Bioactive Small Molecules
Selleck Chemical LLC Pexidartinib
Pexidartinib (PLX3397) is an oral potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R Kit (c-Kit) and FLT3 with IC50 of 20 nM 10 nM and 160 nM respectively Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity Phase 3
Selleck Chemical LLC Itacitinib
Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity
Selleck Chemical LLC Tucatinib
Tucatinib (Irbinitinib ONT-380 ARRY-380) is an oral potent selective reversible and ATP-competitive small-molecule inhibitor of ErbB-2 (also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2 respectively in cell-based assays showing 500-fold selective for HER2 vs EGFR It has potential antineoplastic activity
Selleck Chemical LLC Belotecan
Belotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor
Cayman Chemical ANTIBODY TFAP 25mg
An inhibitor of COX-1 (IC50 = 0.8 μM); selective for COX-1 over COX-2 (IC50 = 210 μM); reduces acetic acid-induced writhing in mice at 10 and 30 mg/kg; has analgesic activity in the formalin test in rats at 30 mg/kg; does not induce gastric damage in rats at doses up to 300 mg/kg
Cayman Chemical ANTIBODY Sparsentn 25mg
A dual antagonist of AT1 and ETA (Kis = 0.8 and 9.3 nM, respectively, for the human receptors); selective for these receptors over AT2 and ETB receptors (Kis = >10 µM for both); inhibits angiotensin II-induced pressor responses in conscious normotensive rats (ED50 = 3.6 µmol/kg, p.o); reduces mean arterial pressure in spontaneously hypertensive rats at 10, 30, or 100 µmol/kg per day, p.o.; reduces albuminuria and inhibits development of glomerulosclerosis in the gddY mouse model of IgA nephropathy when administered in the diet at 1,800 ppm
Medchemexpress LLC (1R,2R)-2-(pyridin-3-yl)cyclopropane-1-carboxylic acid | 1423769-08-7 | MFCD22419060 | 163.18 g/mol | C9H9NO2 | 5 G
(1R,2R)-2-(pyridin-3-yl)cyclopropane-1-carboxylic acid is a chiral cyclopropane carboxylic acid intermediate used in medicinal chemistry research. Supplied as a powder for research use.
- Chiral cyclopropane carboxylic acid intermediate.
- CAS number 1423769-08-7.
- Molecular formula C9H9NO2.
- Molecular weight 163.18 g/mol.
- Supplied as powder suitable for synthetic applications.
Cayman Chemical NG 25hydrochLRIde hydrAT 10mg
An inhibitor of MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively); also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively); prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells at 100 nM; inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells; decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells; reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12D mouse orthotopic model of colorectal cancer
Medchemexpress LLC Exendin-3 | 130357-25-4 | 98.3% | 4202.57 | 5 MG
Exendin-3 is a biologically active peptide isolated from the venoms of the Gila monster lizards, *Heloderma horridum*. It interacts with vasoactive intestinal peptide (VIP) receptors and a newly described putative exendin receptor on dispersed acini from guinea pig pancreas. At high concentrations (>100 nM), it causes a significant increase in cAMP and stimulates amylase release. At lower concentrations (0.1-3 nM), it interacts with the putative exendin receptor, leading to a smaller increase in cAMP.
- Interacts with VIP receptors and a putative exendin receptor
- Isolated from *Heloderma horridum* venoms
- Causes an increase in cAMP and stimulates amylase release
Medchemexpress LLC CGP77675 | 234772-64-6 | 99.5% | 443.54 g·mol⁻¹ | C26H29N5O2 | 50 MG
CGP77675 is a small-molecule inhibitor of Src family kinases used in biochemical and cell-based research. It inhibits phosphorylation of peptide substrates and autophosphorylation of c-Src, and shows low-nanomolar potency against Src family members.
- Potent Src family kinase inhibitor with low-nanomolar activity.
- Useful for studying signal transduction and cell biology pathways.
- Reported activity against Src, Lck, and c-Yes.
- Provided as a solid with high purity for research use.
- Commonly used in assays investigating bone resorption and epithelial tight junctions.
Cayman Chemical ANTIBODY ACY-738 10mg
An inhibitor of HDAC6 (IC50 = 1.7 nM); selective for HDAC6 over HDAC1-3 (IC50s = 94, 128, and 218 nM, respectively); increases acetylation of α-tubulin in mouse brain at 5 mg/kg; increases exploratory activity in a novel open-field test and reduces immobility time in a tail suspension test in wild-type, but not neural cell-selective HDAC6 knockout, mice at 50 mg/kg; attenuates decreases in caudal nerve SNAP amplitude and increases in hind paw mechanical hypersensitivity in a mouse model of vincristine-induced peripheral neuropathy at 100 mg/kg in the diet; decreases hepatorenal cystogenesis in a rat model of polycystic liver disease at 30 mg/kg
Cayman Chemical ANTIBODY OlaquIndox 500mg
An antibiotic and swine growth regulator; decreases E. coli-induced diarrhea and the number of intraepithelial lymphocytes in the ileum and increases body weight in geld piglets at 100 mg/kg; induces bleeding, intramuscular edema, vacuolar degeneration, and deformation of renal tubules in C. carpio; decreases mean body weight and increases the number of dead fetuses in pregnant rats at 110 mg/kg; increases the number of external deformities, including bent tail, cranioarchschisis, exencephaly, and anophthalmia in rat pups born to exposed pregnant mothers
Cayman Chemical ANTIBODY CHM-1 10mg
An inhibitor of tubulin polymerization (IC50 = 0.68 µM); inhibits chochicine tubulin binding at 5 µM; inhibits the growth of K562, NCI H226, HCT116, OVCAR-3, RXF 393L, SK-MEL-5, SF-268, and SF-295 cancer cells (mean GI50 = 130 nM); induces apoptosis in HA22T hepatocellular carcinoma cells; reduces tumor volume and increases survival in an HA22T mouse xenograft model at 10 mg/kg
Cayman Chemical ANTIBODY TP-0903 25mg
An inhibitor of Axl (IC50 = 27 nM ); exhibits greater than 50% inhibition of 11 kinases, including MER, TYRO3, JAK2, ALK, and Abl1, in a panel of 75 kinases at 200 nM, with IC50 values of 3 and 12.4 nM for Aurora A and B, respectively; decreases the phosphorylation of Akt and Axl in GAS6-stimulated, serum-starved PSN-1 pancreatic cancer cells (EC50s = 305 and 222 nM, respectively); decreases cell viability (IC50 = 6 nM) and induces cell cycle arrest at the G2/M phase in PSN-1 cells at 30 nM; reduces the viability of CRC cell lines (IC50s = 4.5-123 nM); exhibits 69 and 44% tumor growth inhibition in an HCT116 mouse xenograft model and a K-Ras-mutant CRC PDX mouse model, respectively, at 40 mg/kg