Activators & Inhibitors

Activity: BCR-ABL inhibitor . Function/Pharmacology: A novel, selective BCR-ABL inhibitor. More potent than imatinib against wild-type BCR-ABL (IC50 < 30 nM)1. Induces apoptosis2. Chemical Name: 4-Methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide

Activity: PI 3-K and mTOR inhibitor . Function/Pharmacology: A dual PI3K and mTOR kinase inhibitor1. It inhibits VEGF-induced proliferation and angiogenesis2. Reverses lapatinib resistance3. It induces G1 arrest and reduces cyclin D1 expression in melanoma cells with negligible apoptosis4. Inhibits the growth of cancer cells with activating PI3K mutations5. Active in vivo. Chemical Name: 2-Methyl-2-{4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile

Activity: PARP1 inhibitor . Function/Pharmacology: A highly potent and selective PARP-inhibitor with IC₅₀ values of 5 nM and 1 nM for PARP-1 and PARP-2, respectively.1 In a genetically engineered mouse model for BRCA1-associated breast cancer olaparib inhibited tumor growth and improved survival with no signs of toxicity.2 Synergizes with many other anticancer agents.3 Shows efficacy in colorectal cancers.4 Prevents house dust mite allergen-induced asthma in a mouse model.5 Chemical Name: 4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazine-1(2H)-one

Activity: NFκB inhibitor . Function/Pharmacology: Active metabolite of cyclooxygenase inhibitor sulindac.1 Strongly inhibits Ras induced malignant transformation and Ras/Raf dependent transactivation.2 Induces apoptosis in cancer cells via PDE5 inhibition.3,4 Chemical Name: (Z)-5-Fluoro-2-methyl-1-[p-(methylthio)benzylidene]indene-3-acetic acid

Activity: HDAC inhibitor . Function/Pharmacology: A potent inhibitor of class I and II HDACs1. Cotreatment with panobinostat and an HSP90 inhibitor caused synergistic apoptosis in human CML-BC and AML cells2. A potent antimyeloma agent that overcomes drug resistance3. Chemical Name: (E)-N-Hydroxy-3-(4-((2-(2-methyl-1H-indol-3-yl)ethylamino)methyl)phenyl)acrylamide

Activity: MEK inhibitor . Function/Pharmacology: Inhibitor of mitogen-activated protein kinase kinase (MKK / MEK). Acts via binding to the inactivated form of MEK, preventing its phosphorylation by cRAF or MEK kinase (IC50=2-7M).1,2 Accelerates differentiation of RAW264.7 cells into osteoclast-like cells.3 Mimics BMP4 in supporting self renewal of embryonic stem cells4. Chemical Name: 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one

Activity: MEK inhibitor . Function/Pharmacology: A selective non-ATP competitive MEK inhibitor (IC50 = 0.33 nM).1 Inhibits growth and/or proliferation of a variety of cancer cells.2 Enhances self-renewal of embryonic stem cells.3 In combination with vitamin C, synergistically induces hypomethylation of mouse embryonic stem cells.4 In combination with CHIR-99021 and A83-01 induces generation of ground state iPS cells from human and rat somatic cells.5 Chemical Name: N-[(2R(-))-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide

Activity: Antifolate; antitumor agent . Function/Pharmacology: Pemetrexed is a multi-targeted antifolate with antitumor activity. It potently inhibits folate-dependent enzymes involved in both purine and pyrimidine synthesis including thymidylate synthase (Ki = 109 nM), dihydrofolate reductase (Ki = 7 nM), glycinamide ribonucleotide formyltransferase (Ki = 9.3 μM), and aminoimidazole carboxamide ribonucleotide formyltransferase (Ki = 3.6 μM).1 A clinically useful anticancer agent.2 Indirectly activates the metabolic kinase AMPK and consequently influences the mTORC1 pathway in human carcinomas.3 Activation of AMPK is associated with pemetrexed resistance.4 Induces G0/G1-phase cell cycle arrest in esophageal squamous cell carcinoma cells.5 Chemical Name: N-[4-[2-(2-Amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid, disodium salt

Activity: PKC activator . Function/Pharmacology: Activates protein kinase C (10-100 ng/ml)1. May display PKC-independent effects in various cell types2. Warning: Skin irritant. Avoid contact with this compound. Chemical Name: 12-O-Tetradecanoylphorbol-13-acetate