Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H6824 |
PACMA31 |
1401089-31-3 | An orally active, irreversible inhibitor of protein disulfide isomerase (PDI), forming a covalent bond with the active site cysteines of PDI; significantly inhibits human ovarian cancer cells OVCAR-8, HEY, and OVCAR-8 growth with IC50 of 0.9, 1.4, and 0.32 uM; significantly suppresses ovarian tumor growth without causing toxicity to normal tissues in mouse xenograft model of human OVCAR-8 ovarian cancer. |
H6823 |
ML359 |
1069858-99-6 | ML359 is a small molecule, specific inhibitor of Protein disulfide isomerase (PDI) with IC50 of 250 nM; displays >100-fold selectivity over other thiol isomerases (Erp5, Thioredoxin, Thioredoxin reductase); shows no cytotoxicity in three human cell lines, and some activity in inhibiting platelet aggregation in vitro. |
H6822 |
LOC-14 |
877963-94-5 | A small molecule reversible Protein disulfide isomerase (PDI) inhibitor with Kd of 62 nM; LOC14-induced oxidation of PDI has a neuroprotective effect not only in cell culture, but also in corticostriatal brain slice cultures; exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding; |
H6821 |
KSC-34 |
2226201-97-2 |
KSC-34 (PDIA1 inhibitor KSC-34) is a potent, selective protein disulfide isomerase A1 (PDIA1) inhibitor, 30-fold selectivity for the A-site over the A' site; displays time-dependent inhibition of PDIA1 reductase activity in vitro with a kinact/ KI of 9.66 ¡Á 103 M-1 s-1 and is selective for PDIA1 over other members of the PDI family, and other cellular cysteine-containing proteins; significantly decreases the rate of secretion of a destabilized, amyloidogenic antibody light chain, thereby minimizing pathogenic amyloidogenic extracellular proteins in treated cells. |
H6820 |
Juniferdin |
74724-29-1 | Juniferdin is a small molecule, potent Protein disulfide isomerase (PDI) inhibitor with IC50 of 156 nM, inhibits PDI-mediated reduction of HIV-1 envelope glycoprotein gp120; significantly reduces the replication of influenza A and B viruses in MDCK and A549 cells. |
H6819 |
E64FC26 |
2285446-62-8 |
E64FC26 is a highly potent pan-style inhibitor of Protein Disulfide Isomerase (PDI) with IC50 of 1.9 uM (PDIA1), also inhibits all other members of the PDI family, including PDIA3, PDIA4, TXNDC5, and PDIA6; induces robust ER stress response in MM cells, with expression of ER stress markers ATF4 and CHOP; induces an oxidative stress response in a panel of heterogeneous PI sensitive and resistant cell lines that was characterized by the induction of Nrf2, synergistically enhances the anti-MM cytotoxic effects of PIs; improves survival and enhanced the activity of bortezomib without any adverse effects. |
H6818 |
CCF-642 |
346640-08-2 |
CCF-642 (CCF642) is a novel covalent protein disulfide isomerase (PDI) inhibitor that shows antimyeloma activity; inhibits PDI reductase activity about 100-fold more potently than PACMA 31 and LOC14; shows cytotoxicity against MM cells with a submicromolar IC50, causes acute ER stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release; displays potent efficacy and prolongs the lifespan in an aggressive syngeneic mouse model of multiple myeloma. |
H6817 |
16F16 |
922507-80-0 | A small molecule protein disulfide isomerase (PDI) inhibitor that suppress apoptosis induced by misfolded proteins; protects rat neurons from cell death triggered by Aβ peptide; reduces Zika virus replication in vitro but demonstrates notable toxicity; inhibits CHIKV E1-induced cell-cell fusion. |
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