Chemicals
Showing 18151–18300 of 41137 results
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Brand:CaymanSKU:760158 - 1 eaAvailable on backorder
Dutasteride is a dual inhibitor of 5α-reductase types I and II (Kis = 6 and 7 nM, respectively).{25831,25832,43107} Its inhibition is time-dependent inhibitor with apparent Ki values of 17 and 4.3 nM at 10- and 30-minute reaction times, respectively.{25831} Dutasteride decreases prostate weight in a rat model of benign prostatic hypertrophy induced by testosterone after castration when administered daily for 28 days at doses of 0.045 mg/kg as a solution or 0.756 mg/kg in subcutaneous microspheres.{43105} It also decreases prostate weight in large probasin-large T antigen mice, a transgenic model of prostate cancer.{43106} Formulations containing dutasteride have been used in the treatment of benign prostatic hyperplasia.
Brand:CaymanSKU:- Dutasteride is a dual inhibitor of 5α-reductase types I and II (Kis = 6 and 7 nM, respectively).{25831,25832,43107} Its inhibition is time-dependent inhibitor with apparent Ki values of 17 and 4.3 nM at 10- and 30-minute reaction times, respectively.{25831} Dutasteride decreases prostate weight in a rat model of benign prostatic hypertrophy induced by testosterone after castration when administered daily for 28 days at doses of 0.045 mg/kg as a solution or 0.756 mg/kg in subcutaneous microspheres.{43105} It also decreases prostate weight in large probasin-large T antigen mice, a transgenic model of prostate cancer.{43106} Formulations containing dutasteride have been used in the treatment of benign prostatic hyperplasia.
Brand:CaymanSKU:- Dutasteride is a dual inhibitor of 5α-reductase types I and II (Kis = 6 and 7 nM, respectively).{25831,25832,43107} Its inhibition is time-dependent inhibitor with apparent Ki values of 17 and 4.3 nM at 10- and 30-minute reaction times, respectively.{25831} Dutasteride decreases prostate weight in a rat model of benign prostatic hypertrophy induced by testosterone after castration when administered daily for 28 days at doses of 0.045 mg/kg as a solution or 0.756 mg/kg in subcutaneous microspheres.{43105} It also decreases prostate weight in large probasin-large T antigen mice, a transgenic model of prostate cancer.{43106} Formulations containing dutasteride have been used in the treatment of benign prostatic hyperplasia.
Brand:CaymanSKU:- Dutasteride is a dual inhibitor of 5α-reductase types I and II (Kis = 6 and 7 nM, respectively).{25831,25832,43107} Its inhibition is time-dependent inhibitor with apparent Ki values of 17 and 4.3 nM at 10- and 30-minute reaction times, respectively.{25831} Dutasteride decreases prostate weight in a rat model of benign prostatic hypertrophy induced by testosterone after castration when administered daily for 28 days at doses of 0.045 mg/kg as a solution or 0.756 mg/kg in subcutaneous microspheres.{43105} It also decreases prostate weight in large probasin-large T antigen mice, a transgenic model of prostate cancer.{43106} Formulations containing dutasteride have been used in the treatment of benign prostatic hyperplasia.
Brand:CaymanSKU:-
DWK-1339 is an inhibitor of amyloid-β (Aβ) aggregation.{35159} It inhibits aggregation of monomeric Aβ (1-42) (Aβ42) and induces disaggregation of Aβ42 fibrils in vitro when used at concentrations ranging from 3.1 to 50 µM. DWK-1339 (10 µM) reduces Aβ42-induced toxicity in HT-22 cells. In vivo, DWK-1339 (10 mg/kg) increases step-through latency in a passive avoidance test and increases spontaneous alteration in the Y-maze compared with vehicle control mice in a mouse model of Aβ42-induced acute Alzheimer’s disease. It also decreases brain levels of Aβ42 and increases spontaneous alteration in the Y-maze in the APP/PS1 transgenic mouse model of Alzheimer’s disease.
Brand:CaymanSKU:27642 - 1 mgAvailable on backorder
DWK-1339 is an inhibitor of amyloid-β (Aβ) aggregation.{35159} It inhibits aggregation of monomeric Aβ (1-42) (Aβ42) and induces disaggregation of Aβ42 fibrils in vitro when used at concentrations ranging from 3.1 to 50 µM. DWK-1339 (10 µM) reduces Aβ42-induced toxicity in HT-22 cells. In vivo, DWK-1339 (10 mg/kg) increases step-through latency in a passive avoidance test and increases spontaneous alteration in the Y-maze compared with vehicle control mice in a mouse model of Aβ42-induced acute Alzheimer’s disease. It also decreases brain levels of Aβ42 and increases spontaneous alteration in the Y-maze in the APP/PS1 transgenic mouse model of Alzheimer’s disease.
Brand:CaymanSKU:27642 - 5 mgAvailable on backorder
DWK-1339 is an inhibitor of amyloid-β (Aβ) aggregation.{35159} It inhibits aggregation of monomeric Aβ (1-42) (Aβ42) and induces disaggregation of Aβ42 fibrils in vitro when used at concentrations ranging from 3.1 to 50 µM. DWK-1339 (10 µM) reduces Aβ42-induced toxicity in HT-22 cells. In vivo, DWK-1339 (10 mg/kg) increases step-through latency in a passive avoidance test and increases spontaneous alteration in the Y-maze compared with vehicle control mice in a mouse model of Aβ42-induced acute Alzheimer’s disease. It also decreases brain levels of Aβ42 and increases spontaneous alteration in the Y-maze in the APP/PS1 transgenic mouse model of Alzheimer’s disease.
Brand:CaymanSKU:27642 - 500 µgAvailable on backorder
The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the ER family and are expressed in tissues with high metabolic demand. DY 131 is a selective agonist of the ERRβ/γ receptor (EC50 = 130 nM).{30646,30644} It does not affect the ERRα receptor nor the ERs α and β at concentrations up to 30 µM.{30646,30644} DY 131 has been used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines in order to demonstrate an antiproliferative/tumor-suppressing function for ERRγ in prostate cancer.{30645}
Brand:CaymanSKU:-Available on backorder
The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the ER family and are expressed in tissues with high metabolic demand. DY 131 is a selective agonist of the ERRβ/γ receptor (EC50 = 130 nM).{30646,30644} It does not affect the ERRα receptor nor the ERs α and β at concentrations up to 30 µM.{30646,30644} DY 131 has been used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines in order to demonstrate an antiproliferative/tumor-suppressing function for ERRγ in prostate cancer.{30645}
Brand:CaymanSKU:-Available on backorder
The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the ER family and are expressed in tissues with high metabolic demand. DY 131 is a selective agonist of the ERRβ/γ receptor (EC50 = 130 nM).{30646,30644} It does not affect the ERRα receptor nor the ERs α and β at concentrations up to 30 µM.{30646,30644} DY 131 has been used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines in order to demonstrate an antiproliferative/tumor-suppressing function for ERRγ in prostate cancer.{30645}
Brand:CaymanSKU:-Available on backorder
The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the ER family and are expressed in tissues with high metabolic demand. DY 131 is a selective agonist of the ERRβ/γ receptor (EC50 = 130 nM).{30646,30644} It does not affect the ERRα receptor nor the ERs α and β at concentrations up to 30 µM.{30646,30644} DY 131 has been used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines in order to demonstrate an antiproliferative/tumor-suppressing function for ERRγ in prostate cancer.{30645}
Brand:CaymanSKU:-Available on backorder
DY 268 is a farnesoid X receptor (FXR) antagonist (IC50 = 7.5 nM in a time-resolved FRET assay).{46589} It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM.
Brand:CaymanSKU:29475 - 1 mgAvailable on backorder
DY 268 is a farnesoid X receptor (FXR) antagonist (IC50 = 7.5 nM in a time-resolved FRET assay).{46589} It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM.
Brand:CaymanSKU:29475 - 10 mgAvailable on backorder
DY 268 is a farnesoid X receptor (FXR) antagonist (IC50 = 7.5 nM in a time-resolved FRET assay).{46589} It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM.
Brand:CaymanSKU:29475 - 25 mgAvailable on backorder
DY 268 is a farnesoid X receptor (FXR) antagonist (IC50 = 7.5 nM in a time-resolved FRET assay).{46589} It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM.
Brand:CaymanSKU:29475 - 5 mgAvailable on backorder
Dyclonine is a topical anesthetic that also has antimicrobial, anticancer, and neuroprotective properties.{52157,52158,52159} It is active against S. aureus, B. subtilis, E. coli, P. vulgaris, P. aeruginosa, C. albicans, M. lanosum, and T. mentagrophytes with minimum microbicidal concentrations (MMCs) ranging from 0.006 to 0.8% v/v.{52157} Dyclonine (25-100 μM) reduces aldehyde dehydrogenase (ALDH) activity in and viability of HSC-4 oral squamous cell carcinoma cells and enhances HSC-4 and OSC19 cell death induced by sulfasalazine (Item No. 15025).{52158} In vivo, dyclonine (5 mg/kg per day) reduces tumor volume in an HSC-2 mouse xenograft model when administered alone or in combination with sulfasalazine. Dyclonine also induces cerebral frataxin (FXN) production and decreases time to cross and the number of foot slips in a level beam test in a mouse model of Friedreich’s ataxia.{52159}
Brand:CaymanSKU:27667 - 10 gAvailable on backorder
Dyclonine is a topical anesthetic that also has antimicrobial, anticancer, and neuroprotective properties.{52157,52158,52159} It is active against S. aureus, B. subtilis, E. coli, P. vulgaris, P. aeruginosa, C. albicans, M. lanosum, and T. mentagrophytes with minimum microbicidal concentrations (MMCs) ranging from 0.006 to 0.8% v/v.{52157} Dyclonine (25-100 μM) reduces aldehyde dehydrogenase (ALDH) activity in and viability of HSC-4 oral squamous cell carcinoma cells and enhances HSC-4 and OSC19 cell death induced by sulfasalazine (Item No. 15025).{52158} In vivo, dyclonine (5 mg/kg per day) reduces tumor volume in an HSC-2 mouse xenograft model when administered alone or in combination with sulfasalazine. Dyclonine also induces cerebral frataxin (FXN) production and decreases time to cross and the number of foot slips in a level beam test in a mouse model of Friedreich’s ataxia.{52159}
Brand:CaymanSKU:27667 - 25 gAvailable on backorder
Dyclonine is a topical anesthetic that also has antimicrobial, anticancer, and neuroprotective properties.{52157,52158,52159} It is active against S. aureus, B. subtilis, E. coli, P. vulgaris, P. aeruginosa, C. albicans, M. lanosum, and T. mentagrophytes with minimum microbicidal concentrations (MMCs) ranging from 0.006 to 0.8% v/v.{52157} Dyclonine (25-100 μM) reduces aldehyde dehydrogenase (ALDH) activity in and viability of HSC-4 oral squamous cell carcinoma cells and enhances HSC-4 and OSC19 cell death induced by sulfasalazine (Item No. 15025).{52158} In vivo, dyclonine (5 mg/kg per day) reduces tumor volume in an HSC-2 mouse xenograft model when administered alone or in combination with sulfasalazine. Dyclonine also induces cerebral frataxin (FXN) production and decreases time to cross and the number of foot slips in a level beam test in a mouse model of Friedreich’s ataxia.{52159}
Brand:CaymanSKU:27667 - 5 gAvailable on backorder
Dydrogesterone is a synthetic progestogen that has no estrogenic, androgenic, glucocorticoid, or anabolic effects, although it is an agonist of progesterone receptors (EC50 = 12.3 nM) and an antagonist of androgen, mineralocorticoid, and glucocorticoid receptors (IC50s = 28.6, 82.7, and 363 nM, respectively).{46018,46019} Dydrogesterone protects against sound stress-induced abortion in mice when administered at a dose of 1.25 mg per animal prior to the stressor on day five of pregnancy.{46020} Formulations containing dydrogesterone have been used in hormone replacement therapy, in the treatment of menstrual disorders, and to prevent miscarriage.
Brand:CaymanSKU:20514 -Available on backorder
Dydrogesterone is a synthetic progestogen that has no estrogenic, androgenic, glucocorticoid, or anabolic effects, although it is an agonist of progesterone receptors (EC50 = 12.3 nM) and an antagonist of androgen, mineralocorticoid, and glucocorticoid receptors (IC50s = 28.6, 82.7, and 363 nM, respectively).{46018,46019} Dydrogesterone protects against sound stress-induced abortion in mice when administered at a dose of 1.25 mg per animal prior to the stressor on day five of pregnancy.{46020} Formulations containing dydrogesterone have been used in hormone replacement therapy, in the treatment of menstrual disorders, and to prevent miscarriage.
Brand:CaymanSKU:20514 -Available on backorder
Dydrogesterone is a synthetic progestogen that has no estrogenic, androgenic, glucocorticoid, or anabolic effects, although it is an agonist of progesterone receptors (EC50 = 12.3 nM) and an antagonist of androgen, mineralocorticoid, and glucocorticoid receptors (IC50s = 28.6, 82.7, and 363 nM, respectively).{46018,46019} Dydrogesterone protects against sound stress-induced abortion in mice when administered at a dose of 1.25 mg per animal prior to the stressor on day five of pregnancy.{46020} Formulations containing dydrogesterone have been used in hormone replacement therapy, in the treatment of menstrual disorders, and to prevent miscarriage.
Brand:CaymanSKU:20514 -Available on backorder
Mild oxidation can convert the sulfhydryl group of cysteine residues on proteins to cysteine-sulfenic acid derivatives (Cys-SOH).{20734} Protein sulfenylation, then, is a post-translational modification that is relevant to redox signaling. DYn-2 is a chemoselective probe for detecting sulfenylated proteins in intact cells.{20729} DYn-2 consists of 1,3-cyclohexanedione coupled to an alkyne moiety by a 3-carbon spacer. The cyclohexanedione group selectively reacts with protein sulfenic acid modifications.{20729} The alkyne group of DYn-2 can then be detected using azide-bearing tags by standard click chemistry. This approach offers superior sensitivity relative to using azide-modified probes with alkynyl detection tags.{20733}
Brand:CaymanSKU:11220 - 1 mgAvailable on backorder
Mild oxidation can convert the sulfhydryl group of cysteine residues on proteins to cysteine-sulfenic acid derivatives (Cys-SOH).{20734} Protein sulfenylation, then, is a post-translational modification that is relevant to redox signaling. DYn-2 is a chemoselective probe for detecting sulfenylated proteins in intact cells.{20729} DYn-2 consists of 1,3-cyclohexanedione coupled to an alkyne moiety by a 3-carbon spacer. The cyclohexanedione group selectively reacts with protein sulfenic acid modifications.{20729} The alkyne group of DYn-2 can then be detected using azide-bearing tags by standard click chemistry. This approach offers superior sensitivity relative to using azide-modified probes with alkynyl detection tags.{20733}
Brand:CaymanSKU:11220 - 10 mgAvailable on backorder
Mild oxidation can convert the sulfhydryl group of cysteine residues on proteins to cysteine-sulfenic acid derivatives (Cys-SOH).{20734} Protein sulfenylation, then, is a post-translational modification that is relevant to redox signaling. DYn-2 is a chemoselective probe for detecting sulfenylated proteins in intact cells.{20729} DYn-2 consists of 1,3-cyclohexanedione coupled to an alkyne moiety by a 3-carbon spacer. The cyclohexanedione group selectively reacts with protein sulfenic acid modifications.{20729} The alkyne group of DYn-2 can then be detected using azide-bearing tags by standard click chemistry. This approach offers superior sensitivity relative to using azide-modified probes with alkynyl detection tags.{20733}
Brand:CaymanSKU:11220 - 25 mgAvailable on backorder
Mild oxidation can convert the sulfhydryl group of cysteine residues on proteins to cysteine-sulfenic acid derivatives (Cys-SOH).{20734} Protein sulfenylation, then, is a post-translational modification that is relevant to redox signaling. DYn-2 is a chemoselective probe for detecting sulfenylated proteins in intact cells.{20729} DYn-2 consists of 1,3-cyclohexanedione coupled to an alkyne moiety by a 3-carbon spacer. The cyclohexanedione group selectively reacts with protein sulfenic acid modifications.{20729} The alkyne group of DYn-2 can then be detected using azide-bearing tags by standard click chemistry. This approach offers superior sensitivity relative to using azide-modified probes with alkynyl detection tags.{20733}
Brand:CaymanSKU:11220 - 5 mgAvailable on backorder
Dynasore is a cell-permeable, reversible inhibitor of dynamin 1, dynamin 2, and mitochondrial dynamin, Drp1 GTPase activity (IC50 = 15 μM).{22175}{22174} Through this action, dynasore inhibits clathrin-dependent vesicle formation and endocytosis, which is necessary for internalization of certain parasites and viruses, as well as particles and receptor ligands.{22171}{22170}{22172} In some cases, dynasore can also augment the release of neurotransmitters and secreted cytokines.{22173}{22176}
Brand:CaymanSKU:- Dynasore is a cell-permeable, reversible inhibitor of dynamin 1, dynamin 2, and mitochondrial dynamin, Drp1 GTPase activity (IC50 = 15 μM).{22175}{22174} Through this action, dynasore inhibits clathrin-dependent vesicle formation and endocytosis, which is necessary for internalization of certain parasites and viruses, as well as particles and receptor ligands.{22171}{22170}{22172} In some cases, dynasore can also augment the release of neurotransmitters and secreted cytokines.{22173}{22176}
Brand:CaymanSKU:- Dynasore is a cell-permeable, reversible inhibitor of dynamin 1, dynamin 2, and mitochondrial dynamin, Drp1 GTPase activity (IC50 = 15 μM).{22175}{22174} Through this action, dynasore inhibits clathrin-dependent vesicle formation and endocytosis, which is necessary for internalization of certain parasites and viruses, as well as particles and receptor ligands.{22171}{22170}{22172} In some cases, dynasore can also augment the release of neurotransmitters and secreted cytokines.{22173}{22176}
Brand:CaymanSKU:- Dynasore is a cell-permeable, reversible inhibitor of dynamin 1, dynamin 2, and mitochondrial dynamin, Drp1 GTPase activity (IC50 = 15 μM).{22175}{22174} Through this action, dynasore inhibits clathrin-dependent vesicle formation and endocytosis, which is necessary for internalization of certain parasites and viruses, as well as particles and receptor ligands.{22171}{22170}{22172} In some cases, dynasore can also augment the release of neurotransmitters and secreted cytokines.{22173}{22176}
Brand:CaymanSKU:-
Dyngo-4a is an inhibitor of dynamin with IC50 values of 380 and 2,300 nM for native sheep brain dynamin 1 and recombinant rat dynamin 2, respectively.{46647} It inhibits dynamin 1 helix formation induced by L-phosphatidylserine (PS) liposomes (IC50 = 0.38 µM) more potently than dynamin 1 single-ring formation induced by Grb2 (IC50 = 39.2 µM) and does not inhibit the basal GTPase activity of dynamin.{46647,46648} Dyngo-4a inhibits non-neuronal clathrin-mediated (IC50 = 5.7 µM in U2OS cells) and synaptic vesicle endocytosis (IC50 = 26.8 µM in rat brain synaptosomes).{46647}
Brand:CaymanSKU:29479 - 10 mgAvailable on backorder
Dyngo-4a is an inhibitor of dynamin with IC50 values of 380 and 2,300 nM for native sheep brain dynamin 1 and recombinant rat dynamin 2, respectively.{46647} It inhibits dynamin 1 helix formation induced by L-phosphatidylserine (PS) liposomes (IC50 = 0.38 µM) more potently than dynamin 1 single-ring formation induced by Grb2 (IC50 = 39.2 µM) and does not inhibit the basal GTPase activity of dynamin.{46647,46648} Dyngo-4a inhibits non-neuronal clathrin-mediated (IC50 = 5.7 µM in U2OS cells) and synaptic vesicle endocytosis (IC50 = 26.8 µM in rat brain synaptosomes).{46647}
Brand:CaymanSKU:29479 - 100 mgAvailable on backorder
Dyngo-4a is an inhibitor of dynamin with IC50 values of 380 and 2,300 nM for native sheep brain dynamin 1 and recombinant rat dynamin 2, respectively.{46647} It inhibits dynamin 1 helix formation induced by L-phosphatidylserine (PS) liposomes (IC50 = 0.38 µM) more potently than dynamin 1 single-ring formation induced by Grb2 (IC50 = 39.2 µM) and does not inhibit the basal GTPase activity of dynamin.{46647,46648} Dyngo-4a inhibits non-neuronal clathrin-mediated (IC50 = 5.7 µM in U2OS cells) and synaptic vesicle endocytosis (IC50 = 26.8 µM in rat brain synaptosomes).{46647}
Brand:CaymanSKU:29479 - 5 mgAvailable on backorder
Dyngo-4a is an inhibitor of dynamin with IC50 values of 380 and 2,300 nM for native sheep brain dynamin 1 and recombinant rat dynamin 2, respectively.{46647} It inhibits dynamin 1 helix formation induced by L-phosphatidylserine (PS) liposomes (IC50 = 0.38 µM) more potently than dynamin 1 single-ring formation induced by Grb2 (IC50 = 39.2 µM) and does not inhibit the basal GTPase activity of dynamin.{46647,46648} Dyngo-4a inhibits non-neuronal clathrin-mediated (IC50 = 5.7 µM in U2OS cells) and synaptic vesicle endocytosis (IC50 = 26.8 µM in rat brain synaptosomes).{46647}
Brand:CaymanSKU:29479 - 50 mgAvailable on backorder
Dynorphin A is a heptadecapeptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system, where it is implicated in antinociceptive functions.{29497,29499,29498} It acts as an opioid receptor agonist with nanomolar binding affinity to the three major isotypes κ, µ, and δ (Kis = 0.5-1 nM) and has also been shown to activate human ORL1, a novel opioid receptor-like receptor (Ki = 386 nM).{29543}
Brand:CaymanSKU:-Available on backorder
Dynorphin A is a heptadecapeptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system, where it is implicated in antinociceptive functions.{29497,29499,29498} It acts as an opioid receptor agonist with nanomolar binding affinity to the three major isotypes κ, µ, and δ (Kis = 0.5-1 nM) and has also been shown to activate human ORL1, a novel opioid receptor-like receptor (Ki = 386 nM).{29543}
Brand:CaymanSKU:-Available on backorder
Dynorphin A is a heptadecapeptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system, where it is implicated in antinociceptive functions.{29497,29499,29498} It acts as an opioid receptor agonist with nanomolar binding affinity to the three major isotypes κ, µ, and δ (Kis = 0.5-1 nM) and has also been shown to activate human ORL1, a novel opioid receptor-like receptor (Ki = 386 nM).{29543}
Brand:CaymanSKU:-Available on backorder
Dynorphin A is a heptadecapeptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system, where it is implicated in antinociceptive functions.{29497,29499,29498} It acts as an opioid receptor agonist with nanomolar binding affinity to the three major isotypes κ, µ, and δ (Kis = 0.5-1 nM) and has also been shown to activate human ORL1, a novel opioid receptor-like receptor (Ki = 386 nM).{29543}
Brand:CaymanSKU:-Available on backorder
Dynorphin B is a 13-residue opioid peptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system.{29497,29499} It acts as a κ1b-opioid receptor agonist (Ki = 1.1 nM) and has been implicated in antinociceptive functions.{29498} Dynorphin B has also been used to prime cardiogenesis in pluripotent embryonic stem cells.{29500}
Brand:CaymanSKU:-Available on backorder
Dynorphin B is a 13-residue opioid peptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system.{29497,29499} It acts as a κ1b-opioid receptor agonist (Ki = 1.1 nM) and has been implicated in antinociceptive functions.{29498} Dynorphin B has also been used to prime cardiogenesis in pluripotent embryonic stem cells.{29500}
Brand:CaymanSKU:-Available on backorder
Dynorphin B is a 13-residue opioid peptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system.{29497,29499} It acts as a κ1b-opioid receptor agonist (Ki = 1.1 nM) and has been implicated in antinociceptive functions.{29498} Dynorphin B has also been used to prime cardiogenesis in pluripotent embryonic stem cells.{29500}
Brand:CaymanSKU:-Available on backorder
Dynorphin B is a 13-residue opioid peptide released from the cleavage of prodynorphin and found widely distributed in the central nervous system.{29497,29499} It acts as a κ1b-opioid receptor agonist (Ki = 1.1 nM) and has been implicated in antinociceptive functions.{29498} Dynorphin B has also been used to prime cardiogenesis in pluripotent embryonic stem cells.{29500}
Brand:CaymanSKU:-Available on backorder
Dyphylline is a xanthine derivative that acts as an A1 and A2 adenosine receptor antagonist and phosphodiesterase inhibitor and exhibits bronchodilator and vasodilator effects.{29139,29142} It also moderately inhibits microsomal prostaglandin E synthase-1 with an IC50 value of 200 µM and downregulates ABCG2 drug transporter expression in multidrug resistant tumor cells.{29140,29141}
Brand:CaymanSKU:-Available on backorder
Dyphylline is a xanthine derivative that acts as an A1 and A2 adenosine receptor antagonist and phosphodiesterase inhibitor and exhibits bronchodilator and vasodilator effects.{29139,29142} It also moderately inhibits microsomal prostaglandin E synthase-1 with an IC50 value of 200 µM and downregulates ABCG2 drug transporter expression in multidrug resistant tumor cells.{29140,29141}
Brand:CaymanSKU:-Available on backorder
Dyphylline is a xanthine derivative that acts as an A1 and A2 adenosine receptor antagonist and phosphodiesterase inhibitor and exhibits bronchodilator and vasodilator effects.{29139,29142} It also moderately inhibits microsomal prostaglandin E synthase-1 with an IC50 value of 200 µM and downregulates ABCG2 drug transporter expression in multidrug resistant tumor cells.{29140,29141}
Brand:CaymanSKU:-Available on backorder
Dyphylline is a xanthine derivative that acts as an A1 and A2 adenosine receptor antagonist and phosphodiesterase inhibitor and exhibits bronchodilator and vasodilator effects.{29139,29142} It also moderately inhibits microsomal prostaglandin E synthase-1 with an IC50 value of 200 µM and downregulates ABCG2 drug transporter expression in multidrug resistant tumor cells.{29140,29141}
Brand:CaymanSKU:-Available on backorder
Voltage-gated potassium ERG channels (Kv11.1), encoded by the ether-a-go-go related gene, mediate the inwardly rectifying potassium (K+) current that repolarizes myocardial cells, gut smooth muscle cells, and interstitial cells of Cajal.{24506} E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM).{24130,24505} E-4031 inhibits the ERG1, ERG2, and ERG3 isoforms with KD values of 99, 116, and 193 nM, respectively.{24503} However, at higher μM concentrations E-4031 can demonstrate pro-arrhythmic activity, inducing early after depolarizations (prolonged repolarization) in cell models and torsade de pointes in animal models.{24131} E-4031 has been used to pharmacologically rescue misprocessed ERG in long QT syndrome type 2, an autosomal dominant cardiac disease associated with prolongation of the QT interval and torsade de pointes.{24504}
Brand:CaymanSKU:- Voltage-gated potassium ERG channels (Kv11.1), encoded by the ether-a-go-go related gene, mediate the inwardly rectifying potassium (K+) current that repolarizes myocardial cells, gut smooth muscle cells, and interstitial cells of Cajal.{24506} E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM).{24130,24505} E-4031 inhibits the ERG1, ERG2, and ERG3 isoforms with KD values of 99, 116, and 193 nM, respectively.{24503} However, at higher μM concentrations E-4031 can demonstrate pro-arrhythmic activity, inducing early after depolarizations (prolonged repolarization) in cell models and torsade de pointes in animal models.{24131} E-4031 has been used to pharmacologically rescue misprocessed ERG in long QT syndrome type 2, an autosomal dominant cardiac disease associated with prolongation of the QT interval and torsade de pointes.{24504}
Brand:CaymanSKU:- Voltage-gated potassium ERG channels (Kv11.1), encoded by the ether-a-go-go related gene, mediate the inwardly rectifying potassium (K+) current that repolarizes myocardial cells, gut smooth muscle cells, and interstitial cells of Cajal.{24506} E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM).{24130,24505} E-4031 inhibits the ERG1, ERG2, and ERG3 isoforms with KD values of 99, 116, and 193 nM, respectively.{24503} However, at higher μM concentrations E-4031 can demonstrate pro-arrhythmic activity, inducing early after depolarizations (prolonged repolarization) in cell models and torsade de pointes in animal models.{24131} E-4031 has been used to pharmacologically rescue misprocessed ERG in long QT syndrome type 2, an autosomal dominant cardiac disease associated with prolongation of the QT interval and torsade de pointes.{24504}
Brand:CaymanSKU:- Voltage-gated potassium ERG channels (Kv11.1), encoded by the ether-a-go-go related gene, mediate the inwardly rectifying potassium (K+) current that repolarizes myocardial cells, gut smooth muscle cells, and interstitial cells of Cajal.{24506} E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM).{24130,24505} E-4031 inhibits the ERG1, ERG2, and ERG3 isoforms with KD values of 99, 116, and 193 nM, respectively.{24503} However, at higher μM concentrations E-4031 can demonstrate pro-arrhythmic activity, inducing early after depolarizations (prolonged repolarization) in cell models and torsade de pointes in animal models.{24131} E-4031 has been used to pharmacologically rescue misprocessed ERG in long QT syndrome type 2, an autosomal dominant cardiac disease associated with prolongation of the QT interval and torsade de pointes.{24504}
Brand:CaymanSKU:-
E-64 is a fungal metabolite originally isolated from Aspergillus japonicus that has diverse biological activities.{52880,17474,54647,52881,52882} It inhibits a variety of cysteine proteases, including cathepsins B, H, and L, as well as papain, ficin, and bromelain, but not the serine proteases plasmin, trypsin, and tissue kallikrein or the aspartic protease pepsin.{17474,52880} E-64 (0.1-2 mg/ml) reduces the autocatalytic activity of the foot-and-mouth-disease virus (FMDV) leader protease.{54647} It is active against the FCR3 P. falciparum strain with an IC50 value of 836 nM.{52881} E-64 (5-25 µM) reduces bone resorption in embryonic mouse bone explants.{52882}
Brand:CaymanSKU:10007963 - 10 mgAvailable on backorder
E-64 is a fungal metabolite originally isolated from Aspergillus japonicus that has diverse biological activities.{52880,17474,54647,52881,52882} It inhibits a variety of cysteine proteases, including cathepsins B, H, and L, as well as papain, ficin, and bromelain, but not the serine proteases plasmin, trypsin, and tissue kallikrein or the aspartic protease pepsin.{17474,52880} E-64 (0.1-2 mg/ml) reduces the autocatalytic activity of the foot-and-mouth-disease virus (FMDV) leader protease.{54647} It is active against the FCR3 P. falciparum strain with an IC50 value of 836 nM.{52881} E-64 (5-25 µM) reduces bone resorption in embryonic mouse bone explants.{52882}
Brand:CaymanSKU:10007963 - 25 mgAvailable on backorder
E-64 is a fungal metabolite originally isolated from Aspergillus japonicus that has diverse biological activities.{52880,17474,54647,52881,52882} It inhibits a variety of cysteine proteases, including cathepsins B, H, and L, as well as papain, ficin, and bromelain, but not the serine proteases plasmin, trypsin, and tissue kallikrein or the aspartic protease pepsin.{17474,52880} E-64 (0.1-2 mg/ml) reduces the autocatalytic activity of the foot-and-mouth-disease virus (FMDV) leader protease.{54647} It is active against the FCR3 P. falciparum strain with an IC50 value of 836 nM.{52881} E-64 (5-25 µM) reduces bone resorption in embryonic mouse bone explants.{52882}
Brand:CaymanSKU:10007963 - 5 mgAvailable on backorder
E-64 is a fungal metabolite originally isolated from Aspergillus japonicus that has diverse biological activities.{52880,17474,54647,52881,52882} It inhibits a variety of cysteine proteases, including cathepsins B, H, and L, as well as papain, ficin, and bromelain, but not the serine proteases plasmin, trypsin, and tissue kallikrein or the aspartic protease pepsin.{17474,52880} E-64 (0.1-2 mg/ml) reduces the autocatalytic activity of the foot-and-mouth-disease virus (FMDV) leader protease.{54647} It is active against the FCR3 P. falciparum strain with an IC50 value of 836 nM.{52881} E-64 (5-25 µM) reduces bone resorption in embryonic mouse bone explants.{52882}
Brand:CaymanSKU:10007963 - 50 mgAvailable on backorder
E-64c is an active metabolite of the protease inhibitor E-64d (Item No. 13533).{14249,58182,54647,54648} E-64c inhibits the cysteine proteases cathepsin B, cathepsin H, and papain but not the serine proteases trypsin, chymotrypsin, or elastase.{17474,54649} It reduces the autocatalytic activity of the foot-and-mouth-disease virus (FMDV) leader protease when used at concentrations ranging from 0.1 to 1 mg/ml.{54647} E-64c reduces infection of HEK293T cells by an HIV-based virus system pseudotyped with severe acute respiratory syndrome coronavirus (SARS-CoV) surface glycoprotein, also known as the spike glycoprotein, in a concentration-dependent manner.{54648}
Brand:CaymanSKU:10007964 - 1 mgAvailable on backorder
E-64c is an active metabolite of the protease inhibitor E-64d (Item No. 13533).{14249,58182,54647,54648} E-64c inhibits the cysteine proteases cathepsin B, cathepsin H, and papain but not the serine proteases trypsin, chymotrypsin, or elastase.{17474,54649} It reduces the autocatalytic activity of the foot-and-mouth-disease virus (FMDV) leader protease when used at concentrations ranging from 0.1 to 1 mg/ml.{54647} E-64c reduces infection of HEK293T cells by an HIV-based virus system pseudotyped with severe acute respiratory syndrome coronavirus (SARS-CoV) surface glycoprotein, also known as the spike glycoprotein, in a concentration-dependent manner.{54648}
Brand:CaymanSKU:10007964 - 10 mgAvailable on backorder
E-64c is an active metabolite of the protease inhibitor E-64d (Item No. 13533).{14249,58182,54647,54648} E-64c inhibits the cysteine proteases cathepsin B, cathepsin H, and papain but not the serine proteases trypsin, chymotrypsin, or elastase.{17474,54649} It reduces the autocatalytic activity of the foot-and-mouth-disease virus (FMDV) leader protease when used at concentrations ranging from 0.1 to 1 mg/ml.{54647} E-64c reduces infection of HEK293T cells by an HIV-based virus system pseudotyped with severe acute respiratory syndrome coronavirus (SARS-CoV) surface glycoprotein, also known as the spike glycoprotein, in a concentration-dependent manner.{54648}
Brand:CaymanSKU:10007964 - 25 mgAvailable on backorder
E-64c is an active metabolite of the protease inhibitor E-64d (Item No. 13533).{14249,58182,54647,54648} E-64c inhibits the cysteine proteases cathepsin B, cathepsin H, and papain but not the serine proteases trypsin, chymotrypsin, or elastase.{17474,54649} It reduces the autocatalytic activity of the foot-and-mouth-disease virus (FMDV) leader protease when used at concentrations ranging from 0.1 to 1 mg/ml.{54647} E-64c reduces infection of HEK293T cells by an HIV-based virus system pseudotyped with severe acute respiratory syndrome coronavirus (SARS-CoV) surface glycoprotein, also known as the spike glycoprotein, in a concentration-dependent manner.{54648}
Brand:CaymanSKU:10007964 - 5 mgAvailable on backorder
E-64d is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases and has diverse biological activities.{18463,14249,18464,49542} It is a synthetic analog of E-64 (Item No. 10007963) and prodrug form of E-64c (Item No. 10007964) that inhibits calpain and the cysteine proteases cathepsins F, -K, -B, -H, and -L.{18463, 58182} E-64d (20-200 µM) induces cell cycle arrest at the G2/M phase in A431 human epidermoid carcinoma cells.{14249} It inhibits protease-resistant prion protein accumulation in scrapie-infected neuroblastoma cells with an IC50 value of 0.5 µM.{18464} E-64d also inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) and SARS-CoV-2 surface glycoprotein incorporation into pseudotyped vesicular stomatitis virus (VSV) particles in Vero cells, an effect that is reduced by expression of the serine protease TMPRSS2.{49542}
Brand:CaymanSKU:- E-64d is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases and has diverse biological activities.{18463,14249,18464,49542} It is a synthetic analog of E-64 (Item No. 10007963) and prodrug form of E-64c (Item No. 10007964) that inhibits calpain and the cysteine proteases cathepsins F, -K, -B, -H, and -L.{18463, 58182} E-64d (20-200 µM) induces cell cycle arrest at the G2/M phase in A431 human epidermoid carcinoma cells.{14249} It inhibits protease-resistant prion protein accumulation in scrapie-infected neuroblastoma cells with an IC50 value of 0.5 µM.{18464} E-64d also inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) and SARS-CoV-2 surface glycoprotein incorporation into pseudotyped vesicular stomatitis virus (VSV) particles in Vero cells, an effect that is reduced by expression of the serine protease TMPRSS2.{49542}
Brand:CaymanSKU:- E-64d is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases and has diverse biological activities.{18463,14249,18464,49542} It is a synthetic analog of E-64 (Item No. 10007963) and prodrug form of E-64c (Item No. 10007964) that inhibits calpain and the cysteine proteases cathepsins F, -K, -B, -H, and -L.{18463, 58182} E-64d (20-200 µM) induces cell cycle arrest at the G2/M phase in A431 human epidermoid carcinoma cells.{14249} It inhibits protease-resistant prion protein accumulation in scrapie-infected neuroblastoma cells with an IC50 value of 0.5 µM.{18464} E-64d also inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) and SARS-CoV-2 surface glycoprotein incorporation into pseudotyped vesicular stomatitis virus (VSV) particles in Vero cells, an effect that is reduced by expression of the serine protease TMPRSS2.{49542}
Brand:CaymanSKU:- E-64d is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases and has diverse biological activities.{18463,14249,18464,49542} It is a synthetic analog of E-64 (Item No. 10007963) and prodrug form of E-64c (Item No. 10007964) that inhibits calpain and the cysteine proteases cathepsins F, -K, -B, -H, and -L.{18463, 58182} E-64d (20-200 µM) induces cell cycle arrest at the G2/M phase in A431 human epidermoid carcinoma cells.{14249} It inhibits protease-resistant prion protein accumulation in scrapie-infected neuroblastoma cells with an IC50 value of 0.5 µM.{18464} E-64d also inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) and SARS-CoV-2 surface glycoprotein incorporation into pseudotyped vesicular stomatitis virus (VSV) particles in Vero cells, an effect that is reduced by expression of the serine protease TMPRSS2.{49542}
Brand:CaymanSKU:-
E2012 is a modulator of γ-secretase.{48834} It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-β (Aβ) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by γ-secretase, when used at a concentration of 1 µM in luciferase assays.{48835} E2012 also inhibits the activity of the cholesterol synthesis enzyme 3β-hydroxysterol ∆24-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively).{48836} It reduces Aβ (1-42) (Aβ42) production in primary rat embryonic cerebral cortex neurons with an IC50 value of 220 nM.{48837} E2012 (100 mg/kg) also decreases Aβ42 levels in guinea pig brain and cerebral spinal fluid (CSF).{48837}
Brand:CaymanSKU:29710 - 10 mgAvailable on backorder
E2012 is a modulator of γ-secretase.{48834} It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-β (Aβ) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by γ-secretase, when used at a concentration of 1 µM in luciferase assays.{48835} E2012 also inhibits the activity of the cholesterol synthesis enzyme 3β-hydroxysterol ∆24-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively).{48836} It reduces Aβ (1-42) (Aβ42) production in primary rat embryonic cerebral cortex neurons with an IC50 value of 220 nM.{48837} E2012 (100 mg/kg) also decreases Aβ42 levels in guinea pig brain and cerebral spinal fluid (CSF).{48837}
Brand:CaymanSKU:29710 - 25 mgAvailable on backorder
E2012 is a modulator of γ-secretase.{48834} It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-β (Aβ) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by γ-secretase, when used at a concentration of 1 µM in luciferase assays.{48835} E2012 also inhibits the activity of the cholesterol synthesis enzyme 3β-hydroxysterol ∆24-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively).{48836} It reduces Aβ (1-42) (Aβ42) production in primary rat embryonic cerebral cortex neurons with an IC50 value of 220 nM.{48837} E2012 (100 mg/kg) also decreases Aβ42 levels in guinea pig brain and cerebral spinal fluid (CSF).{48837}
Brand:CaymanSKU:29710 - 5 mgAvailable on backorder
E2012 is a modulator of γ-secretase.{48834} It selectively inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-β (Aβ) over Notch cleavage to its signaling effector Notch intracellular domain (NICD), processes both mediated by γ-secretase, when used at a concentration of 1 µM in luciferase assays.{48835} E2012 also inhibits the activity of the cholesterol synthesis enzyme 3β-hydroxysterol ∆24-reductase (DHCR24) in primary rat hepatocytes and HepG2 cells (IC50s = 11 and 15 nM, respectively).{48836} It reduces Aβ (1-42) (Aβ42) production in primary rat embryonic cerebral cortex neurons with an IC50 value of 220 nM.{48837} E2012 (100 mg/kg) also decreases Aβ42 levels in guinea pig brain and cerebral spinal fluid (CSF).{48837}
Brand:CaymanSKU:29710 - 50 mgAvailable on backorder
E3330 is an inhibitor of apurinic-apyrimidinic endonuclease 1/redox factor-1 (APE1/Ref-1) redox activity.{59711,59712} It inhibits APE1-mediated AP-1 DNA binding activity with an IC50 value of 6.5 µM in a redox EMSA but has no effect on APE1-mediated DNA repair activity in endonuclease or gap-filling assays when used at concentrations ranging from 0.01 to 50 µM.{59711} E3330 reduces basal activation of NF-κB, AP-1, and HIF-1 in reporter assays using PANC-1 pancreatic cancer cells.{59712} It inhibits proliferation of PaCa-2 and PANC-1 pancreatic cancer cells (EC50s = 135 and 87 µM, respectively). E3330 (25 mg/kg) inhibits tumor growth in a PaCa-2 mouse xenograft model and pancreatic cancer patient-derived xenograft (PDX) mouse models.
Brand:CaymanSKU:32830 - 10 mgAvailable on backorder
E3330 is an inhibitor of apurinic-apyrimidinic endonuclease 1/redox factor-1 (APE1/Ref-1) redox activity.{59711,59712} It inhibits APE1-mediated AP-1 DNA binding activity with an IC50 value of 6.5 µM in a redox EMSA but has no effect on APE1-mediated DNA repair activity in endonuclease or gap-filling assays when used at concentrations ranging from 0.01 to 50 µM.{59711} E3330 reduces basal activation of NF-κB, AP-1, and HIF-1 in reporter assays using PANC-1 pancreatic cancer cells.{59712} It inhibits proliferation of PaCa-2 and PANC-1 pancreatic cancer cells (EC50s = 135 and 87 µM, respectively). E3330 (25 mg/kg) inhibits tumor growth in a PaCa-2 mouse xenograft model and pancreatic cancer patient-derived xenograft (PDX) mouse models.
Brand:CaymanSKU:32830 - 25 mgAvailable on backorder
E3330 is an inhibitor of apurinic-apyrimidinic endonuclease 1/redox factor-1 (APE1/Ref-1) redox activity.{59711,59712} It inhibits APE1-mediated AP-1 DNA binding activity with an IC50 value of 6.5 µM in a redox EMSA but has no effect on APE1-mediated DNA repair activity in endonuclease or gap-filling assays when used at concentrations ranging from 0.01 to 50 µM.{59711} E3330 reduces basal activation of NF-κB, AP-1, and HIF-1 in reporter assays using PANC-1 pancreatic cancer cells.{59712} It inhibits proliferation of PaCa-2 and PANC-1 pancreatic cancer cells (EC50s = 135 and 87 µM, respectively). E3330 (25 mg/kg) inhibits tumor growth in a PaCa-2 mouse xenograft model and pancreatic cancer patient-derived xenograft (PDX) mouse models.
Brand:CaymanSKU:32830 - 5 mgAvailable on backorder
E6005 is an inhibitor of phosphodiesterase 4 (PDE4; IC50 = 2.8 nM).{53585} It is selective for PDE4 over PDE1, PDE2, PDE3, and PDE5 with only 46.1, 51.6, 69.4, and 57.4% inhibition, respectively, at 30 µM. It inhibits the production of various cytokines in isolated human lymphocytes and monocytes (IC50s = 0.49-3.1 nM). Topical application of E6005 (0.003-0.3%) reduces ear thickness in a mouse model of oxazolone-induced skin inflammation, as well as reduces oxazolone-induced scratching in mice. It reduces the severity of skin lesions in a model of mite-induced atopic dermatitis. Topical application of E6005 (0.03%) also inhibits the production of leukotriene B4 (LTB4; Item No. 20110) in mouse skin, as well as reduces scratching and cutaneous nerve firing induced by the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 (Item No. 16723) in mice.{53586}
Brand:CaymanSKU:30203 - 1 mgAvailable on backorder
E6005 is an inhibitor of phosphodiesterase 4 (PDE4; IC50 = 2.8 nM).{53585} It is selective for PDE4 over PDE1, PDE2, PDE3, and PDE5 with only 46.1, 51.6, 69.4, and 57.4% inhibition, respectively, at 30 µM. It inhibits the production of various cytokines in isolated human lymphocytes and monocytes (IC50s = 0.49-3.1 nM). Topical application of E6005 (0.003-0.3%) reduces ear thickness in a mouse model of oxazolone-induced skin inflammation, as well as reduces oxazolone-induced scratching in mice. It reduces the severity of skin lesions in a model of mite-induced atopic dermatitis. Topical application of E6005 (0.03%) also inhibits the production of leukotriene B4 (LTB4; Item No. 20110) in mouse skin, as well as reduces scratching and cutaneous nerve firing induced by the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 (Item No. 16723) in mice.{53586}
Brand:CaymanSKU:30203 - 10 mgAvailable on backorder
E6005 is an inhibitor of phosphodiesterase 4 (PDE4; IC50 = 2.8 nM).{53585} It is selective for PDE4 over PDE1, PDE2, PDE3, and PDE5 with only 46.1, 51.6, 69.4, and 57.4% inhibition, respectively, at 30 µM. It inhibits the production of various cytokines in isolated human lymphocytes and monocytes (IC50s = 0.49-3.1 nM). Topical application of E6005 (0.003-0.3%) reduces ear thickness in a mouse model of oxazolone-induced skin inflammation, as well as reduces oxazolone-induced scratching in mice. It reduces the severity of skin lesions in a model of mite-induced atopic dermatitis. Topical application of E6005 (0.03%) also inhibits the production of leukotriene B4 (LTB4; Item No. 20110) in mouse skin, as well as reduces scratching and cutaneous nerve firing induced by the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 (Item No. 16723) in mice.{53586}
Brand:CaymanSKU:30203 - 25 mgAvailable on backorder
E6005 is an inhibitor of phosphodiesterase 4 (PDE4; IC50 = 2.8 nM).{53585} It is selective for PDE4 over PDE1, PDE2, PDE3, and PDE5 with only 46.1, 51.6, 69.4, and 57.4% inhibition, respectively, at 30 µM. It inhibits the production of various cytokines in isolated human lymphocytes and monocytes (IC50s = 0.49-3.1 nM). Topical application of E6005 (0.003-0.3%) reduces ear thickness in a mouse model of oxazolone-induced skin inflammation, as well as reduces oxazolone-induced scratching in mice. It reduces the severity of skin lesions in a model of mite-induced atopic dermatitis. Topical application of E6005 (0.03%) also inhibits the production of leukotriene B4 (LTB4; Item No. 20110) in mouse skin, as well as reduces scratching and cutaneous nerve firing induced by the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 (Item No. 16723) in mice.{53586}
Brand:CaymanSKU:30203 - 5 mgAvailable on backorder
E7046 is a specific antagonist of the type 4 prostaglandin E2 (PGE2) receptor EP4. It possesses significant antitumor growth activity in multiple preclinical tumor models through modulating myeloid cells, including tumor-associated macrophages and myeloid-derived suppressor cells.{31905} E7046 is being evaluated in cancer models and clinical trials, alone or in combination with other immunotherapeutic compounds.{31904,31906}
Brand:CaymanSKU:19673 -Available on backorder
E7046 is a specific antagonist of the type 4 prostaglandin E2 (PGE2) receptor EP4. It possesses significant antitumor growth activity in multiple preclinical tumor models through modulating myeloid cells, including tumor-associated macrophages and myeloid-derived suppressor cells.{31905} E7046 is being evaluated in cancer models and clinical trials, alone or in combination with other immunotherapeutic compounds.{31904,31906}
Brand:CaymanSKU:19673 -Available on backorder
E7046 is a specific antagonist of the type 4 prostaglandin E2 (PGE2) receptor EP4. It possesses significant antitumor growth activity in multiple preclinical tumor models through modulating myeloid cells, including tumor-associated macrophages and myeloid-derived suppressor cells.{31905} E7046 is being evaluated in cancer models and clinical trials, alone or in combination with other immunotherapeutic compounds.{31904,31906}
Brand:CaymanSKU:19673 -Available on backorder
E7046 is a specific antagonist of the type 4 prostaglandin E2 (PGE2) receptor EP4. It possesses significant antitumor growth activity in multiple preclinical tumor models through modulating myeloid cells, including tumor-associated macrophages and myeloid-derived suppressor cells.{31905} E7046 is being evaluated in cancer models and clinical trials, alone or in combination with other immunotherapeutic compounds.{31904,31906}
Brand:CaymanSKU:19673 -Available on backorder
E7449 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 1 and 1.2 nM, respectively) as well as tankyrase (TNKS) 1/2 (IC50s = 50-100 nM).{42154} It is selective for PARP1, PARP2, and TNKS1/2 over PARP3 and PARP6-15 (IC50s = >3 μM). E7449 binds to chromatin in a concentration-dependent manner and inhibits growth of DT40 cells in a PARP-dependent manner (IC50s = 3.2 and >15 μM for wild-type and PARP-/- cells, respectively). It also decreases expression of the Wnt/β-catenin signaling pathway proteins axin2, total and active β-catenin, and cyclin D1 in SW480 cells. In vivo, E7449 enhances tumor growth inhibition induced by temozolomide (TMZ; Item No. 14163) in a B16/F10 isograft model as well as antitumor activity of the DNA-crosslinking agent carboplatin (Item No. 13112) in an MX-1 mouse xenograft model. E7449 (30 and 100 mg/kg per day) inhibits tumor growth in a BRCA1 mutant MDA-MB-436 breast cancer mouse xenograft model and induces complete inhibition of tumor cell PARP activity in an NCI-H460 lung cancer mouse xenograft model when administered at a dose of 100 mg/kg. It also delays hair regrowth, a TNKS-dependent process, in mice following hair removal.
Brand:CaymanSKU:21658 -Out of stock
E7449 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 1 and 1.2 nM, respectively) as well as tankyrase (TNKS) 1/2 (IC50s = 50-100 nM).{42154} It is selective for PARP1, PARP2, and TNKS1/2 over PARP3 and PARP6-15 (IC50s = >3 μM). E7449 binds to chromatin in a concentration-dependent manner and inhibits growth of DT40 cells in a PARP-dependent manner (IC50s = 3.2 and >15 μM for wild-type and PARP-/- cells, respectively). It also decreases expression of the Wnt/β-catenin signaling pathway proteins axin2, total and active β-catenin, and cyclin D1 in SW480 cells. In vivo, E7449 enhances tumor growth inhibition induced by temozolomide (TMZ; Item No. 14163) in a B16/F10 isograft model as well as antitumor activity of the DNA-crosslinking agent carboplatin (Item No. 13112) in an MX-1 mouse xenograft model. E7449 (30 and 100 mg/kg per day) inhibits tumor growth in a BRCA1 mutant MDA-MB-436 breast cancer mouse xenograft model and induces complete inhibition of tumor cell PARP activity in an NCI-H460 lung cancer mouse xenograft model when administered at a dose of 100 mg/kg. It also delays hair regrowth, a TNKS-dependent process, in mice following hair removal.
Brand:CaymanSKU:21658 -Out of stock
E7449 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 1 and 1.2 nM, respectively) as well as tankyrase (TNKS) 1/2 (IC50s = 50-100 nM).{42154} It is selective for PARP1, PARP2, and TNKS1/2 over PARP3 and PARP6-15 (IC50s = >3 μM). E7449 binds to chromatin in a concentration-dependent manner and inhibits growth of DT40 cells in a PARP-dependent manner (IC50s = 3.2 and >15 μM for wild-type and PARP-/- cells, respectively). It also decreases expression of the Wnt/β-catenin signaling pathway proteins axin2, total and active β-catenin, and cyclin D1 in SW480 cells. In vivo, E7449 enhances tumor growth inhibition induced by temozolomide (TMZ; Item No. 14163) in a B16/F10 isograft model as well as antitumor activity of the DNA-crosslinking agent carboplatin (Item No. 13112) in an MX-1 mouse xenograft model. E7449 (30 and 100 mg/kg per day) inhibits tumor growth in a BRCA1 mutant MDA-MB-436 breast cancer mouse xenograft model and induces complete inhibition of tumor cell PARP activity in an NCI-H460 lung cancer mouse xenograft model when administered at a dose of 100 mg/kg. It also delays hair regrowth, a TNKS-dependent process, in mice following hair removal.
Brand:CaymanSKU:21658 -Out of stock
E7449 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 1 and 1.2 nM, respectively) as well as tankyrase (TNKS) 1/2 (IC50s = 50-100 nM).{42154} It is selective for PARP1, PARP2, and TNKS1/2 over PARP3 and PARP6-15 (IC50s = >3 μM). E7449 binds to chromatin in a concentration-dependent manner and inhibits growth of DT40 cells in a PARP-dependent manner (IC50s = 3.2 and >15 μM for wild-type and PARP-/- cells, respectively). It also decreases expression of the Wnt/β-catenin signaling pathway proteins axin2, total and active β-catenin, and cyclin D1 in SW480 cells. In vivo, E7449 enhances tumor growth inhibition induced by temozolomide (TMZ; Item No. 14163) in a B16/F10 isograft model as well as antitumor activity of the DNA-crosslinking agent carboplatin (Item No. 13112) in an MX-1 mouse xenograft model. E7449 (30 and 100 mg/kg per day) inhibits tumor growth in a BRCA1 mutant MDA-MB-436 breast cancer mouse xenograft model and induces complete inhibition of tumor cell PARP activity in an NCI-H460 lung cancer mouse xenograft model when administered at a dose of 100 mg/kg. It also delays hair regrowth, a TNKS-dependent process, in mice following hair removal.
Brand:CaymanSKU:21658 -Out of stock