Benzoxazines
AdipoGen PF-0477736
Chemical. CAS 952021-60-2. Formula C22H25N7O2. MW 419.5. PF-0477736 is a potent, selective ATP-competitive inhibitor of Chk1 Ki = 0.49nM with 100-fold selectivity over Chk2 Ki = 47nM. When used in combination with various chemotherapeutics e.g. gemcitabine and carboplatin, PF-0477736 abrogates DNA damage-induced cell cycle arrest, sensitizes cells to DNA damage, potentiating the antiproliferative effects of these compounds in vitro and in vivo in tumor cell lines and xenografts. PF-0477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3 and Ret Ki = 10, 14, 23, 23, 25 and 39 nM, respectively. Checkpoint kinase 1 Chk1 belongs to the Ca2/calmodulin-dependent protein kinase class of enzymes CAMK. CAMKs are activated by increases in the concentration of intracellular calcium ions Ca2 and calmodulin.
AdipoGen DMAT
Chemical. CAS 749234-11-5. Formula C9H7Br4N3. MW 476.8. Synthetic. Potent high affinity ATP-competitive inhibitor of casein kinase II CK2 IC50=0.13µM. Inhibits CK2 in rat liver with >1000-fold greater selectivity for CK2 than for CK1 IC50=140nM and >200 µM, respectively. DYRK1A and DYRK2 inhibitor IC50= ~0.4µM for both. Shown to inhibit additional kinases, such as PIM1, PIM3, HIPK2, HIPK3, PKD1 and CDK2 in the submicromolar range. Anticancer agent. Apoptosis inducer in different cancer cell lines. Induces reactive oxygen species ROS and DNA double strand breaks in tumor cells. Induces apoptosis in cells expressing an inhibitor-resistant CK2, by inhibiting quinone reductase 2 NQO2, binding with similar affinities to the oxidized and reduced forms of NQO2. Useful for in vivo studies due to cell permeability and high efficacy in cultured cells and implications in research and treatment of neoplasia and infective diseases, in which CK2 plays a role.
AdipoGen Ponatinib
Chemical. CAS 943319-70-8. Formula C29H27F3N6O. MW 532.6. Soluble in DMSO 30mg/ml, DMF 30mg/ml or ethanol 5mg/ml. Ponatinib is a potent multi-target kinase inhibitor with antiangiogenic and antineoplastic activities. It targets protein tyrosine kinases PTK, which catalyze the transfer of ATP-γ-phosphate to the tyrosine residues of the substrate proteins. Tyrosine kinase inhibitors TKIs compete with ATP for the ATP binding site of PTK and reduce tyrosine kinase phosphorylation, thereby inhibiting cancer cell proliferation. Ponatinib is an orally bioavailable Bcr-Abl tyrosine kinase inhibitor of native BCR-ABL IC50 = 0.37nM, the tyrosine kinase inhibitor-resistant mutant Bcr-AblT315I IC50 = 2nM, as well as Bcr-AblQ252H, Bcr-AblY253F, Bcr-AblM351T and Bcr-AblH396P mutants IC50s = 0.44, 0.3, 0.3, and 0.34nM, respectively in biochemical assays.
AdipoGen Taspine
Chemical. CAS 602-07-3. Formula C20H19NO6. MW 369.4. Taspine is an alkaloid with multifunctional pharmacological properties, including apoptosis-inducing, anti-angiogenic, anticancer, cytotoxic, anti-inflammatory and wound-healing activities, thereby modulating multiple targets. Taspine is a potent acetylcholinesterase AChE inhibitor and wound healing promoter cicatrizant, by regulating the expression of keratinocyte growth factor KGF FGF-7 in early phases. Taspine has anticancer properties targeting DNA topoisomerase IB and was shown to be a dual topoisomerase inhibitor. Taspine is an apoptosis-inducing compound. It induces conformational activation of the pro-apoptotic proteins Bak and Bax, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. It induced tumor apoptosis in vitro and in vivo. Taspine can inhibit tumor angiogenesis acting as a multi-target VEGFR-2 inhibitor.
AdipoGen Enniatin B
Chemical. CAS 917-13-5. Formula C33H57N3O9. MW 639.8. Isolated from fungus Fusarium sp. Cyclohexadepsipeptide mycotoxin. One of four major analogs in the enniatin complex. Commonly found food contaminant in cereals and their products. Ionophore antibiotic less ionophoric than Enniatin A. Incorporation into the cell membrane forms dimeric structures that transport monovalent ions across the membrane especially the mitochondrial membranes affecting oxidative phosphorylation uncoupling. Anticancer compound. Triggers apoptosis in several cancer cell lines. Moderate inhibitor of ACAT acylcoenzyme Acholesterolacyl transferase. Inhibitor of the pleiotropic drug resistance protein 5 Pdr5p in yeast. Shown to have a variety of other biological activities such as antifungal, anthelmintic, insecticidal, immunomodulatory and phytotoxic activity.
AdipoGen Glucosylglycerol
Natural chemical product. CAS 22160-26-5. Formula C9H18O8. MW 254.2. Enzymatically processed from natural succrose and glycerine. Glucosylglycerol belongs to the class of compatible solutes osmolytes. It is a non-toxic, non-irritating protective osmolyte responsible for the osmotic adaptation of blue-green algae, rhizobacteria and Pseudomonas and also found in the drought-resistant resurrection plant Myrothamnus flabellifolia. Glucosylglycerol protects its host against osmotic stress, heat, desiccation and UV. Glucosylglycerol is an animal free and protein-free low molecular weight stabilizer which is an excellent cryoprotector for proteins in vitro, especially antibodies. In vitro models and skin models demonstrate strong activity of glucosylglycerol on aged and stressed skin cells with rejuvenating, recovering and radical scavenging properties.
AdipoGen Cyclopenin
Chemical. CAS 19553-26-5 and 20007-87-8. Formula C17H14N2O3. MW 294.3. Isolated from Penicillium sp. Antimicrobial. Phytotoxic. Specific acetylcholinesterase AChE inhibitor.
AdipoGen Umbellulone
Chemical. CAS 546-78-1. Formula C10H14O. MW 150.2. Isolated from Umbellularia californica Nutt. Offensive principle of the so-called "headache tree". Causes a painful cold sensation. Selective TRPA1 activator. Weak TRPM8 activator. Releases CGRP calcitonin gene-related peptide after TRPA1 activation which leads to activation of trigeminovascular pathways and CGRP-mediated neurogenic vasodilatation relevant to produce headache/migraine.
TARGETMOL CHEMICALS INC CABOTEGRAVIR 50MG
Also available in 10 mg 25 mg 100 mg 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. Cabotegravir (S/GSK1265744) (GSK744 GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50 3.0 nM). purity: 99%
TARGETMOL CHEMICALS INC THIAMET G 25MG
Also available in 2 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. Thiamet G is a potent selective O-GlcNAcase inhibitor with Kiof 21 nM while exhibiting 37 000-fold selectivity over human lysosomal –hexosaminidase. purity: 99%
TARGETMOL CHEMICALS INC BLU0588 5MG
Also available in 1 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. BLU0588 is a selective PRKACA inhibitor. BLU0588 inhibits PRKACA catalytic activity with a half-maximal inhibitory concentration (IC50) of 1 nM.
TARGETMOL CHEMICALS INC OXYBERBERINE 20MG
Also available in 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. Oxyberberine (8-Oxoberberine) is isolated from the methanol extract of A. mexicana. It has been used to study the SW480 human colon cancer cell line. purity: 98%
TARGETMOL CHEMICALS INC CATHEPSIN X-IN-1 5MG
Also available in 1 mg 10 mg 25 mg 50 mg 100 mg 500 mg and bulk. Please contact Fisher for quotes. Cathepsin X-IN-1 (compound 25) reduces the migration of PC-3 cell with low cytotoxic that is a potent inhibitor of Cathepsin X (IC 50 = 7.13 uM) [1]. purity: 99%
TARGETMOL CHEMICALS INC IBEZAPOLSTAT HYDROCHLORI 5MG
Also available in 1 mg 2 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. Ibezapolstat hydrochloride is an antibacterial agent. purity: 99%
TARGETMOL CHEMICALS INC MM3122 5MG
Also available in 1 mg 2 mg 10 mg 25 mg 50 mg 100 mg and bulk. Please contact Fisher for quotes. MM3122 (MM-3122) is a selective type II transmembrane serine protease (TMPRSS2) inhibitor IC50 = 0.34 nM. MM3122 effectively blocks TMPRSS2 thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells. purity: 100%