Phenanthrenes and derivatives
Medchemexpress LLC Quinacrine dihydrochloride | 69-05-6 | MFCD00012659 | 99.4% | 472.88 | 200 MG
Quinacrine dihydrochloride (Mepacrine dihydrochloride) is an orally bioavailable antimalarial agent with anticancer effects both in vitro and in vivo. It suppresses NF-κB and activates p53 signaling, leading to the induction of apoptosis. It is for research use only and not sold to patients.
- Orally bioavailable antimalarial agent
- Exhibits anticancer effects in vitro and in vivo
- Suppresses NF-κB and activates p53 signaling
- Induces apoptosis
- Increases proapoptotic proteins and decreases antiapoptotic proteins
- Suppresses circulating blast cells in AML models
- Increases median survival time in AML models
Medchemexpress LLC Vardenafil hydrochloride | 224785-91-5 | 99.8% | 200 MG
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5) with an IC50 of 0.7 nM, showing lower inhibition of PDE1, PDE6, PDE3, and PDE4. It competitively inhibits cGMP hydrolysis, leading to increased cGMP levels. It is used for research of erectile dysfunction, hepatitis, and diabetes.
- Specifically inhibits cGMP hydrolysis by PDE5, increasing intracellular cGMP levels for increased dilation and blood flow.
- Exhibits facilitator effects in rats with cavernous nerve injury.
- Protects the liver against Con A-induced hepatitis in mice and decreases NF-κB expression.
- Prevents reduction of tissue cGMP levels and increased 3-NT generation in ZDF hearts.
Apexbio Technology LLC CVT-313 199986-75-9 200mg
CVT-313 (CAS 199986-75-9) is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) an enzyme essential for G1/S transition during cell cycle progression By targeting CDK2 CVT-313 effectively reduces hyperphosphorylation of retinoblastoma protein (Rb) leading to cell cycle arrest at the G1/S boundary In vitro studies with MRC-5 fibroblasts demonstrated significant growth inhibition Additionally CVT-313 induces apoptosis in diffuse large B-cell lymphoma by diminishing phosphorylation of Rb at T821 and downregulating anti-apoptotic protein Mcl-1 In animal models of arterial restenosis CVT-313 significantly reduces neointimal proliferation indicating potential utility for proliferative disorders research
Medchemexpress LLC PROTAC BCR-ABL1 ligand 1 | 2489876-34-6 | 99.17% | 50 MG
PROTAC BCR-ABL1 ligand 1, also known as compound GMB-475, is a PROTAC ligand that allosterically targets the BCR-ABL1 protein. It functions by recruiting the E3 ligase Von Hippel-Lindau, which leads to the ubiquitination and subsequent degradation of BCR-ABL1.
- Allosterically targets the BCR-ABL1 protein.
- Recruits the E3 ligase Von Hippel-Lindau.
- Induces ubiquitination and subsequent degradation of BCR-ABL1.
- Inhibits cell proliferation with IC50 values of 1.11 μM for WT cells, 1.98 μM for T315I cells, and 0.37 μM for G250E cells.
- Induces the degradation of c-ABL1.
- Inhibits downstream signaling through the STAT5 pathway in K562 and Ba/F3 cells.
Medchemexpress LLC Alvespimycin (hydrochloride) | 467214-21-7 | 98.8% | 653.21 | 200 MG
Alvespimycin hydrochloride is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 ± 29 nM. It inhibits the growth of human cancer cell lines SKBR3 and SKOV3, which overexpress Hsp90 client protein Her2, leading to down-regulation of Her2 and induction of Hsp70. It also induces dose-dependent apoptosis in chronic lymphocytic leukemia (CLL) cells.
- Potent inhibitor of Hsp90
- Binds to Hsp90 with an EC50 of 62 ± 29 nM
- Inhibits the growth of human cancer cell lines SKBR3 and SKOV3
- Causes down-regulation of Her2
- Induces Hsp70
- Induces dose-dependent apoptosis in chronic lymphocytic leukemia (CLL) cells
- Significant reduction in tumor size in animal models
Medchemexpress LLC Crizotinib hydrochloride | 1415560-69-8 | 99.7% | C21H23Cl3FN5O | 200 MG
Crizotinib hydrochloride is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor. It also acts as a ROS proto-oncogene 1 (ROS1) inhibitor, demonstrating effective tumor growth inhibition.
- Inhibits tyrosine phosphorylation of NPM-ALK and c-Met in cell-based assays
- Potently prevents cell proliferation by inducing G(1)-S-phase cell cycle arrest and apoptosis
- Causes marked regression of large established tumors in preclinical models
- Demonstrates a significant dose-dependent reduction of CD31-positive endothelial cells
- Leads to marked inhibition of phosphorylated c-Met, Akt, Erk, PLCλ1, and STAT5 levels
Medchemexpress LLC PROTAC BCR-ABL1 ligand 1 | 2489876-34-6 | 99.2% | 100 MG
PROTAC BCR-ABL1 ligand 1, also known as compound GMB-475, is a PROTAC ligand that allosterically targets the BCR-ABL1 protein. It recruits the E3 ligase Von Hippel-Lindau, leading to ubiquitination and subsequent degradation of BCR-ABL1. It is for research use only and not sold to patients.
- Allosterically targets the BCR-ABL1 protein.
- Recruits the E3 ligase Von Hippel-Lindau for ubiquitination and degradation of BCR-ABL1.
- Exhibits cell proliferation with IC50 values of 1.11, 1.98, and 0.37 μM for BCR-ABL1 WT, T315I, and G250E cells.
- Induces the degradation of BCR-ABL1 and c-ABL1.
- Inhibits downstream signaling via the STAT5 pathway in K562 and Ba/F3 cells.
- Intended for research use only.