Cayman
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Piromidic acid is a quinolone antibiotic that is active against Gram-positive and Gram-negative bacteria including S. aureus and E. coli (MICs = 10 and 1 µg/ml, respectively).{36759,36760} It inhibits growth of nalidixic acid-sensitive strains of E. coli in an in vitro model of bacterial cystitis when used at concentrations of 10 and 50 mg/L.{36760} Piromidic acid also has antimalarial properties and is active against chloroquine-sensitive and -resistant strains of P. falciparum in vitro (IC50s = 41.4 and 14.4 µg/ml, respectively) as well as against hepatic stages of P. yoelii yoelii (IC50 = 21.6 µg/ml).{36761}
Brand:CaymanSKU:-Available on backorder
Piromidic acid is a quinolone antibiotic that is active against Gram-positive and Gram-negative bacteria including S. aureus and E. coli (MICs = 10 and 1 µg/ml, respectively).{36759,36760} It inhibits growth of nalidixic acid-sensitive strains of E. coli in an in vitro model of bacterial cystitis when used at concentrations of 10 and 50 mg/L.{36760} Piromidic acid also has antimalarial properties and is active against chloroquine-sensitive and -resistant strains of P. falciparum in vitro (IC50s = 41.4 and 14.4 µg/ml, respectively) as well as against hepatic stages of P. yoelii yoelii (IC50 = 21.6 µg/ml).{36761}
Brand:CaymanSKU:-Available on backorder
Pironetin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including anti-proliferative, immunosuppressive, and plant growth regulatory properties.{46452,46453,46454,46455} It binds to tubulin with a Kd value of 0.33 μM and increases the critical concentration (CrC) for tubulin assembly in glycerol-assembling buffer (GAB) at a concentration of 25 μM.{46453,46454} It also induces G2/M phase cell cycle arrest in 3Y1 rat fibroblasts and apoptosis in HL-60 human leukemia cells when used at concentrations of 50 ng/ml and 33 nM, respectively.{46453,46456} It inhibits the growth of HT-29 human colorectal and MCF-7 human breast cancer cells (IC50s = 6.4 and 6 nM, respectively) but also of non-cancerous human HEK293 cells (IC50 = 17 nM). It also inhibits the growth of A2780 human ovarian carcinoma cells, as well as of the drug-resistant, P-glycoprotein-expressing A2780AD subline (IC50s = 8 and 25 nM, respectively). Pironetin (5 mg/kg) decreases the generation of cytotoxic T lymphocytes in mice in response to immunization by EL4 allogeneic mouse T lymphocytes.{46455} It also inhibits rice plant growth by 23% when applied nine days prior to heading.{46452}
Brand:CaymanSKU:28853 - 1 mgAvailable on backorder
Piroxicam is a non-steroidal anti-inflammatory drug (NSAID) that non-selectively and reversibly inhibits both isoforms of cyclooxygenase (COX; IC50 = 1.57 and 1.69 μM for COX-1 and COX-2, respectively).{17755} It has an extended half-life of about 40 hours, which allows once daily administration leading to sustained plasma and tissue levels. In addition to its anti-inflammatory effects, piroxicam is known to be an effective analgesic that has been used extensively in the treatment of arthritis. It has also been used to inhibit COX activity for treatment of certain cancers in animals. As with other NSAIDs, the extended use of piroxicam results in damage to the gastrointestinal lining.
Brand:CaymanSKU:- Piroxicam is a non-steroidal anti-inflammatory drug (NSAID) that non-selectively and reversibly inhibits both isoforms of cyclooxygenase (COX; IC50 = 1.57 and 1.69 μM for COX-1 and COX-2, respectively).{17755} It has an extended half-life of about 40 hours, which allows once daily administration leading to sustained plasma and tissue levels. In addition to its anti-inflammatory effects, piroxicam is known to be an effective analgesic that has been used extensively in the treatment of arthritis. It has also been used to inhibit COX activity for treatment of certain cancers in animals. As with other NSAIDs, the extended use of piroxicam results in damage to the gastrointestinal lining.
Brand:CaymanSKU:- Piroxicam is a non-steroidal anti-inflammatory drug (NSAID) that non-selectively and reversibly inhibits both isoforms of cyclooxygenase (COX; IC50 = 1.57 and 1.69 μM for COX-1 and COX-2, respectively).{17755} It has an extended half-life of about 40 hours, which allows once daily administration leading to sustained plasma and tissue levels. In addition to its anti-inflammatory effects, piroxicam is known to be an effective analgesic that has been used extensively in the treatment of arthritis. It has also been used to inhibit COX activity for treatment of certain cancers in animals. As with other NSAIDs, the extended use of piroxicam results in damage to the gastrointestinal lining.
Brand:CaymanSKU:- Piroxicam is a non-steroidal anti-inflammatory drug (NSAID) that non-selectively and reversibly inhibits both isoforms of cyclooxygenase (COX; IC50 = 1.57 and 1.69 μM for COX-1 and COX-2, respectively).{17755} It has an extended half-life of about 40 hours, which allows once daily administration leading to sustained plasma and tissue levels. In addition to its anti-inflammatory effects, piroxicam is known to be an effective analgesic that has been used extensively in the treatment of arthritis. It has also been used to inhibit COX activity for treatment of certain cancers in animals. As with other NSAIDs, the extended use of piroxicam results in damage to the gastrointestinal lining.
Brand:CaymanSKU:-
PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer.{12235} PIT-1 is a selective nonphosphoinositide inhibitor that specifically disrupts PIP3/Akt PH domain binding with an IC50 value of 31 μM.{18957} PIT-1 suppresses PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM).{18957}
Brand:CaymanSKU:10728 - 10 mgAvailable on backorder
PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer.{12235} PIT-1 is a selective nonphosphoinositide inhibitor that specifically disrupts PIP3/Akt PH domain binding with an IC50 value of 31 μM.{18957} PIT-1 suppresses PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM).{18957}
Brand:CaymanSKU:10728 - 100 mgAvailable on backorder
PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer.{12235} PIT-1 is a selective nonphosphoinositide inhibitor that specifically disrupts PIP3/Akt PH domain binding with an IC50 value of 31 μM.{18957} PIT-1 suppresses PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM).{18957}
Brand:CaymanSKU:10728 - 5 mgAvailable on backorder
PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer.{12235} PIT-1 is a selective nonphosphoinositide inhibitor that specifically disrupts PIP3/Akt PH domain binding with an IC50 value of 31 μM.{18957} PIT-1 suppresses PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM).{18957}
Brand:CaymanSKU:10728 - 50 mgAvailable on backorder
The statins are a family of compounds that inhibit 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase, a pivotal enzyme in cholesterol biosynthesis.{20936} Pitavastatin is a potent inhibitor of HMG-CoA reductase (Ki = 1.7 nM).{25250} It lowers both total cholesterol and low density lipoprotein cholesterol in animals and humans.{25248} Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.{25248} Moreover, pitavastatin causes atherosclerosis regression in humans with subclinical carotid atherosclerosis and improves cardiac function and survival in a rat model of hypertensive heart failure.{25249,25247}
Brand:CaymanSKU:- The statins are a family of compounds that inhibit 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase, a pivotal enzyme in cholesterol biosynthesis.{20936} Pitavastatin is a potent inhibitor of HMG-CoA reductase (Ki = 1.7 nM).{25250} It lowers both total cholesterol and low density lipoprotein cholesterol in animals and humans.{25248} Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.{25248} Moreover, pitavastatin causes atherosclerosis regression in humans with subclinical carotid atherosclerosis and improves cardiac function and survival in a rat model of hypertensive heart failure.{25249,25247}
Brand:CaymanSKU:- The statins are a family of compounds that inhibit 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase, a pivotal enzyme in cholesterol biosynthesis.{20936} Pitavastatin is a potent inhibitor of HMG-CoA reductase (Ki = 1.7 nM).{25250} It lowers both total cholesterol and low density lipoprotein cholesterol in animals and humans.{25248} Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.{25248} Moreover, pitavastatin causes atherosclerosis regression in humans with subclinical carotid atherosclerosis and improves cardiac function and survival in a rat model of hypertensive heart failure.{25249,25247}
Brand:CaymanSKU:- The statins are a family of compounds that inhibit 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase, a pivotal enzyme in cholesterol biosynthesis.{20936} Pitavastatin is a potent inhibitor of HMG-CoA reductase (Ki = 1.7 nM).{25250} It lowers both total cholesterol and low density lipoprotein cholesterol in animals and humans.{25248} Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.{25248} Moreover, pitavastatin causes atherosclerosis regression in humans with subclinical carotid atherosclerosis and improves cardiac function and survival in a rat model of hypertensive heart failure.{25249,25247}
Brand:CaymanSKU:-
Pitavastatin lactone is a major phase 2 metabolite of pitavastatin (Item No. 15414), an inhibitor of HMG-CoA reductase, that is found in plasma of rats and humans following oral administration.{37247},{25250} Pitavastatin lactone is formed when pitavastatin undergoes glucuronidation by the UDP-glucuronysyl transferases UGT1A1, UGT1A3, or UGT2B7 to form pitavastatin glucuronide, which then undergoes non-enzymatic conversion to pitavastatin lactone. It can be converted back to pitavastatin via hydrolysis.
Brand:CaymanSKU:21785 -Out of stock
Pitavastatin lactone is a major phase 2 metabolite of pitavastatin (Item No. 15414), an inhibitor of HMG-CoA reductase, that is found in plasma of rats and humans following oral administration.{37247},{25250} Pitavastatin lactone is formed when pitavastatin undergoes glucuronidation by the UDP-glucuronysyl transferases UGT1A1, UGT1A3, or UGT2B7 to form pitavastatin glucuronide, which then undergoes non-enzymatic conversion to pitavastatin lactone. It can be converted back to pitavastatin via hydrolysis.
Brand:CaymanSKU:21785 -Out of stock
Pitavastatin lactone is a major phase 2 metabolite of pitavastatin (Item No. 15414), an inhibitor of HMG-CoA reductase, that is found in plasma of rats and humans following oral administration.{37247},{25250} Pitavastatin lactone is formed when pitavastatin undergoes glucuronidation by the UDP-glucuronysyl transferases UGT1A1, UGT1A3, or UGT2B7 to form pitavastatin glucuronide, which then undergoes non-enzymatic conversion to pitavastatin lactone. It can be converted back to pitavastatin via hydrolysis.
Brand:CaymanSKU:21785 -Out of stock
Pitofenone is an antispasmodic agent and an inhibitor of acetylcholinesterase (AChE; Kis = 36 and 45 μM for bovine erythrocyte and electric eel enzyme, respectively).{45085} It inhibits acetylcholine-induced contractions of isolated guinea pig ileum when used at a concentration of 2.5 μM.{45086}
Brand:CaymanSKU:23865 - 10 mgAvailable on backorder
Pitofenone is an antispasmodic agent and an inhibitor of acetylcholinesterase (AChE; Kis = 36 and 45 μM for bovine erythrocyte and electric eel enzyme, respectively).{45085} It inhibits acetylcholine-induced contractions of isolated guinea pig ileum when used at a concentration of 2.5 μM.{45086}
Brand:CaymanSKU:23865 - 25 mgAvailable on backorder
Pitofenone is an antispasmodic agent and an inhibitor of acetylcholinesterase (AChE; Kis = 36 and 45 μM for bovine erythrocyte and electric eel enzyme, respectively).{45085} It inhibits acetylcholine-induced contractions of isolated guinea pig ileum when used at a concentration of 2.5 μM.{45086}
Brand:CaymanSKU:23865 - 5 mgAvailable on backorder
Pitofenone is an antispasmodic agent and an inhibitor of acetylcholinesterase (AChE; Kis = 36 and 45 μM for bovine erythrocyte and electric eel enzyme, respectively).{45085} It inhibits acetylcholine-induced contractions of isolated guinea pig ileum when used at a concentration of 2.5 μM.{45086}
Brand:CaymanSKU:23865 - 50 mgAvailable on backorder
Pitolisant is a nonimidazole histamine H3 receptor antagonist (Ki = 0.16 nM) and inverse agonist (EC50 = 1.5 nM).{47015} It increases the levels of tele-methylhistamine in mouse brain, indicating histaminergic neuron activity, with an ED50 value of 1.6 mg/kg. Pitolisant also increases dopamine and acetylcholine levels in the rat prefrontal cortex when administered at a dose of 10 mg/kg. It decreases the time spent in slow wave sleep and increases the time spent awake in cats. Pitolisant (2.5 and 5 mg/kg), when administered post-training, facilitates contextual fear memory consolidation and reverses dizocilpine-induced amnesia in mice.{47016} When administered following reactivation, it reverses dizocilpine-induced reconsolidation deficits.
Brand:CaymanSKU:-Available on backorder
Pitolisant is a nonimidazole histamine H3 receptor antagonist (Ki = 0.16 nM) and inverse agonist (EC50 = 1.5 nM).{47015} It increases the levels of tele-methylhistamine in mouse brain, indicating histaminergic neuron activity, with an ED50 value of 1.6 mg/kg. Pitolisant also increases dopamine and acetylcholine levels in the rat prefrontal cortex when administered at a dose of 10 mg/kg. It decreases the time spent in slow wave sleep and increases the time spent awake in cats. Pitolisant (2.5 and 5 mg/kg), when administered post-training, facilitates contextual fear memory consolidation and reverses dizocilpine-induced amnesia in mice.{47016} When administered following reactivation, it reverses dizocilpine-induced reconsolidation deficits.
Brand:CaymanSKU:-Available on backorder
Pitolisant is a nonimidazole histamine H3 receptor antagonist (Ki = 0.16 nM) and inverse agonist (EC50 = 1.5 nM).{47015} It increases the levels of tele-methylhistamine in mouse brain, indicating histaminergic neuron activity, with an ED50 value of 1.6 mg/kg. Pitolisant also increases dopamine and acetylcholine levels in the rat prefrontal cortex when administered at a dose of 10 mg/kg. It decreases the time spent in slow wave sleep and increases the time spent awake in cats. Pitolisant (2.5 and 5 mg/kg), when administered post-training, facilitates contextual fear memory consolidation and reverses dizocilpine-induced amnesia in mice.{47016} When administered following reactivation, it reverses dizocilpine-induced reconsolidation deficits.
Brand:CaymanSKU:-Available on backorder
Pitolisant is a nonimidazole histamine H3 receptor antagonist (Ki = 0.16 nM) and inverse agonist (EC50 = 1.5 nM).{47015} It increases the levels of tele-methylhistamine in mouse brain, indicating histaminergic neuron activity, with an ED50 value of 1.6 mg/kg. Pitolisant also increases dopamine and acetylcholine levels in the rat prefrontal cortex when administered at a dose of 10 mg/kg. It decreases the time spent in slow wave sleep and increases the time spent awake in cats. Pitolisant (2.5 and 5 mg/kg), when administered post-training, facilitates contextual fear memory consolidation and reverses dizocilpine-induced amnesia in mice.{47016} When administered following reactivation, it reverses dizocilpine-induced reconsolidation deficits.
Brand:CaymanSKU:-Available on backorder
Pitstop2 is an inhibitor of the interaction between the clathrin terminal domain and amphiphysin (IC50 = 12 μM).{20347} It inhibits clathrin-mediated transferrin uptake in HeLa and U2OS cells (IC50s = 12-15 and 9.7 μM, respectively). Pitstop2 inhibits HIV-1 entry and infectivity in HeLa reporter cell lines. It also inhibits clathrin-independent endocytosis of CD44, CD98, and CD147 in HeLa cells.{51182}
Brand:CaymanSKU:23885 - 1 mgAvailable on backorder
Pitstop2 is an inhibitor of the interaction between the clathrin terminal domain and amphiphysin (IC50 = 12 μM).{20347} It inhibits clathrin-mediated transferrin uptake in HeLa and U2OS cells (IC50s = 12-15 and 9.7 μM, respectively). Pitstop2 inhibits HIV-1 entry and infectivity in HeLa reporter cell lines. It also inhibits clathrin-independent endocytosis of CD44, CD98, and CD147 in HeLa cells.{51182}
Brand:CaymanSKU:23885 - 10 mgAvailable on backorder
Pitstop2 is an inhibitor of the interaction between the clathrin terminal domain and amphiphysin (IC50 = 12 μM).{20347} It inhibits clathrin-mediated transferrin uptake in HeLa and U2OS cells (IC50s = 12-15 and 9.7 μM, respectively). Pitstop2 inhibits HIV-1 entry and infectivity in HeLa reporter cell lines. It also inhibits clathrin-independent endocytosis of CD44, CD98, and CD147 in HeLa cells.{51182}
Brand:CaymanSKU:23885 - 5 mgAvailable on backorder
Pixantrone is an aza-anthracenedione analog that intercalates in DNA, directly alkylates DNA, and forms stable DNA adducts.{32717} It has demonstrated significant activity in preclinical models of solid tumors and hematologic malignancies.{32717,32715} Pixantrone has revealed little or no measurable cardiotoxicity in several animal models.{32717,32715} It also prevents acute experimental allergic encephalomyelitis development in animal studies, suggesting value in multiple sclerosis.{32716}
Brand:CaymanSKU:20055 -Available on backorder
Pixantrone is an aza-anthracenedione analog that intercalates in DNA, directly alkylates DNA, and forms stable DNA adducts.{32717} It has demonstrated significant activity in preclinical models of solid tumors and hematologic malignancies.{32717,32715} Pixantrone has revealed little or no measurable cardiotoxicity in several animal models.{32717,32715} It also prevents acute experimental allergic encephalomyelitis development in animal studies, suggesting value in multiple sclerosis.{32716}
Brand:CaymanSKU:20055 -Available on backorder
Pixantrone is an aza-anthracenedione analog that intercalates in DNA, directly alkylates DNA, and forms stable DNA adducts.{32717} It has demonstrated significant activity in preclinical models of solid tumors and hematologic malignancies.{32717,32715} Pixantrone has revealed little or no measurable cardiotoxicity in several animal models.{32717,32715} It also prevents acute experimental allergic encephalomyelitis development in animal studies, suggesting value in multiple sclerosis.{32716}
Brand:CaymanSKU:20055 -Available on backorder
Pixantrone is an aza-anthracenedione analog that intercalates in DNA, directly alkylates DNA, and forms stable DNA adducts.{32717} It has demonstrated significant activity in preclinical models of solid tumors and hematologic malignancies.{32717,32715} Pixantrone has revealed little or no measurable cardiotoxicity in several animal models.{32717,32715} It also prevents acute experimental allergic encephalomyelitis development in animal studies, suggesting value in multiple sclerosis.{32716}
Brand:CaymanSKU:20055 -Available on backorder
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species.{22577,22591} PJ-34 is an inhibitor of PARPs which can be used in cells or in animals.{22593,22588,22592} It binds and inhibits the PARP tankyrase1 (IC50 = 1 μM).{22590} PJ-34 also inhibits matrix metalloproteinase-2 when used at higher concentrations (IC50 = 56 μM).{20001}
Brand:CaymanSKU:- The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species.{22577,22591} PJ-34 is an inhibitor of PARPs which can be used in cells or in animals.{22593,22588,22592} It binds and inhibits the PARP tankyrase1 (IC50 = 1 μM).{22590} PJ-34 also inhibits matrix metalloproteinase-2 when used at higher concentrations (IC50 = 56 μM).{20001}
Brand:CaymanSKU:- The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species.{22577,22591} PJ-34 is an inhibitor of PARPs which can be used in cells or in animals.{22593,22588,22592} It binds and inhibits the PARP tankyrase1 (IC50 = 1 μM).{22590} PJ-34 also inhibits matrix metalloproteinase-2 when used at higher concentrations (IC50 = 56 μM).{20001}
Brand:CaymanSKU:- The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species.{22577,22591} PJ-34 is an inhibitor of PARPs which can be used in cells or in animals.{22593,22588,22592} It binds and inhibits the PARP tankyrase1 (IC50 = 1 μM).{22590} PJ-34 also inhibits matrix metalloproteinase-2 when used at higher concentrations (IC50 = 56 μM).{20001}
Brand:CaymanSKU:-
Benzodiazepines bind two types of receptors, the central γ-aminobutyric acid A receptor and the peripheral translocator protein (TSPO). PK 11195 binds the peripheral benzodiazepine receptor, TSPO, with selectivity and high affinity (Ki = 3.1 nM in cerebellum, 4.1 nM in spinal cord).{20753,20752} PK 11195, which lacks the 7-member heterocycle of diazepines, blocks binding of typical benzodiazepines to TSPO.{20753} In addition, the binding of labeled PK 11195 to tissues is used to detect the presence of TSPO by various methods.{20752,20751} PK 11195 has been used to study the ligand binding site of the B. cereus TSPO.{28284}
Brand:CaymanSKU:10525 - 10 mgAvailable on backorder
Benzodiazepines bind two types of receptors, the central γ-aminobutyric acid A receptor and the peripheral translocator protein (TSPO). PK 11195 binds the peripheral benzodiazepine receptor, TSPO, with selectivity and high affinity (Ki = 3.1 nM in cerebellum, 4.1 nM in spinal cord).{20753,20752} PK 11195, which lacks the 7-member heterocycle of diazepines, blocks binding of typical benzodiazepines to TSPO.{20753} In addition, the binding of labeled PK 11195 to tissues is used to detect the presence of TSPO by various methods.{20752,20751} PK 11195 has been used to study the ligand binding site of the B. cereus TSPO.{28284}
Brand:CaymanSKU:10525 - 50 mgAvailable on backorder
PK-THPP is a brain-penetrant inhibitor of the two-pore domain potassium channel K2P9.1/TASK-3 (IC50 = 0.035 µM).{53780} It is selective for K2P9.1/TASK-3 over K2P2.1/TREK1 and the voltage-gated potassium channel subtype Kv1.5 (IC50s = ~5 and >10 µM, respectively), as well as a panel of more than 100 receptors, ion channels, and enzymes at 10 µM but does inhibit K2P3.1/TASK-1 (IC50 = 0.3 µM). PK-THPP (100 mg/kg, s.c.) increases the time spent awake and decreases the duration of rapid eye movement (REM) and delta sleep in mice.
Brand:CaymanSKU:29473 - 1 mgAvailable on backorder
PK-THPP is a brain-penetrant inhibitor of the two-pore domain potassium channel K2P9.1/TASK-3 (IC50 = 0.035 µM).{53780} It is selective for K2P9.1/TASK-3 over K2P2.1/TREK1 and the voltage-gated potassium channel subtype Kv1.5 (IC50s = ~5 and >10 µM, respectively), as well as a panel of more than 100 receptors, ion channels, and enzymes at 10 µM but does inhibit K2P3.1/TASK-1 (IC50 = 0.3 µM). PK-THPP (100 mg/kg, s.c.) increases the time spent awake and decreases the duration of rapid eye movement (REM) and delta sleep in mice.
Brand:CaymanSKU:29473 - 10 mgAvailable on backorder
PK-THPP is a brain-penetrant inhibitor of the two-pore domain potassium channel K2P9.1/TASK-3 (IC50 = 0.035 µM).{53780} It is selective for K2P9.1/TASK-3 over K2P2.1/TREK1 and the voltage-gated potassium channel subtype Kv1.5 (IC50s = ~5 and >10 µM, respectively), as well as a panel of more than 100 receptors, ion channels, and enzymes at 10 µM but does inhibit K2P3.1/TASK-1 (IC50 = 0.3 µM). PK-THPP (100 mg/kg, s.c.) increases the time spent awake and decreases the duration of rapid eye movement (REM) and delta sleep in mice.
Brand:CaymanSKU:29473 - 25 mgAvailable on backorder
PK-THPP is a brain-penetrant inhibitor of the two-pore domain potassium channel K2P9.1/TASK-3 (IC50 = 0.035 µM).{53780} It is selective for K2P9.1/TASK-3 over K2P2.1/TREK1 and the voltage-gated potassium channel subtype Kv1.5 (IC50s = ~5 and >10 µM, respectively), as well as a panel of more than 100 receptors, ion channels, and enzymes at 10 µM but does inhibit K2P3.1/TASK-1 (IC50 = 0.3 µM). PK-THPP (100 mg/kg, s.c.) increases the time spent awake and decreases the duration of rapid eye movement (REM) and delta sleep in mice.
Brand:CaymanSKU:29473 - 5 mgAvailable on backorder
PKI PKA Inhibitor (5-24) is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) (Ki = 2.3 nM) derived from the active site of the skeletal muscle inhibitor protein.{26247} It mimics the protein substrate by binding to the catalytic site through the arginine-cluster basic subsite.{26247} The prominent enzyme-substrate interaction site occurs where PKA catalytic subunit residues Tyr235 and Phe239 form a sandwich-like structure with residue Phe10 of PKI (5-24).{26246}
Brand:CaymanSKU:- PKI PKA Inhibitor (5-24) is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) (Ki = 2.3 nM) derived from the active site of the skeletal muscle inhibitor protein.{26247} It mimics the protein substrate by binding to the catalytic site through the arginine-cluster basic subsite.{26247} The prominent enzyme-substrate interaction site occurs where PKA catalytic subunit residues Tyr235 and Phe239 form a sandwich-like structure with residue Phe10 of PKI (5-24).{26246}
Brand:CaymanSKU:- PKI PKA Inhibitor (5-24) is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) (Ki = 2.3 nM) derived from the active site of the skeletal muscle inhibitor protein.{26247} It mimics the protein substrate by binding to the catalytic site through the arginine-cluster basic subsite.{26247} The prominent enzyme-substrate interaction site occurs where PKA catalytic subunit residues Tyr235 and Phe239 form a sandwich-like structure with residue Phe10 of PKI (5-24).{26246}
Brand:CaymanSKU:-
PKA inhibitor fragment (6-22) amide is a synthetic peptide inhibitor of cAMP-dependent protein kinase (PKA; Ki = 1.7 nM) derived from the heat-stable PKA inhibitor protein PKI.{28748} It is the shortest synthetic PKI peptide that retains high potency for PKA inhibition. Both the arginine-containing pseudosubstrate site of the PKI peptide in its COOH terminus and the residue Phe10 in NH2-terminal portion are required for this high affinity binding.{28747}
Brand:CaymanSKU:-Available on backorder
PKA inhibitor fragment (6-22) amide is a synthetic peptide inhibitor of cAMP-dependent protein kinase (PKA; Ki = 1.7 nM) derived from the heat-stable PKA inhibitor protein PKI.{28748} It is the shortest synthetic PKI peptide that retains high potency for PKA inhibition. Both the arginine-containing pseudosubstrate site of the PKI peptide in its COOH terminus and the residue Phe10 in NH2-terminal portion are required for this high affinity binding.{28747}
Brand:CaymanSKU:-Available on backorder
PKA inhibitor fragment (6-22) amide is a synthetic peptide inhibitor of cAMP-dependent protein kinase (PKA; Ki = 1.7 nM) derived from the heat-stable PKA inhibitor protein PKI.{28748} It is the shortest synthetic PKI peptide that retains high potency for PKA inhibition. Both the arginine-containing pseudosubstrate site of the PKI peptide in its COOH terminus and the residue Phe10 in NH2-terminal portion are required for this high affinity binding.{28747}
Brand:CaymanSKU:-Available on backorder
PKA inhibitor fragment (6-22) amide is a synthetic peptide inhibitor of cAMP-dependent protein kinase (PKA; Ki = 1.7 nM) derived from the heat-stable PKA inhibitor protein PKI.{28748} It is the shortest synthetic PKI peptide that retains high potency for PKA inhibition. Both the arginine-containing pseudosubstrate site of the PKI peptide in its COOH terminus and the residue Phe10 in NH2-terminal portion are required for this high affinity binding.{28747}
Brand:CaymanSKU:-Available on backorder
PKC 412 is a cell-permeable, reversible inhibitor of several serine/threonine and tyrosine kinases, including conventional PKC isoforms (α, β, and γ), Syk, FLK1, Akt, PKA, c-Kit, C-Fgr, c-Src, FLT3, PDFRβ, VEGFR1, and VEGFR2 with IC50 values ranging from 80-500 nM.{18276,18281,18279,18278} It also upregulates the expression of endothelial nitric oxide synthase (eNOS) in mice.{18277} PKC 412 inhibits growth or induces apoptosis in many cancer cell types, blocks angiogenesis in tumors, and sensitizes cancer cells to ionizing radiation, supporting its use in cancer therapy.{18276,17279,18280}
Brand:CaymanSKU:10459 - 1 mgAvailable on backorder
PKC 412 is a cell-permeable, reversible inhibitor of several serine/threonine and tyrosine kinases, including conventional PKC isoforms (α, β, and γ), Syk, FLK1, Akt, PKA, c-Kit, C-Fgr, c-Src, FLT3, PDFRβ, VEGFR1, and VEGFR2 with IC50 values ranging from 80-500 nM.{18276,18281,18279,18278} It also upregulates the expression of endothelial nitric oxide synthase (eNOS) in mice.{18277} PKC 412 inhibits growth or induces apoptosis in many cancer cell types, blocks angiogenesis in tumors, and sensitizes cancer cells to ionizing radiation, supporting its use in cancer therapy.{18276,17279,18280}
Brand:CaymanSKU:10459 - 10 mgAvailable on backorder
PKC 412 is a cell-permeable, reversible inhibitor of several serine/threonine and tyrosine kinases, including conventional PKC isoforms (α, β, and γ), Syk, FLK1, Akt, PKA, c-Kit, C-Fgr, c-Src, FLT3, PDFRβ, VEGFR1, and VEGFR2 with IC50 values ranging from 80-500 nM.{18276,18281,18279,18278} It also upregulates the expression of endothelial nitric oxide synthase (eNOS) in mice.{18277} PKC 412 inhibits growth or induces apoptosis in many cancer cell types, blocks angiogenesis in tumors, and sensitizes cancer cells to ionizing radiation, supporting its use in cancer therapy.{18276,17279,18280}
Brand:CaymanSKU:10459 - 25 mgAvailable on backorder
PKC 412 is a cell-permeable, reversible inhibitor of several serine/threonine and tyrosine kinases, including conventional PKC isoforms (α, β, and γ), Syk, FLK1, Akt, PKA, c-Kit, C-Fgr, c-Src, FLT3, PDFRβ, VEGFR1, and VEGFR2 with IC50 values ranging from 80-500 nM.{18276,18281,18279,18278} It also upregulates the expression of endothelial nitric oxide synthase (eNOS) in mice.{18277} PKC 412 inhibits growth or induces apoptosis in many cancer cell types, blocks angiogenesis in tumors, and sensitizes cancer cells to ionizing radiation, supporting its use in cancer therapy.{18276,17279,18280}
Brand:CaymanSKU:10459 - 5 mgAvailable on backorder
PKC-9 is an inhibitor of PKCζ that is 8,000-, 20,671-, 711-, 918-, 1,895-, 12,424-, 10-, and 1,218-fold selective for PKCζ over PKCα, PKCβII, PKCγ, PKCδ, PKCε, PKCη, PKCι, and PKCθ, respectively.{36787} It also inhibits 27 additional kinases in a panel of 37 kinases when used at a concentration of 10 μM.
Brand:CaymanSKU:25556 - 1 mgAvailable on backorder
PKC-9 is an inhibitor of PKCζ that is 8,000-, 20,671-, 711-, 918-, 1,895-, 12,424-, 10-, and 1,218-fold selective for PKCζ over PKCα, PKCβII, PKCγ, PKCδ, PKCε, PKCη, PKCι, and PKCθ, respectively.{36787} It also inhibits 27 additional kinases in a panel of 37 kinases when used at a concentration of 10 μM.
Brand:CaymanSKU:25556 - 10 mgAvailable on backorder
PKC-9 is an inhibitor of PKCζ that is 8,000-, 20,671-, 711-, 918-, 1,895-, 12,424-, 10-, and 1,218-fold selective for PKCζ over PKCα, PKCβII, PKCγ, PKCδ, PKCε, PKCη, PKCι, and PKCθ, respectively.{36787} It also inhibits 27 additional kinases in a panel of 37 kinases when used at a concentration of 10 μM.
Brand:CaymanSKU:25556 - 5 mgAvailable on backorder
Protein kinase Cɛ (PKCɛ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine/threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.{9056} PKCɛ inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKCɛ.{28594} It selectively and reversibly inhibits the translocation of PKCɛ to intracellular membranes, blocking activation.{28594} PKCɛ inhibitor peptide is commonly used in cells to evaluate the role of PKCɛ in various cellular responses.{28596,28597,28595}
Brand:CaymanSKU:-Available on backorder
Protein kinase Cɛ (PKCɛ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine/threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.{9056} PKCɛ inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKCɛ.{28594} It selectively and reversibly inhibits the translocation of PKCɛ to intracellular membranes, blocking activation.{28594} PKCɛ inhibitor peptide is commonly used in cells to evaluate the role of PKCɛ in various cellular responses.{28596,28597,28595}
Brand:CaymanSKU:-Available on backorder
Protein kinase Cɛ (PKCɛ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine/threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.{9056} PKCɛ inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKCɛ.{28594} It selectively and reversibly inhibits the translocation of PKCɛ to intracellular membranes, blocking activation.{28594} PKCɛ inhibitor peptide is commonly used in cells to evaluate the role of PKCɛ in various cellular responses.{28596,28597,28595}
Brand:CaymanSKU:-Available on backorder
Protein kinase Cɛ (PKCɛ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine/threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.{9056} PKCɛ inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKCɛ.{28594} It selectively and reversibly inhibits the translocation of PKCɛ to intracellular membranes, blocking activation.{28594} PKCɛ inhibitor peptide is commonly used in cells to evaluate the role of PKCɛ in various cellular responses.{28596,28597,28595}
Brand:CaymanSKU:-Available on backorder
PKCε inhibitor scramble peptide is a scrambled peptide with identical amino acid composition to PKCε inhibitor peptide (Item No. 17476). It is intended for use as a negative control for PKCε inhibitor peptide activity.
Brand:CaymanSKU:31761 - 1 mgAvailable on backorder
The atypical protein kinase C isoform, PKCζ, is critical for mediating mitogenic signal transduction, cell survival, and some of the physiological actions of insulin.{9056} PKCζ pseudosubstrate inhibitor is a synthetic peptide that corresponds to a pseudosubstrate domain of this PKC isoform.{29579} It selectively, reversibly, and substrate-competitively inhibits PKCζ activity and, thus, is used to delineate the signaling functions of PKCζ.{29580,29578,29581}
Brand:CaymanSKU:-Available on backorder
The atypical protein kinase C isoform, PKCζ, is critical for mediating mitogenic signal transduction, cell survival, and some of the physiological actions of insulin.{9056} PKCζ pseudosubstrate inhibitor is a synthetic peptide that corresponds to a pseudosubstrate domain of this PKC isoform.{29579} It selectively, reversibly, and substrate-competitively inhibits PKCζ activity and, thus, is used to delineate the signaling functions of PKCζ.{29580,29578,29581}
Brand:CaymanSKU:-Available on backorder
The atypical protein kinase C isoform, PKCζ, is critical for mediating mitogenic signal transduction, cell survival, and some of the physiological actions of insulin.{9056} PKCζ pseudosubstrate inhibitor is a synthetic peptide that corresponds to a pseudosubstrate domain of this PKC isoform.{29579} It selectively, reversibly, and substrate-competitively inhibits PKCζ activity and, thus, is used to delineate the signaling functions of PKCζ.{29580,29578,29581}
Brand:CaymanSKU:-Available on backorder
PKF118-310 is an inhibitor of the interaction between T cell factor 4 (Tcf4) and β-catenin that is produced by Actinomycete strains.{40755} It disrupts binding of β-catenin to a GST-Tcf4 fusion protein in HCT116 cell lysates (IC50 = 0.8 µM). PKF118-310 blocks appearance of the Tcf4 and β-catenin complex bound to DNA in an EMSA assay. It reduces levels of the β-catenin regulated proteins c-Myc and cyclin D1 but has no effect on cyclin E in HCT116 cells. PKF118-310 (0.5 pmol) abrogates β-catenin, but not siamois, ventral body axis duplication induced by mRNA in Xenopus embryos. It reduces growth of HCT116, HT-29, PC3, and DU145 cancer cells in vitro (IC50s = 170-300 nM). PKF118-310 (1 mg/kg twice per week) reduces tumor growth and expression of c-Myc, cyclin D1, and Survivin in a HepG2 mouse xenograft model.{40756}
Brand:CaymanSKU:22440 -Out of stock
PKF118-310 is an inhibitor of the interaction between T cell factor 4 (Tcf4) and β-catenin that is produced by Actinomycete strains.{40755} It disrupts binding of β-catenin to a GST-Tcf4 fusion protein in HCT116 cell lysates (IC50 = 0.8 µM). PKF118-310 blocks appearance of the Tcf4 and β-catenin complex bound to DNA in an EMSA assay. It reduces levels of the β-catenin regulated proteins c-Myc and cyclin D1 but has no effect on cyclin E in HCT116 cells. PKF118-310 (0.5 pmol) abrogates β-catenin, but not siamois, ventral body axis duplication induced by mRNA in Xenopus embryos. It reduces growth of HCT116, HT-29, PC3, and DU145 cancer cells in vitro (IC50s = 170-300 nM). PKF118-310 (1 mg/kg twice per week) reduces tumor growth and expression of c-Myc, cyclin D1, and Survivin in a HepG2 mouse xenograft model.{40756}
Brand:CaymanSKU:22440 -Out of stock
PKF118-310 is an inhibitor of the interaction between T cell factor 4 (Tcf4) and β-catenin that is produced by Actinomycete strains.{40755} It disrupts binding of β-catenin to a GST-Tcf4 fusion protein in HCT116 cell lysates (IC50 = 0.8 µM). PKF118-310 blocks appearance of the Tcf4 and β-catenin complex bound to DNA in an EMSA assay. It reduces levels of the β-catenin regulated proteins c-Myc and cyclin D1 but has no effect on cyclin E in HCT116 cells. PKF118-310 (0.5 pmol) abrogates β-catenin, but not siamois, ventral body axis duplication induced by mRNA in Xenopus embryos. It reduces growth of HCT116, HT-29, PC3, and DU145 cancer cells in vitro (IC50s = 170-300 nM). PKF118-310 (1 mg/kg twice per week) reduces tumor growth and expression of c-Myc, cyclin D1, and Survivin in a HepG2 mouse xenograft model.{40756}
Brand:CaymanSKU:22440 -Out of stock
PKG drug G1 is an activator of protein kinase GIα (PKGIα).{46709} It induces relaxation in U-46619-precontracted mesenteric arteries isolated from wild-type, but not oxidation-insensitive Cys42Ser PKGIα knock-in, mice in a concentration-dependent manner. PKG drug G1 (14.8 mg/kg) induces oxidation of PKGIα, a marker of activation, in the aorta in a mouse model of angiotensin II-induced hypertension. It decreases mean arterial pressure in the same model when administered at a dose of 20 mg/kg per day for four days.
Brand:CaymanSKU:29768 - 10 mgAvailable on backorder
PKG drug G1 is an activator of protein kinase GIα (PKGIα).{46709} It induces relaxation in U-46619-precontracted mesenteric arteries isolated from wild-type, but not oxidation-insensitive Cys42Ser PKGIα knock-in, mice in a concentration-dependent manner. PKG drug G1 (14.8 mg/kg) induces oxidation of PKGIα, a marker of activation, in the aorta in a mouse model of angiotensin II-induced hypertension. It decreases mean arterial pressure in the same model when administered at a dose of 20 mg/kg per day for four days.
Brand:CaymanSKU:29768 - 100 mgAvailable on backorder
PKG drug G1 is an activator of protein kinase GIα (PKGIα).{46709} It induces relaxation in U-46619-precontracted mesenteric arteries isolated from wild-type, but not oxidation-insensitive Cys42Ser PKGIα knock-in, mice in a concentration-dependent manner. PKG drug G1 (14.8 mg/kg) induces oxidation of PKGIα, a marker of activation, in the aorta in a mouse model of angiotensin II-induced hypertension. It decreases mean arterial pressure in the same model when administered at a dose of 20 mg/kg per day for four days.
Brand:CaymanSKU:29768 - 5 mgAvailable on backorder
PKG drug G1 is an activator of protein kinase GIα (PKGIα).{46709} It induces relaxation in U-46619-precontracted mesenteric arteries isolated from wild-type, but not oxidation-insensitive Cys42Ser PKGIα knock-in, mice in a concentration-dependent manner. PKG drug G1 (14.8 mg/kg) induces oxidation of PKGIα, a marker of activation, in the aorta in a mouse model of angiotensin II-induced hypertension. It decreases mean arterial pressure in the same model when administered at a dose of 20 mg/kg per day for four days.
Brand:CaymanSKU:29768 - 50 mgAvailable on backorder
PKG inhibitor is a specific cGMP-dependent PKG inhibitor (Ki = 86 µM).{26244} This synthetic peptide is a nonphosphorylatable analog of a substrate corresponding to the serine-32 phosphorylation site in histone H2B.{26244} PKG inhibitor has been reported to block cGMP-dependent NMDA potentiation and nitric oxide-induced depression of GABA currents in cultured retinal amacrine cells.{26245}
Brand:CaymanSKU:- PKG inhibitor is a specific cGMP-dependent PKG inhibitor (Ki = 86 µM).{26244} This synthetic peptide is a nonphosphorylatable analog of a substrate corresponding to the serine-32 phosphorylation site in histone H2B.{26244} PKG inhibitor has been reported to block cGMP-dependent NMDA potentiation and nitric oxide-induced depression of GABA currents in cultured retinal amacrine cells.{26245}
Brand:CaymanSKU:- PKG inhibitor is a specific cGMP-dependent PKG inhibitor (Ki = 86 µM).{26244} This synthetic peptide is a nonphosphorylatable analog of a substrate corresponding to the serine-32 phosphorylation site in histone H2B.{26244} PKG inhibitor has been reported to block cGMP-dependent NMDA potentiation and nitric oxide-induced depression of GABA currents in cultured retinal amacrine cells.{26245}
Brand:CaymanSKU:-
PKI-166 is an ATP-competitive inhibitor of the EGF receptor (EGFR; IC50 = 0.0007 µM for the intracellular kinase domain).{42915} It is selective for the EGFR intracellular kinase domain over the serine/threonine kinases PKCα and Cdc2/cyclin B (IC50s = >100 and 78 µM, respectively), as well as FLK, c-Met, and Tek (IC50 = >1 µM for all), but does inhibit c-Src, c-Abl, VEGFR2/KDR, FLT1, and c-Kit (IC50s = 0.103, 0.028, 0.327, 0.962, and 2.21 µM, respectively). PKI-166 prevents phosphorylation of EGFR induced by EGF in L3.6pl pancreatic cancer cells in a concentration-dependent manner. It enhances the cytotoxicity of gemcitabine (Item No. 11690) in L3.6pl cells and reduces tumor growth and metastasis and increases survival in an L3.6pl mouse xenograft model when administered alone at a dose of 100 mg/kg per day with additive effects on these parameters when administered in combination with gemcitabine. PKI-166 also reduces tumor growth and inhibits angiogenesis in an SN12-PM6 human renal cell carcinoma mouse orthotopic model.
Brand:CaymanSKU:21896 -Out of stock
PKI-166 is an ATP-competitive inhibitor of the EGF receptor (EGFR; IC50 = 0.0007 µM for the intracellular kinase domain).{42915} It is selective for the EGFR intracellular kinase domain over the serine/threonine kinases PKCα and Cdc2/cyclin B (IC50s = >100 and 78 µM, respectively), as well as FLK, c-Met, and Tek (IC50 = >1 µM for all), but does inhibit c-Src, c-Abl, VEGFR2/KDR, FLT1, and c-Kit (IC50s = 0.103, 0.028, 0.327, 0.962, and 2.21 µM, respectively). PKI-166 prevents phosphorylation of EGFR induced by EGF in L3.6pl pancreatic cancer cells in a concentration-dependent manner. It enhances the cytotoxicity of gemcitabine (Item No. 11690) in L3.6pl cells and reduces tumor growth and metastasis and increases survival in an L3.6pl mouse xenograft model when administered alone at a dose of 100 mg/kg per day with additive effects on these parameters when administered in combination with gemcitabine. PKI-166 also reduces tumor growth and inhibits angiogenesis in an SN12-PM6 human renal cell carcinoma mouse orthotopic model.
Brand:CaymanSKU:21896 -Out of stock
PKI-166 is an ATP-competitive inhibitor of the EGF receptor (EGFR; IC50 = 0.0007 µM for the intracellular kinase domain).{42915} It is selective for the EGFR intracellular kinase domain over the serine/threonine kinases PKCα and Cdc2/cyclin B (IC50s = >100 and 78 µM, respectively), as well as FLK, c-Met, and Tek (IC50 = >1 µM for all), but does inhibit c-Src, c-Abl, VEGFR2/KDR, FLT1, and c-Kit (IC50s = 0.103, 0.028, 0.327, 0.962, and 2.21 µM, respectively). PKI-166 prevents phosphorylation of EGFR induced by EGF in L3.6pl pancreatic cancer cells in a concentration-dependent manner. It enhances the cytotoxicity of gemcitabine (Item No. 11690) in L3.6pl cells and reduces tumor growth and metastasis and increases survival in an L3.6pl mouse xenograft model when administered alone at a dose of 100 mg/kg per day with additive effects on these parameters when administered in combination with gemcitabine. PKI-166 also reduces tumor growth and inhibits angiogenesis in an SN12-PM6 human renal cell carcinoma mouse orthotopic model.
Brand:CaymanSKU:21896 -Out of stock
PKI-166 is an ATP-competitive inhibitor of the EGF receptor (EGFR; IC50 = 0.0007 µM for the intracellular kinase domain).{42915} It is selective for the EGFR intracellular kinase domain over the serine/threonine kinases PKCα and Cdc2/cyclin B (IC50s = >100 and 78 µM, respectively), as well as FLK, c-Met, and Tek (IC50 = >1 µM for all), but does inhibit c-Src, c-Abl, VEGFR2/KDR, FLT1, and c-Kit (IC50s = 0.103, 0.028, 0.327, 0.962, and 2.21 µM, respectively). PKI-166 prevents phosphorylation of EGFR induced by EGF in L3.6pl pancreatic cancer cells in a concentration-dependent manner. It enhances the cytotoxicity of gemcitabine (Item No. 11690) in L3.6pl cells and reduces tumor growth and metastasis and increases survival in an L3.6pl mouse xenograft model when administered alone at a dose of 100 mg/kg per day with additive effects on these parameters when administered in combination with gemcitabine. PKI-166 also reduces tumor growth and inhibits angiogenesis in an SN12-PM6 human renal cell carcinoma mouse orthotopic model.
Brand:CaymanSKU:21896 -Out of stock
PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR).{39367} In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.
Brand:CaymanSKU:21202 -Out of stock
PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR).{39367} In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.
Brand:CaymanSKU:21202 -Out of stock