PX-12 structure
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Common Name | PX-12 | ||
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CAS Number | 141400-58-0 | Molecular Weight | 188.314 | |
Density | 1.2±0.1 g/cm3 | Boiling Point | 330.0±25.0 °C at 760 mmHg | |
Molecular Formula | C7H12N2S2 | Melting Point | N/A | |
MSDS | Chinese USA | Flash Point | 153.4±23.2 °C | |
Symbol |
GHS07 |
Signal Word | Warning |
Use of PX-12PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively. |
Name | 2-(butan-2-yldisulfanyl)-1H-imidazole |
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Synonym | More Synonyms |
Description | PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively. |
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Related Catalog | |
Target |
IC50: 1.9 (MCF-7), 2.9 μM (HT-29 cells)[1] |
In Vitro | PX-12 inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively[1]. PX-12 particularly reduces the activity of Trx-1 by means of thio-alkylating critical cysteine residue (Cys73) which is located in the outside the conserved redox catalytic site of Trx-1. PX-12 affects the oxidation state of thiols in a number of cell surface proteins. Key surface receptors for platelet adhesion and activation are affected, including the collagen receptor GPVI and the von Willebrand factor receptor, GPIb. PX-12 inhibits thrombus formation over Type I collagen in whole blood under flow conditions[2]. Thioredoxin-1 (Trx-1) is a cellular redox protein that promotes tumor growth, inhibits apoptosis, and up-regulates hypoxia-inducible factor-1α and vascular endothelial growth factor[3]. PX-12 inhibits the growth of colorectal cancer DLD-1 and SW620 cells in a dose- and time-dependent manner. PX-12 reduces cell colony formation and induced a G2/M phase arrest of the cell cycle. PX-12 treatment induces apoptosis. PX-12 inhibits colorectal cancer cell migration and invasion. Treatment of cancer cells with PX-12 reduces NOX1, CDH17 and S100A4 mRNA expression, and increases KLF17 mRNA expression. PX-12 decreases S100A4 protein expression in the colorectal cancer cells[4]. |
In Vivo | PX-12 has been shown to have in vivo antitumor activity against human tumor xenografts including HT-29 colon cancer in SCID mice and has been tested in a phase I clinical trial in patients[3]. |
References |
Density | 1.2±0.1 g/cm3 |
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Boiling Point | 330.0±25.0 °C at 760 mmHg |
Molecular Formula | C7H12N2S2 |
Molecular Weight | 188.314 |
Flash Point | 153.4±23.2 °C |
Exact Mass | 188.044189 |
PSA | 79.28000 |
LogP | 3.40 |
Vapour Pressure | 0.0±0.7 mmHg at 25°C |
Index of Refraction | 1.590 |
Storage condition | -20℃ |
Symbol |
GHS07 |
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Signal Word | Warning |
Hazard Statements | H315-H319-H335 |
Precautionary Statements | P261-P305 + P351 + P338 |
RIDADR | NONH for all modes of transport |
HS Code | 2933290090 |
HS Code | 2933290090 |
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Summary | 2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
The overexpression and nuclear translocation of Trx-1 during hypoxia confers on HepG2 cells resistance to DDP, and GL-V9 reverses the resistance by suppressing the Trx-1/Ref-1 axis.
Free Radic. Biol. Med. 82 , 29-41, (2015) Microenvironmental hypoxia gives many tumor cells the capacity for drug resistance. Thioredoxin family members play critical roles in the regulation of cellular redox homeostasis in a stressed environ... |
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Inhibition of thioredoxin 1 leads to apoptosis in drug-resistant multiple myeloma.
Oncotarget 6 , 15410-24, (2015) Multiple myeloma (MM) is a hematological malignancy characterized by the aberrant accumulation of clonal plasma cells in the bone marrow. Despite recent advancement in anti-myeloma treatment, MM remai... |
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Thioredoxin is involved in endothelial cell extracellular transglutaminase 2 activation mediated by celiac disease patient IgA.
PLoS ONE 8 , e77277, (2013) To investigate the role of thioredoxin (TRX), a novel regulator of extracellular transglutaminase 2 (TG2), in celiac patients IgA (CD IgA) mediated TG2 enzymatic activation.TG2 enzymatic activity was ... |
2-(butan-2-yldisulfanyl)-1H-imidazole |
IV-2 compound |
UNII:8PQ9CZ8BTJ |
1-methylpropyl 2-imidazolyl disulfide |
PX 12 |
1-methyl-1-propyl 2-imidazolyl disulfide |
2-(sec-Butyldisulfanyl)-1H-imidazole |
1-methylpropyl 2-mercaptoimidazolyl disulfide |
2-[(1-Methylpropyl)dithio]-1H-imidazole |
1H-Imidazole, 2-[(1-methylpropyl)dithio]- |
PX-12 |