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背景介绍 CREBBP (CBP) and EP300 are general transcriptional co-activators, which are involved in many biological processes like maintenance of genomic stability by affecting DNA replication and DNA repair as well as cell growth, transformation and development. They also play and essential role in neuronal plasticity/ memory formation hematopoiesis and energy homeostasis as demonstrated in a variety of mouse models. They possess both acetyl-transferase enzymatic and bromodomain containing regions. Through acetylation of non-histone proteins CREBBP can have a positive or negative effect on transcriptional regulation by affecting protein- protein interactions, protein-DNA interactions, nuclear retention or protein half-life. 产品介绍 Potent CREBBP/EP300 bromodomain inhibitor
询价背景介绍 Rolipram is a racemic drug that increases brain cAMP availability by inhibiting phosphodiesterase. The S-(+)-Rolipram enantiomer is 2-10x less potent than the R-(-)-Rolipram compound. PDE4B is involved in dopamine-associated and stress-related behaviours, and is believed to be the PDE4 subtype involved in the antipsychotic effects of PDE4 inhibitors such as rolipram. 产品介绍 S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 µM. It has anti-inflammatory and anti-depressant activity in the central nervous system.
询价背景介绍 Rolipram is a racemic drug that increases brain cAMP availability by inhibiting phosphodiesterase. The S-(+)-Rolipram enantiomer is 2-10x less potent than the R-(-)-Rolipram compound. PDE4B is involved in dopamine-associated and stress-related behaviours, and is believed to be the PDE4 subtype involved in the antipsychotic effects of PDE4 inhibitors such as rolipram. 产品介绍 S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 µM. It has anti-inflammatory and anti-depressant activity in the central nervous system.
询价背景介绍 Rolipram is a racemic drug that increases brain cAMP availability by inhibiting phosphodiesterase. The S-(+)-Rolipram enantiomer is 2-10x less potent than the R-(-)-Rolipram compound. PDE4B is involved in dopamine-associated and stress-related behaviours, and is believed to be the PDE4 subtype involved in the antipsychotic effects of PDE4 inhibitors such as rolipram. 产品介绍 S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 µM. It has anti-inflammatory and anti-depressant activity in the central nervous system.
询价背景介绍 Rucaparib, also named as AG-014699 or PF-01367338, is a poly (ADP ribose) polymerase (PARP) inhibitor. PARP is a DNA damage-activated nuclear enzyme that has a key signaling role in the base excision repair pathway. So, rucaparib has been also found to be most effective in cells deficient in DNA repair, where the cells deficient are caused by exposure to genotoxic agents, such as irradiation produces DNA damage and its toxicity is augmented when the DNA repair is impaired. Increased radiosensitivity in presence of rucaparib was associated with persistent DNA breaks as determined by gamma-H2AX and p53BP1 foci. Rucaparib radiosensitizes prostate cancer cells, most effectively those that are PTEN-deficient and are expressing ETS gene fusion proteins, which inhibits NHEJ DNA repair. 产品介绍 Rucaparib, also known as AG-014699 or PF-01367338, is an inhibitor of PARP1 with Ki of 1.4 nM.
询价背景介绍 Rucaparib, also named as AG-014699 or PF-01367338, is a poly (ADP ribose) polymerase (PARP) inhibitor. PARP is a DNA damage-activated nuclear enzyme that has a key signaling role in the base excision repair pathway. So, rucaparib has been also found to be most effective in cells deficient in DNA repair, where the cells deficient are caused by exposure to genotoxic agents, such as irradiation produces DNA damage and its toxicity is augmented when the DNA repair is impaired. Increased radiosensitivity in presence of rucaparib was associated with persistent DNA breaks as determined by gamma-H2AX and p53BP1 foci. Rucaparib radiosensitizes prostate cancer cells, most effectively those that are PTEN-deficient and are expressing ETS gene fusion proteins, which inhibits NHEJ DNA repair. 产品介绍 Rucaparib, also known as AG-014699 or PF-01367338, is an inhibitor of PARP1 with Ki of 1.4 nM.
询价背景介绍 Rucaparib, also named as AG-014699 or PF-01367338, is a poly (ADP ribose) polymerase (PARP) inhibitor. PARP is a DNA damage-activated nuclear enzyme that has a key signaling role in the base excision repair pathway. So, rucaparib has been also found to be most effective in cells deficient in DNA repair, where the cells deficient are caused by exposure to genotoxic agents, such as irradiation produces DNA damage and its toxicity is augmented when the DNA repair is impaired. Increased radiosensitivity in presence of rucaparib was associated with persistent DNA breaks as determined by gamma-H2AX and p53BP1 foci. Rucaparib radiosensitizes prostate cancer cells, most effectively those that are PTEN-deficient and are expressing ETS gene fusion proteins, which inhibits NHEJ DNA repair. 产品介绍 Rucaparib, also known as AG-014699 or PF-01367338, is an inhibitor of PARP1 with Ki of 1.4 nM.
询价背景介绍 Romidepsin is a bicyclic depsipeptide antibiotic isolated from the bacterium Chromobacterium violaceum with antineoplastic activity. After intracellular activation, romidepsin binds to and inhibits histone deacetylase (HDAC), resulting in alterations in gene expression and the induction of cell differentiation, cell cycle arrest, and apoptosis. This agent also inhibits hypoxia-induced angiogenesis and depletes several heat shock protein 90 (Hsp90)-dependent oncoproteins. In vitro, romidepsin causes the accumulation of acetylated histones, and induces cell cycle arrest and apoptosis of some cancer cell lines with IC50 values in the nanomolar range. 产品介绍 Romidepsin, also known as FK228 or depsipeptide, is a potent and selective inhibitor of HDAC1 and HDAC2 , which are associated with the regulation of re-expression of silenced tumor suppressor genes. It was the first HDAC inhibitor to manifest anti-tumor activity and originally isolated from a rod-shaped Gram-negative bacterium, Chromobacterium violaceum, found in a Japanese soil sample. Romidepsin exhibits a stronger inhibition towards HDAC1 and HDAC2 enzymes (class I), removing acetyl groups from the lysine residues of N-terminal histone tails and maintaining a more open and transcriptionally active chromatin state, than HDAC4 and HDAC6 enzymes (class II). Besides HDAC inhibition, romidepsin is also able to induce cell cycle arrest, cellular differentiation, apoptosis and alteration of gene expression in adult malignancies.
询价背景介绍 Romidepsin is a bicyclic depsipeptide antibiotic isolated from the bacterium Chromobacterium violaceum with antineoplastic activity. After intracellular activation, romidepsin binds to and inhibits histone deacetylase (HDAC), resulting in alterations in gene expression and the induction of cell differentiation, cell cycle arrest, and apoptosis. This agent also inhibits hypoxia-induced angiogenesis and depletes several heat shock protein 90 (Hsp90)-dependent oncoproteins. In vitro, romidepsin causes the accumulation of acetylated histones, and induces cell cycle arrest and apoptosis of some cancer cell lines with IC50 values in the nanomolar range. 产品介绍 Romidepsin, also known as FK228 or depsipeptide, is a potent and selective inhibitor of HDAC1 and HDAC2 , which are associated with the regulation of re-expression of silenced tumor suppressor genes. It was the first HDAC inhibitor to manifest anti-tumor activity and originally isolated from a rod-shaped Gram-negative bacterium, Chromobacterium violaceum, found in a Japanese soil sample. Romidepsin exhibits a stronger inhibition towards HDAC1 and HDAC2 enzymes (class I), removing acetyl groups from the lysine residues of N-terminal histone tails and maintaining a more open and transcriptionally active chromatin state, than HDAC4 and HDAC6 enzymes (class II). Besides HDAC inhibition, romidepsin is also able to induce cell cycle arrest, cellular differentiation, apoptosis and alteration of gene expression in adult malignancies.
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