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背景介绍 Selectivity for caspases-3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue. Sequence alignments of the active site residues of the caspases strongly suggest that the basis of this selectivity is due to binding in the S2 subsite comprised of residues Tyr204, Trp206, and Phe256 which are unique to caspases 3 and 7. In some systems inhibition of caspases-3 and -7 can prevent apoptosis and may therefore have important therapeutic implications. 产品介绍 A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 and caspase-7.
询价背景介绍 It has been reported that BIBR 1532 inhibited the reverse transcriptase of telomerase, hTERT, and shortened the length of the telomerase to suppress human cancer cell proliferation. In pre-B acute lymphoblastic leukemia cells, BIBR1532 suppressed c-Myc and hTERT expression in a concentration-dependent manner to inhibit telomerase activity, and high doses of BIBR1532 could induce apoptosis by elevating p73, Bax/Bcl-2 and caspase-3 activation. In NB4 leukemic cells, combined treatments with BIBR 1532 and arsenic trioxide suppressed cell proliferative capacity and inhibited telomerase activity probably via transcriptional suppression of c-Myc and hTERT. 产品介绍 BIBR 1532 is a novel, specific telomerase inhibitor with IC50 = 93 nM.
询价产品介绍 Betulinic acid is a natural pentacyclic triterpenoid that selectively induces apoptosis in tumor cells by directly activating the mitochondrial pathway of apoptosis through a p53- and CD95-independent mechanism. Betulinic acid also displays TGR5 agonist activity (EC50 =1.04 µM). Betulinic acid is used to study its potential cardiovascular role in the modulation of endothelium-dependent relaxation. Betulinic acid displays anti-HIV and antitumor activity.
询价产品介绍 Betulinic acid is a natural pentacyclic triterpenoid that selectively induces apoptosis in tumor cells by directly activating the mitochondrial pathway of apoptosis through a p53- and CD95-independent mechanism. Betulinic acid also displays TGR5 agonist activity (EC50 =1.04 µM). Betulinic acid is used to study its potential cardiovascular role in the modulation of endothelium-dependent relaxation. Betulinic acid displays anti-HIV and antitumor activity.
询价产品介绍 Betulinic acid is a natural pentacyclic triterpenoid that selectively induces apoptosis in tumor cells by directly activating the mitochondrial pathway of apoptosis through a p53- and CD95-independent mechanism. Betulinic acid also displays TGR5 agonist activity (EC50 =1.04 µM). Betulinic acid is used to study its potential cardiovascular role in the modulation of endothelium-dependent relaxation. Betulinic acid displays anti-HIV and antitumor activity.
询价背景介绍 Bendamustine inhibits mitotic checkpoints and induces mitotic catastrophe by inhibiting several mitosis-related genes such as Polo-like kinase 1, Aurora kinase A, and Cyclin B1. In myeloma cell lines, bendamustine induced apoptosis by cleavage of caspase 3, and resulted in G2 cell cycle arrest. In chronic lymphocytic and mantle cell lymphoma cell lines, bendamustine HCl has been shown to activate both the mitochondrial cell death pathway and caspase-dependent apoptosis. 产品介绍 Bendamustine HCl is an alkylating agent associated with DNA damage (IC50 = 50 µM). It is a cytostatic agent that displays activity in non-Hodgkin's lymphomas.
询价背景介绍 Bendamustine inhibits mitotic checkpoints and induces mitotic catastrophe by inhibiting several mitosis-related genes such as Polo-like kinase 1, Aurora kinase A, and Cyclin B1. In myeloma cell lines, bendamustine induced apoptosis by cleavage of caspase 3, and resulted in G2 cell cycle arrest. In chronic lymphocytic and mantle cell lymphoma cell lines, bendamustine HCl has been shown to activate both the mitochondrial cell death pathway and caspase-dependent apoptosis. 产品介绍 Bendamustine HCl is an alkylating agent associated with DNA damage (IC50 = 50 µM). It is a cytostatic agent that displays activity in non-Hodgkin's lymphomas.
询价产品介绍 AT13387, discovered by a high-throughput x-ray craystallography fragment-based platform, is a non-geldanamycin inhibitor of heat shock proterin 90 (HPS90), a molecule chaperone regulating signal transduction pathways for cell growth and survival. It has high affinity for binding HSP90 (Kd = 0.5nM) and exhibited an in vitro cytotoxicity showing a median EC50 value of 41 nM. The antitumor activity of AT13387 against solid tumor and leukemia models is similar to alvespimycin.
询价产品介绍 Apremilast, also known as CC-10004, is a novel and potent small-molecule inhibitor of phosphodiesterase 4 (PDE4), a key enzyme involved in cyclic adenosine monophosphate (cAMP) degradation and cytokine production of inflammatory cells.
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