of IKK inhibitor TPCA-1.
Virology 485 , 340-54, (2015) Vesicular stomatitis virus (VSV) is an effective oncolytic virus against most human pancreatic ductal adenocarcinoma (PDAC) cell lines. However, some PDAC cell lines are highly resistant to oncolytic VSV-ΔM51 infection. To better understand the mechanism of r... |
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Intestinal expression of Fas and Fas ligand is upregulated by bacterial signaling through TLR4 and TLR5, with activation of Fas modulating intestinal TLR-mediated inflammation.
J. Immunol. 193(12) , 6103-13, (2014) TLRs play an important role in mediating intestinal inflammation and homeostasis. Fas is best studied in terms of its function in apoptosis, but recent studies demonstrate that Fas signaling may mediate additional functions such as inflammation. The role of F... |
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Dehydrocrenatidine is a novel janus kinase inhibitor.
Mol. Pharmacol. 87(4) , 572-81, (2015) Janus kinase (JAK) 2 plays a pivotal role in the tumorigenesis of signal transducers and activators of transcription (STAT) 3 constitutively activated solid tumors. JAK2 mutations are involved in the pathogenesis of various types of hematopoietic disorders, s... |
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Divergent signalling pathways regulate lipopolysaccharide-induced eRNA expression in human monocytic THP1 cells.
FEBS Lett. 589(3) , 396-406, (2015) Recent studies have indicated that non-coding RNAs transcribed from enhancer regions are important regulators of enhancer function and gene expression. In this report, we have characterised the expression of six enhancer RNAs (eRNAs) induced in human monocyti... |
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IKKβ regulates endothelial thrombomodulin in a Klf2-dependent manner.
J. Thromb. Haemost. 12(9) , 1533-44, (2014) Endothelial thrombomodulin (TM) is critically involved in anticoagulation, anti-inflammation, cytoprotection and normal fetal development. Tumor necrosis factor alpha (TNFα) suppresses TM expression.TNFα has been shown to down-regulate TM partly via activatio... |
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Inhibition of IGF-1 signalling enhances the apoptotic effect of AS602868, an IKK2 inhibitor, in multiple myeloma cell lines.
PLoS ONE 6(7) , e22641, (2011) Multiple myeloma (MM) is a B cell neoplasm characterized by bone marrow infiltration with malignant plasma cells. IGF-1 signalling has been explored as a therapeutic target in this disease. We analyzed the effect of the IKK2 inhibitor AS602868, in combination... |
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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 proinflammatory cytokines and antigen-induced T cell Proliferation.
J. Pharmacol. Exp. Ther. 312 , 373-381, (2005) Demonstration that IkappaB kinase 2 (IKK-2) plays a pivotal role in the nuclear factor-kappaB-regulated production of proinflammatory molecules by stimuli such as tumor necrosis factor (TNF)-alpha and interleukin (IL)-1 suggests that inhibition of IKK-2 may b... |
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IkappaB kinase-2-independent and -dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic.
Mol. Pharmacol. 69 , 1791-1800, (2006) Nuclear factor kappaB (NF-kappaB) is a transcription factor believed to be central in the expression of numerous inflammatory genes and the pathogenesis of many respiratory diseases. We have previously demonstrated increased NF-kappaB pathway activation in a ... |
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Neutrophil-Mediated Delivery of Therapeutic Nanoparticles across Blood Vessel Barrier for Treatment of Inflammation and Infection.
ACS Nano 9 , 11800-11, (2015) Endothelial cells form a monolayer in lumen of blood vessels presenting a great barrier for delivery of therapeutic nanoparticles (NPs) into extravascular tissues where most diseases occur, such as inflammation disorders and infection. Here, we report a strat... |