Pyridines and derivatives
Apexbio Technology LLC EMD638683 1181770-72-8 5mg
EMD638683 (CAS 1181770-72-8) is a selective inhibitor of serum- and glucocorticoid-inducible kinases (SGKs) including isoforms SGK1 SGK2 and SGK3 SGK1 regulates key cellular processes such as ion transport survival proliferation and responses to steroid hormones EMD638683 shows inhibitory activity against SGK1 SGK2 and SGK3 (IC50 3 M) significantly reducing SGK-dependent phosphorylation of NDRG1 in vitro It demonstrates limited off-target interactions inhibiting only MSK1 and PRK2 at 1 M while sparing numerous other kinases In cell models EMD638683 influences mitochondrial polarization and caspase activity exhibiting antitumor effects in colorectal tumor cells and antihypertensive activity in vivo
Apexbio Technology LLC BMS265246 582315-72-8 10mg
BMS265246 (CAS 582315-72-8) is a potent and selective inhibitor of cyclin-dependent kinases CDK1 and CDK2 demonstrating IC50 values of 6 nM and 9 nM respectively By targeting serine/threonine protein kinases central to cell cycle regulation BMS265246 disrupts CDK-cyclin signaling and effectively inhibits cell proliferation In cellular assays BMS265246 suppresses Cdk4/cycD activity and blocks proliferation in models such as A2780 Cytox cells (IC50 0 23 M and 0 76 M) and HCT-116 cells (EC50 0 293 0 492 M) Treatment induces G2 phase arrest enlarged nuclei and increases in 4N DNA content This compound is valuable for studying cell cycle dynamics and the pharmacology of CDK inhibition in cancer research
Apexbio Technology LLC EMD638683 1181770-72-8 50mg
EMD638683 (CAS 1181770-72-8) is a selective inhibitor of serum- and glucocorticoid-inducible kinases (SGKs) including isoforms SGK1 SGK2 and SGK3 SGK1 regulates key cellular processes such as ion transport survival proliferation and responses to steroid hormones EMD638683 shows inhibitory activity against SGK1 SGK2 and SGK3 (IC50 3 M) significantly reducing SGK-dependent phosphorylation of NDRG1 in vitro It demonstrates limited off-target interactions inhibiting only MSK1 and PRK2 at 1 M while sparing numerous other kinases In cell models EMD638683 influences mitochondrial polarization and caspase activity exhibiting antitumor effects in colorectal tumor cells and antihypertensive activity in vivo
Apexbio Technology LLC BMS265246 582315-72-8 5mg
BMS265246 (CAS 582315-72-8) is a potent and selective inhibitor of cyclin-dependent kinases CDK1 and CDK2 demonstrating IC50 values of 6 nM and 9 nM respectively By targeting serine/threonine protein kinases central to cell cycle regulation BMS265246 disrupts CDK-cyclin signaling and effectively inhibits cell proliferation In cellular assays BMS265246 suppresses Cdk4/cycD activity and blocks proliferation in models such as A2780 Cytox cells (IC50 0 23 M and 0 76 M) and HCT-116 cells (EC50 0 293 0 492 M) Treatment induces G2 phase arrest enlarged nuclei and increases in 4N DNA content This compound is valuable for studying cell cycle dynamics and the pharmacology of CDK inhibition in cancer research
Apexbio Technology LLC Nepafenac 78281-72-8 100mg
Nepafenac (CAS 78281-72-8) is a small-molecule inhibitor targeting cyclooxygenase enzymes COX-1 and COX-2 It is designed to inhibit these enzymes thereby reducing prostaglandin E2 (PGE2) biosynthesis and modulating ocular inflammatory pathways Nepafenac exerts its biological activity primarily through COX-1 and COX-2 inhibition In cell-based studies nepafenac demonstrates inhibitory activity with IC50 values of approximately 250 nM for COX-1 and 150 nM for COX-2 In LPS-induced inflammation models topical application reduces retinal PGE2 concentrations Additionally it has been studied as an inhibitor of cellular proliferation in human uveal melanoma cell lines (SP6 5 92 1 OCM-1 MKT-BR UW-1) Based on these pharmacological properties nepafenac holds research potential in ophthalmologic studies involving inflammatory pathways and ocular malignancies
Medchemexpress LLC Lonicerin | 25694-72-8 | 25 MG
Lonicerin, also known as Veronicastroside, is a flavonoid with a range of biological activities. It is known to inhibit xanthine oxidase, alginate secretion protein (AlgE), *P. aeruginosa*, and *C. albicans*.
- Inhibits xanthine oxidase
- Acts against alginate secretion protein (AlgE)
- Demonstrates antibacterial activity against *P. aeruginosa*
- Exhibits antifungal properties against *C. albicans*
- Provides anti-inflammatory effects
- Has anti-arthritic properties
- Functions as an antioxidant
- Offers neuroprotective benefits
- Reduces biofilm formation
- Suppresses T cell proliferation
- Inhibits nitric oxide production
Medchemexpress LLC Zotiraciclib | 1204918-72-8 | C23H24N4O | 25 MG
Zotiraciclib | 1204918-72-8 | C23H24N4O | 25 MG
Medchemexpress LLC EMD638683 | 1181770-72-8 | C18H18F2N2O4 | 5 MG
EMD638683 is an orally active SGK1 inhibitor with an IC50 of 3 μM, demonstrating strong inhibition of SGK1 and moderate inhibition of SGK2 and SGK3. This compound exhibits excellent selectivity for other AGC kinase family members. It possesses antihypertensive activity by inhibiting SGK1 and effectively prevents heart inflammation and fibrosis caused by hypertension by inhibiting the cardiac NLRP3 inflammation body/IL-1β axis. EMD638683 also promotes apoptosis of colon cancer cells and sensitizes radiotherapy, making it suitable for research concerning hypertension, hypertensive heart damage, and colon cancer.
- Strongly inhibits SGK1 with high selectivity
- Exhibits antihypertensive activity
- Prevents heart inflammation and fibrosis
- Promotes apoptosis in colon cancer cells
- Sensitizes radiotherapy for colon cancer
Medchemexpress LLC Gnf6702 | 1799329-72-8 | 98.3% | 50 MG
Gnf6702 is a selective inhibitor of the kinetoplastid proteasome that clears parasites in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis. Supplied as a 50 mg research-use powder, it has a molecular formula of C22H16FN7O2 and a molecular weight of 429.41 g/mol.
- Selective inhibitor of the kinetoplastid proteasome.
- Demonstrated efficacy in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis.
- Purity reported as 98.33%.
- Soluble in DMSO at 10 mg/mL; in vivo solubility ≥ 1 mg/mL in recommended vehicle.
- Storage: powder stable at -20°C (up to 3 years) and 4°C (up to 2 years); in solution store at -80°C for extended stability.
Medchemexpress LLC Setmelanotide | 920014-72-8 | 99.9% | 10 MG
Setmelanotide is a research-grade peptide agonist selective for the melanocortin 4 receptor (MC4R). It exhibits sub-nanomolar potency (EC50 ≈ 0.27 nM human, 0.28 nM rat), has a molecular weight of 1117.31, and is supplied as a high-purity white to off-white solid. The peptide is highly soluble in water and requires cold, sealed storage for long-term stability.
- Selective melanocortin 4 receptor (MC4R) agonist with sub-nanomolar potency.
- High chemical purity (99.93%).
- White to off-white solid physical form.
- Water solubility approximately 62.5 mg/mL (requires ultrasonic).
- Stable as powder at -80°C for up to 2 years and at -20°C for 1 year.
- Contains a defined peptide sequence with a disulfide bridge.
- Suitable for pharmacology and receptor biology research applications.
Medchemexpress LLC EMD638683 | 1181770-72-8 | C18H18F2N2O4 | 100 MG
EMD638683 | 1181770-72-8 | C18H18F2N2O4 | 100 MG
Medchemexpress LLC Emd638683 | 1181770-72-8 | C18H18F2N2O4 | 1 MG
Emd638683 | 1181770-72-8 | C18H18F2N2O4 | 1 MG
Medchemexpress LLC Zotiraciclib | 1204918-72-8 | C23H24N4O | 5 MG
Zotiraciclib is an orally active inhibitor targeting JAK2, FLT3, and CDK2, with IC50 values of 13 nM, 73 nM, and 56 nM, respectively. It inhibits cancer cell proliferation, tumor growth, and the activity of CYP2D6. This compound is used in research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia, and multiple myeloma.
- Potent inhibitor of JAK2, FLT3, and CDK2.
- Inhibits cancer cell proliferation and tumor growth.
- Demonstrates high plasma protein binding and Caco-2 permeability.
- Exhibits metabolic stability in human and canine liver microsomes.
- Used in research for various cancer types including colon cancer and lymphoma.
Medchemexpress LLC EMD638683 | 1181770-72-8 | C18H18F2N2O4 | 1 ML
EMD638683 is an orally active SGK1 inhibitor with an IC50 of 3 μM. It demonstrates strong inhibition against SGK1, moderate inhibition against SGK2 and SGK3, and excellent selectivity for other AGC kinase family members. This compound exhibits antihypertensive activity by inhibiting SGK1, and prevents heart inflammation and fibrosis caused by hypertension by inhibiting the cardiac NLRP3 inflammation body/IL-1β axis, independent of its blood pressure-lowering effect.
- Orally active SGK1 inhibitor
- Strongly inhibits SGK1, moderately inhibits SGK2 and SGK3
- Shows excellent selectivity for other AGC kinase family members
- Exhibits antihypertensive activity
- Prevents heart inflammation and fibrosis caused by hypertension
- Promotes apoptosis in colon cancer cells
- Sensitizes colon cancer cells to radiotherapy
- Suitable for research related to hypertension, hypertensive heart damage, and colon cancer
Medchemexpress LLC EMD638683 | 1181770-72-8 | C18H18F2N2O4 | 25 MG
EMD638683 (HY-15193) is an orally active SGK1 inhibitor with an IC50 of 3 μM. It strongly inhibits SGK1, moderately inhibits SGK2 and SGK3, and shows excellent selectivity for other AGC kinase family members. EMD638683 exhibits antihypertensive activity by inhibiting SGK1. It can also prevent heart inflammation and fibrosis caused by hypertension by inhibiting the cardiac NLRP3 inflammation body/IL-1β axis, independently of its blood pressure-lowering effect. This product promotes apoptosis of colon cancer cells and sensitizes radiotherapy.
- Orally active SGK1 inhibitor
- Strongly inhibits SGK1; moderately inhibits SGK2 and SGK3
- High selectivity for other AGC kinase family members
- Exhibits antihypertensive activity
- Prevents heart inflammation and fibrosis caused by hypertension
- Promotes apoptosis of colon cancer cells
- Enhances sensitivity to radiotherapy