[CAS NO. 141400-58-0]  PX-12

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PRODUCTS SPECIFICATIONS [141400-58-0]

Catelog
SLK-S7947
Brand
Selleck
CAS
141400-58-0

DESCRIPTION [141400-58-0]

Overview

MDLMFCD18086851
Molecular Weight188.31
Molecular FormulaC7H12N2S2
SMILESCCC(SSC1=NC=CN1)C

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM5.3104 mL26.5520 mL53.1039 mL
5 mM1.0621 mL5.3104 mL10.6208 mL
10 mM0.5310 mL2.6552 mL5.3104 mL
50 mM0.1062 mL0.5310 mL1.0621 mL

Description

PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide) is a potent inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2.

Targets

Trx-1 [1]

In vitro

In MCF-7 and HT-29 cells, PX-12 prevents the hypoxia (1% oxygen)-induced increase in HIF-1alpha protein, and decreases HIF-1-trans-activating activity, VEGF formation, and inducible nitric oxide synthase. PX-12 also inhibits the growth of MCF-7 and HT-29 cells with IC50s of 1.9 μM and 2.9μM, respectively. PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity.

In vivo

In mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density.