Home Metabolism Thioredoxin inhibitor - COVID-19 inhibitor PX-12 For research use only.

PX-12

Synonyms: DB05448, 1-methyl propyl 2-imidazolyl disulfide

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

PX-12 Chemical Structure

PX-12 Chemical Structure

CAS No. 141400-58-0

Purity & Quality Control

PX-12 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T84 Function assay 3 hrs Inhibition of human recombinant thioredoxin-mediated TG2 activation expressed in T84 cells assessed as blockade of 5-biotinamidopentylamine incorporation after 3 hrs by fluorescence microscopic analysis, IC50=2.11μM 23327656
MEF Cytotoxicity assay Cytotoxicity against mouse MEF cells, LD50=2.7μM 22128876
Ramos Cytotoxicity assay 72 hrs Cytotoxicity against human Ramos cells after 72 hrs by MTT assay, LD50=3.4μM 22128876
PancO2 Cytotoxicity assay 72 hrs Cytotoxicity against mouse PancO2 cells after 72 hrs by crystal violet staining, LD50=3.9μM 22128876
T24 Cytotoxicity assay 72 hrs Cytotoxicity against human T24 cells after 72 hrs by crystal violet staining, LD50=4.6μM 22128876
B78 Cytotoxicity assay 72 hrs Cytotoxicity against mouse B78 cells after 72 hrs by crystal violet staining, LD50=5μM 22128876
CT26 Cytotoxicity assay 72 hrs Cytotoxicity against wild type mouse CT26 cells after 72 hrs by crystal violet staining, LD50=5.2μM 22128876
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by MTT assay, LD50=5.5μM 22128876
M21 Antiproliferative assay Antiproliferative activity against human M21 cells, GI50=8.3μM 18502639
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, GI50=8.3μM 18502639
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B method, GI50=8.3μM 18617414
M21 Antiproliferative assay 48 hrs Antiproliferative activity against human M21 cells after 48 hrs by sulforhodamine B method, GI50=8.3μM 18617414
Raji Cytotoxicity assay 72 hrs Cytotoxicity against human Raji cells after 72 hrs by MTT assay, LD50=8.8μM 22128876
EMT6 Cytotoxicity assay 72 hrs Cytotoxicity against mouse EMT6 cells after 72 hrs by crystal violet staining, LD50=11.6μM 22128876
HT29 Antiproliferative assay Antiproliferative activity against human HT29 cells, GI50=25μM 18502639
HT29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B method, GI50=25μM 18617414
M21 Function assay 25 nM 16 hrs Stimulation of nuclear translocation of thioredoxin-1 from cytosol in human M21 cells at 25 nM after 16 hrs by immunocytofluorescence 18617414
Raji Function assay 5 to 10 uM 4 to 24 hrs Induction of Trx mRNA expression in human Raji cells at 5 to 10 uM after 4 to 24 hrs by RT-PCR analysis 22128876
Raji Function assay 10 to 20 uM 4 to 8 hrs Induction of Trx protein expression in human Raji cells at 10 to 20 uM after 4 to 8 hrs by Western blot analysis 22128876
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description PX-12 (DB05448, 1-methyl propyl 2-imidazolyl disulfide) is a potent thioredoxin-1 (Trx-1) inhibitor by irreversibly thioalkylation of Cys73 of Trx-1. Phase 2.
Targets
Trx-1 [1]
In vitro
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. [1] PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. [2] In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. [3] In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity. [4]
Cell Research Cell lines MCF-7 and HT-29 cells
Concentrations ~10 μM
Incubation Time 72 h
Method Cell growth is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cells are exposed to a range of concentrations of PX-12 or pleurotin for 16 h in air or hypoxia (1% oxygen). The cells are then washed with warm drug-free medium and grown in air for the remainder of the 72-h incubation.
In Vivo
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. [1]
Animal Research Animal Models Mice bearing MCF-7 tumor xenografts
Dosages 12 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00736372 Completed
Metastatic Cancer|Advanced Cancer
Cascadian Therapeutics Inc.|Seagen Inc.
 June 2008 Phase 1
NCT00417287 Terminated
Pancreatic Neoplasms
Cascadian Therapeutics Inc.|National Cancer Institute (NCI)|Translational Genomics Research Institute|Seagen Inc.
 December 2006 Phase 2

Chemical Information & Solubility

Molecular Weight 188.31 Formula

C7H12N2S2
CAS No. 141400-58-0 SDF Download PX-12 SDF
Smiles CCC(C)SSC1=NC=CN1
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 38 mg/mL ( (201.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 38 mg/mL

Water : Insoluble


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