Organic metal halides
Medchemexpress LLC Sepantronium (bromide) | 781600-92-9 | >98% | 750.56 | 25MG
Sepantronium bromide (YM155) is a small molecule inhibitor of survivin, a member of the inhibitor of apoptosis protein (IAP) family. It exhibits potent anticancer activity by suppressing survivin expression, leading to apoptosis in various cancer cell lines.
- Small molecule inhibitor of survivin
- IC50 of 0.54 nM in a cell-free assay
- Potent anticancer activity
- Suppresses survivin expression
- Leads to apoptosis in various cancer cell lines
- Under clinical investigation for the treatment of various cancers
Medchemexpress LLC Sepantronium bromide | 781661-94-7 | 99.4% | 443.29 | 50 MG
Sepantronium bromide (YM-155) is a potent survivin inhibitor with an IC50 of 0.54 nM. It is intended for research use only and is not for patient treatment. This compound appears as a solid, ranging from light yellow to green yellow in color.
- Potent survivin inhibitor with an IC50 of 0.54 nM.
- Suppresses endogenous survivin expression in certain human HRPC cells.
- Inhibits various human cancer cell lines with mutated or truncated p53.
- Increases sensitivity of NSCLC cells to γ-radiation.
- Delays repair of radiation-induced double-strand breaks in nuclear DNA.
- Inhibits tumor growth in PC-3 xenografts.
- Highly distributed to tumor tissue in vivo.
Medchemexpress LLC Saroglitazar magnesium | 1639792-20-3 | 98.85% | 901.42 | 25 MG
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist that exhibits predominant PPARα activity and moderate PPARγ activity, with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
- Novel peroxisome proliferator-activated receptor (PPAR) agonist
- Predominant PPARα activity (EC50 of 0.65 pM in HepG2 cells)
- Moderate PPARγ activity (EC50 of 3 nM in HepG2 cells)
- Causes dose-dependent reductions in serum triglycerides (TG), free fatty acids (FFA), and glucose in db/db mice
- Shows lipid-lowering effects in preclinical models
- Indicated low risk of PPAR-associated side effects in humans
- Appears to have good potential as a novel therapeutic agent for the treatment of dyslipidemia and diabetes
Medchemexpress LLC Saroglitazar magnesium | 1639792-20-3 | 98.9% | 901.42 | 1 ML
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively. It is for research use only and not sold to patients.
- Novel peroxisome proliferator-activated receptor (PPAR) agonist
- Predominant PPARα and moderate PPARγ activity
- EC50 values of 0.65 pM (PPARα) and 3 nM (PPARγ) in HepG2 cells
- For research use only
Medchemexpress LLC BAY-677 | 2117404-84-7 | 98.0% | 400.35 | 10 MG
BAY-677 serves as an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective, and cell-permeable inhibitor of human neutrophil elastase (HNE), demonstrating an IC50 of 20 nM. This compound has also been nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
- Inactive control for BAY-678.
- BAY-678 is an orally bioavailable inhibitor.
- Highly potent and selective inhibitor of human neutrophil elastase.
- Cell-permeable.
- IC50 of 20 nM against HNE.
- Nominated as a chemical probe by SGC.
Medchemexpress LLC Tarloxotinib bromide | 1636180-98-7 | 97.2% | 681.77 | 25 MG
Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor. It is a hypoxia-activated irreversible EGFR-TKI that has shown greater activity compared to erlotinib in preclinical NSCLC models. It has been shown to be metabolized efficiently under hypoxia in human NSCLC cell lines. Tarloxotinib bromide treatment can also regress WT EGFR NSCLC tumor models H125 and H1648 in vivo. It is for research use only and not sold to patients.
- Irreversible EGFR/HER2 inhibitor
- Hypoxia-activated irreversible EGFR-TKI
- Greater activity compared to erlotinib in preclinical NSCLC models
- Metabolized efficiently under hypoxia in human NSCLC cell lines
- Can regress WT EGFR NSCLC tumor models H125 and H1648 in vivo
- For research use only
Medchemexpress LLC BAY-677 | 2117404-84-7 | 98.02% | 400.35 | 100 MG
BAY-677 serves as an inactive control for BAY-678, which is an orally bioavailable, highly potent, selective, and cell-permeable inhibitor of human neutrophil elastase (HNE) with an IC50 of 20 nM. BAY-678 has also been designated as a chemical probe to the public by the Structural Genomics Consortium (SGC).
- Functions as an inactive control.
- Associated with potent HNE inhibitor.
- Nominated as a chemical probe.
Medchemexpress LLC Saroglitazar magnesium | 1639792-20-3 | 98.85% | 901.42 | 100 MG
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity, having EC50 values of 0.65 pM and 3 nM in HepG2 cells. This product is intended for research use only.
- Exhibits predominant PPARα and moderate PPARγ activity.
- Effective in preclinical models, reducing serum triglycerides, free fatty acids, and glucose dose-dependently.
- Potential therapeutic agent for treating dyslipidemia and diabetes.
Medchemexpress LLC BAY-677 | 2117404-84-7 | 98.0% | 400.35 | 50 MG
BAY-677 serves as an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective, and cell-permeable inhibitor of human neutrophil elastase (HNE). BAY-678 has also been designated as a chemical probe for public use through the Structural Genomics Consortium (SGC).
- Inactive control for BAY-678
- Used in research for human neutrophil elastase (HNE) studies
- Related to a chemical probe designated for public use
Medchemexpress LLC Tarloxotinib bromide | 1636180-98-7 | 98.8% | 681.77 | 10 MG
Tarloxotinib bromide is an irreversible EGFR/HER2 inhibitor intended for research use only. It is metabolized efficiently under hypoxia in human NSCLC cell lines, a process inhibited by oxygen. This product demonstrates greater activity compared with erlotinib.
- Irreversible EGFR/HER2 inhibitor.
- Hypoxia-activated.
- Effective in inhibiting WT EGFR in vivo.
- Shown to be metabolized efficiently under hypoxia.
- Overcomes erlotinib-resistance in preclinical NSCLC models.
- Associated with tumor regression and durable inhibition of WT EGFR tumor phosphorylation in xenograft models.
Medchemexpress LLC Tarloxotinib bromide | 1636180-98-7 | 98.75% | 681.77 | 1 ML
Tarloxotinib bromide is an irreversible EGFR/HER2 inhibitor that is efficiently metabolized under hypoxia in human NSCLC cell lines. Cellular anti-proliferative and receptor phosphorylation assays show a 14-80 fold reduction of activity relative to TKI, demonstrating greater activity compared with erlotinib. In vivo studies show that treatment with clinically relevant doses leads to tumor regression and durable inhibition of WT EGFR tumor phosphorylation, and can regress WT EGFR NSCLC tumor models H125 and H1648.
- Irreversible EGFR/HER2 inhibitor
- Efficiently metabolized under hypoxia
- Greater activity compared with erlotinib
- Associated with tumor regression and durable inhibition of WT EGFR tumor phosphorylation
- Can regress WT EGFR NSCLC tumor models H125 and H1648