Indoles and derivatives
Medchemexpress LLC MY-875 | C21H25NO6 | 100 MG
MY-875 is a competitive inhibitor of microtubulin polymerization with an IC50 value of 0.92 μM. It functions by targeting colchicine binding sites and activates the Hippo pathway, leading to apoptosis and anticancer activity against various cancer cell lines.
- Competitive inhibitor of microtubulin polymerization
- Targets colchicine binding sites
- Activates the Hippo pathway
- Induces apoptosis and anticancer activity
- Exhibits anti-proliferative activity against various cancer cells
- Inhibits microtubule protein polymerization and β-tubulin alkylation
- Induces phosphorylation of MST and LATS, leading to YAP degradation
- Inhibits cell colony-forming ability and arrests cells in the G2/M phase
Medchemexpress LLC Oncrasin-1 | 75629-57-1 | 98.16% | 269.73 | 1 ML
Oncrasin-1 is an RNA polymerase inhibitor that suppresses the phosphorylation of the largest subunit of RNA polymerase II and the expression of intronless reporter genes in sensitive cells. It effectively kills various human lung cancer cells with K-Ras mutations, leading to coaggregation of PKCι and splicing factors into megaspliceosomes and inducing malfunction in the RNA processing machinery. Oncrasin-1 is an anti-cancer agent and can be studied in research for lung cancer.
- RNA polymerase inhibitor
- Suppresses phosphorylation of the largest subunit of RNA polymerase II
- Suppresses expression of intronless reporter genes in sensitive cells
- Effectively kills various human lung cancer cells with K-Ras mutations
- Leads to coaggregation of PKCι and splicing factors into megaspliceosomes
- Induces malfunction in the RNA processing machinery
- Anti-cancer agent for lung cancer research
Medchemexpress LLC Indomethacin sodium hydrate | 74252-25-8 | MFCD00227184 | 99.85% | 10 MM * 1 ML in DMSO
Indomethacin sodium hydrate is an orally active and BBB-permeable COX1/2 inhibitor, demonstrating IC50 values of 18 nM for COX-1 and 26 nM for COX-2. It exhibits both anticancer and anti-infective activities, making it suitable for research in cancer, inflammation, and viral infections.
- In vitro studies show Indomethacin sodium hydrate (0-150 μM; 24 hours; 3LL-D122 cells) possesses anticancer activity.
- It protects host cells from virus-induced damage by activating PKR, which results in eIF2α phosphorylation.
- This mechanism leads to the inhibition of viral protein translation and replication, with an IC50 of 2 μM.
Medchemexpress LLC ML334 | 1432500-66-7 | 98.1% | 446.50 | 1 ML
ML334 is a potent, cell-permeable activator of NRF2, functioning by inhibiting the Keap1-NRF2 protein-protein interaction. It binds to the Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation, leading to the induction of antioxidant response elements (ARE) activity.
- Potent, cell permeable activator of NRF2.
- Inhibits Keap1-NRF2 protein-protein interaction.
- Binds to Keap1 Kelch domain with a Kd of 1 μM.
- Stimulates NRF2 expression and nuclear translocation.
- Induces antioxidant response elements (ARE) activity.
- Increases NQO1 and TRX1 mRNAs in HEK293 cells.
- Enhances HO-1 mRNA expression in HEK293 cells.
- Induces HO-1 and TRX1 proteins in HEK293 cells.
Medchemexpress LLC Oncrasin-1 | 75629-57-1 | 98.2% | 269.73 | 100 MG
Oncrasin-1 is an RNA polymerase inhibitor that suppresses the phosphorylation of RNA polymerase II and the expression of intronless reporter genes in sensitive cells. It effectively kills various human lung cancer cells with K-Ras mutations. It leads to coaggregation of PKCι and splicing factors into megaspliceosomes, inducing malfunction in the RNA processing machinery. This anti-cancer agent can be studied in research for lung cancer.
- RNA polymerase inhibitor
- Suppresses phosphorylation of RNA polymerase II and expression of intronless reporter genes
- Effectively kills human lung cancer cells with K-Ras mutations
- Induces coaggregation of PKCι and splicing factors into megaspliceosomes
- Causes malfunction in the RNA processing machinery
- Anti-cancer agent for lung cancer research
- Appears as a light yellow to khaki solid
Medchemexpress LLC My-875 | 2974348-62-2 | MFCD34676541 | 99.6% | 387.43 | C21H25NO6 | 10 MG
MY-875 is a competitive microtubulin polymerization inhibitor that targets the colchicine binding site and activates the Hippo signaling pathway. It induces apoptosis, causes G2/M cell-cycle arrest, and exhibits dose-dependent antiproliferative activity in multiple cancer cell lines; reported tubulin polymerization IC50 is 0.92 μM. The compound is supplied as a high-purity solid with high solubility in DMSO and recommended storage to preserve stability.
- Competitive microtubulin polymerization inhibitor targeting colchicine binding sites.
- Activates Hippo pathway leading to YAP degradation.
- Induces apoptosis and G2/M cell-cycle arrest in cancer cells.
- Demonstrates potent antiproliferative activity (tubulin polymerization IC50 ~0.92 μM).
- High purity solid with high DMSO solubility for assay preparation.
- Stable under recommended storage conditions for experimental reproducibility.
Medchemexpress LLC AG-270 | 2201056-66-6 | 99.97% | 489.57 | 50 MG
AG-270 is a first-in-class, allosteric, noncompetitive, reversible, and orally active MAT2A inhibitor with an IC50 of 14 nM. It potently reduces intracellular S-adenosylmethionine (SAM) levels and demonstrates MTAP-null-selective antiproliferative activity. In vivo, AG-270 exhibits excellent metabolic stability and leads to dose-dependent reductions in tumor SAM levels and tumor growth in xenografts. Its combination with taxanes and gemcitabine has shown additive-to-synergistic antitumor activity.
- Potent and selective MAT2A inhibitor
- Reduces intracellular SAM levels
- Shows MTAP-null-selective antiproliferative activity
- Excellent metabolic stability across multiple species
- Exhibits dose-dependent reduction in tumor SAM levels and tumor growth
- Additive-to-synergistic antitumor activity in combination with other therapies