PX-12

Modify Date: 2024-01-02 11:00:57

PX-12 structure	Common Name	PX-12
	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-12

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.

Name	2-(butan-2-yldisulfanyl)-1H-imidazole
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.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cancer
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	[1]. Welsh SJ, et al. The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1alpha and vascular endothelial growth factor formation. Mol Cancer Ther. 2003 Mar;2(3):235-43. [2]. Metcalfe C, et al. Thioredoxin Inhibitors Attenuate Platelet Function and Thrombus Formation.PLoS One. 2016 Oct 7;11(10):e0163006 [3]. Ramanathan RK, et al. A Phase I pharmacokinetic and pharmacodynamic study of PX-12, a novel inhibitor of thioredoxin-1, in patients with advanced solid tumors. Clin Cancer Res. 2007 Apr 1;13(7):2109-14. [4]. Wang F, et al. Thioredoxin-1 inhibitor, 1-methylpropyl 2-imidazolyl disulfide, inhibits the growth, migration and invasion of colorectal cancer cell lines. Oncol Rep. 2015 Feb;33(2):967-73. [5]. Lou M, et al. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149.

Density	1.2±0.1 g/cm3
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℃

PX-12 MSDS(Chinese)

Symbol	GHS07
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
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...

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...

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

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: PX-12
Price: ￥3426.0/50mg ￥676.0/5mg ￥1806.0/25mg ￥896.0/10mg
Purity: 98.0%
Stocking Period: 2 Day
Contact: Liu jia

DC Chemicals Limited
China
Product Name: PX 12
Price: $250.0/100mg $500.0/250mg $1000.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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PX-12

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