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A-1331852 is an orally bioavailable Bcl-xL inhibitor that selectively binds Bcl-xL over Bcl-2, Mcl-1, and Bcl-W (Kis = in vitro (EC50s = 6 and >5,000 nM, respectively). A-1331852 (25 mg/kg twice per day) inhibits tumor growth in a MOLT-4 mouse xenograft model. It also inhibits tumor growth and increases the antitumor activity of docetaxel (Item No. 11637) in MDA-MB-231 LC3 metastatic breast cancer and NCI-H1650 non-small cell lung cancer mouse xenograft models when administered at a dose of 25 mg/kg. A-1331852 also increases venetoclax inhibition of tumor growth in an NCI-H1963.FP5 small cell lung cancer mouse xenograft model.
Brand:CaymanSKU:22963 - 10 mgAvailable on backorder
A-1331852 is an orally bioavailable Bcl-xL inhibitor that selectively binds Bcl-xL over Bcl-2, Mcl-1, and Bcl-W (Kis = in vitro (EC50s = 6 and >5,000 nM, respectively). A-1331852 (25 mg/kg twice per day) inhibits tumor growth in a MOLT-4 mouse xenograft model. It also inhibits tumor growth and increases the antitumor activity of docetaxel (Item No. 11637) in MDA-MB-231 LC3 metastatic breast cancer and NCI-H1650 non-small cell lung cancer mouse xenograft models when administered at a dose of 25 mg/kg. A-1331852 also increases venetoclax inhibition of tumor growth in an NCI-H1963.FP5 small cell lung cancer mouse xenograft model.
Brand:CaymanSKU:22963 - 5 mgAvailable on backorder
A-196 is a selective inhibitor of SUV420H1 and SUV420H2 (IC50s = 25 and 144 nM, respectively) that is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. A-196 has been shown to inhibit the di- and tri-methylation of lysine 20 of histone H4 (H4K20me) in multiple cell lines with IC50 values less than 1 μM. For more information on A-196 please visit the Structural Genomics Consortium (SGC). The negative control, SGC2043 (A-197), for A-196 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:-Available on backorder
A-196 is a selective inhibitor of SUV420H1 and SUV420H2 (IC50s = 25 and 144 nM, respectively) that is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. A-196 has been shown to inhibit the di- and tri-methylation of lysine 20 of histone H4 (H4K20me) in multiple cell lines with IC50 values less than 1 μM. For more information on A-196 please visit the Structural Genomics Consortium (SGC). The negative control, SGC2043 (A-197), for A-196 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:-Available on backorder
A-196 is a selective inhibitor of SUV420H1 and SUV420H2 (IC50s = 25 and 144 nM, respectively) that is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. A-196 has been shown to inhibit the di- and tri-methylation of lysine 20 of histone H4 (H4K20me) in multiple cell lines with IC50 values less than 1 μM. For more information on A-196 please visit the Structural Genomics Consortium (SGC). The negative control, SGC2043 (A-197), for A-196 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:-Available on backorder
A-205804 is a potent inhibitor of E-selectin and ICAM-1 expression in human vascular endothelial cells stimulated with TNF-α (IC50s = 20 and 25 nM, respectively).{33381} It does not block expression of VCAM-1 (IC50 > 1,000 nM).
Brand:CaymanSKU:21252 -Out of stock
A-205804 is a potent inhibitor of E-selectin and ICAM-1 expression in human vascular endothelial cells stimulated with TNF-α (IC50s = 20 and 25 nM, respectively).{33381} It does not block expression of VCAM-1 (IC50 > 1,000 nM).
Brand:CaymanSKU:21252 -Out of stock
A-205804 is a potent inhibitor of E-selectin and ICAM-1 expression in human vascular endothelial cells stimulated with TNF-α (IC50s = 20 and 25 nM, respectively).{33381} It does not block expression of VCAM-1 (IC50 > 1,000 nM).
Brand:CaymanSKU:21252 -Out of stock
A-205804 is a potent inhibitor of E-selectin and ICAM-1 expression in human vascular endothelial cells stimulated with TNF-α (IC50s = 20 and 25 nM, respectively).{33381} It does not block expression of VCAM-1 (IC50 > 1,000 nM).
Brand:CaymanSKU:21252 -Out of stock
A-317491 is a non-nucleotide antagonist of the purinergic receptors P2X3 and P2X2/3 (Kis = 22-92 nM in a calcium influx assay) that is selective over other purinergic and neurotransmitter receptors, ion channels, and enzymes (IC50s = >10 µM).{39363} It reduces thermal hyperalgesia induced by complete Freund’s adjuvant in rats (ED50 = 30 µmol/kg, s.c.) and nociceptive responses to chemically-induced pain. Chronic administration of A-317491 (30 µmol/kg, twice daily) reduces early, but not late, phase pain in a mouse model of bone cancer.{39362} A-317491 does not readily cross the blood-brain barrier and reduces pain responses when applied topically in a rat model of inflammatory pain, indicating that it acts primarily at peripheral purinergic receptors.{39364}
Brand:CaymanSKU:-Available on backorder
A-317491 is a non-nucleotide antagonist of the purinergic receptors P2X3 and P2X2/3 (Kis = 22-92 nM in a calcium influx assay) that is selective over other purinergic and neurotransmitter receptors, ion channels, and enzymes (IC50s = >10 µM).{39363} It reduces thermal hyperalgesia induced by complete Freund’s adjuvant in rats (ED50 = 30 µmol/kg, s.c.) and nociceptive responses to chemically-induced pain. Chronic administration of A-317491 (30 µmol/kg, twice daily) reduces early, but not late, phase pain in a mouse model of bone cancer.{39362} A-317491 does not readily cross the blood-brain barrier and reduces pain responses when applied topically in a rat model of inflammatory pain, indicating that it acts primarily at peripheral purinergic receptors.{39364}
Brand:CaymanSKU:-Available on backorder
A-317491 is a non-nucleotide antagonist of the purinergic receptors P2X3 and P2X2/3 (Kis = 22-92 nM in a calcium influx assay) that is selective over other purinergic and neurotransmitter receptors, ion channels, and enzymes (IC50s = >10 µM).{39363} It reduces thermal hyperalgesia induced by complete Freund’s adjuvant in rats (ED50 = 30 µmol/kg, s.c.) and nociceptive responses to chemically-induced pain. Chronic administration of A-317491 (30 µmol/kg, twice daily) reduces early, but not late, phase pain in a mouse model of bone cancer.{39362} A-317491 does not readily cross the blood-brain barrier and reduces pain responses when applied topically in a rat model of inflammatory pain, indicating that it acts primarily at peripheral purinergic receptors.{39364}
Brand:CaymanSKU:-Available on backorder
A-317491 is a non-nucleotide antagonist of the purinergic receptors P2X3 and P2X2/3 (Kis = 22-92 nM in a calcium influx assay) that is selective over other purinergic and neurotransmitter receptors, ion channels, and enzymes (IC50s = >10 µM).{39363} It reduces thermal hyperalgesia induced by complete Freund’s adjuvant in rats (ED50 = 30 µmol/kg, s.c.) and nociceptive responses to chemically-induced pain. Chronic administration of A-317491 (30 µmol/kg, twice daily) reduces early, but not late, phase pain in a mouse model of bone cancer.{39362} A-317491 does not readily cross the blood-brain barrier and reduces pain responses when applied topically in a rat model of inflammatory pain, indicating that it acts primarily at peripheral purinergic receptors.{39364}
Brand:CaymanSKU:-Available on backorder
A-366 is a potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM).{26028} It displays greater than 1,000-fold selectivity over 21 other methyltransferases.{26028} A-366 significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells without reducing total histone 3, H3K27Me3, or H3K36Me2.{26028} It also blocks the interaction of the methyl lysine reader protein Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM).{30715} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- A-366 is a potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM).{26028} It displays greater than 1,000-fold selectivity over 21 other methyltransferases.{26028} A-366 significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells without reducing total histone 3, H3K27Me3, or H3K36Me2.{26028} It also blocks the interaction of the methyl lysine reader protein Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM).{30715} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- A-366 is a potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50 = 3.3 nM).{26028} It displays greater than 1,000-fold selectivity over 21 other methyltransferases.{26028} A-366 significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells without reducing total histone 3, H3K27Me3, or H3K36Me2.{26028} It also blocks the interaction of the methyl lysine reader protein Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd = 111 nM).{30715} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-
A-39183A is an active component of the A-39183 antibiotic complex produced by aerobic fermentation of Streptomyces NRRL 12049.{38264} It has activity against penicillin-resistant S. aureus 3055 and S. faecalis X66 (MICs = 32 and 32 μg/ml, respectively) and a variety of Gram-positive and Gram-negative anaerobic bacteria (MICs = 16-128 μg/ml) in an agar dilution assay.
Brand:CaymanSKU:23239 - 1 mgAvailable on backorder
A-39183A is an active component of the A-39183 antibiotic complex produced by aerobic fermentation of Streptomyces NRRL 12049.{38264} It has activity against penicillin-resistant S. aureus 3055 and S. faecalis X66 (MICs = 32 and 32 μg/ml, respectively) and a variety of Gram-positive and Gram-negative anaerobic bacteria (MICs = 16-128 μg/ml) in an agar dilution assay.
Brand:CaymanSKU:23239 - 5 mgAvailable on backorder
A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM).{29932} A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.{29929} It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.{41984}
Brand:CaymanSKU:25605 - 1 mgAvailable on backorder
A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM).{29932} A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.{29929} It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.{41984}
Brand:CaymanSKU:25605 - 10 mgAvailable on backorder
A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM).{29932} A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.{29929} It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.{41984}
Brand:CaymanSKU:25605 - 5 mgAvailable on backorder
A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM).{29932} A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.{29929} It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.{41984}
Brand:CaymanSKU:25605 - 500 µgAvailable on backorder
A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM).{29932} A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.{29929} It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.{41984}
Brand:CaymanSKU:-Available on backorder
A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM).{29932} A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.{29929} It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.{41984}
Brand:CaymanSKU:-Available on backorder
A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM).{29932} A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.{29929} It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.{41984}
Brand:CaymanSKU:-Available on backorder
A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, 50 = 3,000 nM) and PKC (IC50 = >33 μM).{29932} A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.{29929} It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.{41984}
Brand:CaymanSKU:-Available on backorder
A-438079 is a competitive antagonist of the nucleotide receptor P2X7 (pIC50 = 6.9).{22914} It inhibits both calcium flux and IL-1β release mediated by P2X7 while not affecting the activity of other P2X receptors.{22914,22913} A-438079 is effective in evaluating the role of P2X7 in nociception, oxidative stress, and apoptosis in cells and animals.{22915,22916,22917}
Brand:CaymanSKU:- A-438079 is a competitive antagonist of the nucleotide receptor P2X7 (pIC50 = 6.9).{22914} It inhibits both calcium flux and IL-1β release mediated by P2X7 while not affecting the activity of other P2X receptors.{22914,22913} A-438079 is effective in evaluating the role of P2X7 in nociception, oxidative stress, and apoptosis in cells and animals.{22915,22916,22917}
Brand:CaymanSKU:- A-438079 is a competitive antagonist of the nucleotide receptor P2X7 (pIC50 = 6.9).{22914} It inhibits both calcium flux and IL-1β release mediated by P2X7 while not affecting the activity of other P2X receptors.{22914,22913} A-438079 is effective in evaluating the role of P2X7 in nociception, oxidative stress, and apoptosis in cells and animals.{22915,22916,22917}
Brand:CaymanSKU:- A-438079 is a competitive antagonist of the nucleotide receptor P2X7 (pIC50 = 6.9).{22914} It inhibits both calcium flux and IL-1β release mediated by P2X7 while not affecting the activity of other P2X receptors.{22914,22913} A-438079 is effective in evaluating the role of P2X7 in nociception, oxidative stress, and apoptosis in cells and animals.{22915,22916,22917}
Brand:CaymanSKU:-
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis. A-443654 is an inhibitor of Akt (Ki = 160 pmol/L for all three isoforms) that interferes with mitotic progression and bipolar spindle formation.{26942,26944} It induces G2/M accumulation, defects in centrosome separation, and formation of either monopolar arrays or disorganized spindles.{26944} A-443654 has been reported to slow the progression of Akt-dependent tumors in in vivo mouse models.{26942} In response to an A-443654-induced decrease in phosphorylation of Akt targets, a concomitant increase in Thr308 and Ser473 phosphorylation of Akt has been observed in human cancer cell lines.{26943} A-443654 has been used to examine the mechanism of this rapid feedback reaction.
Brand:CaymanSKU:-Out of stock
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis. A-443654 is an inhibitor of Akt (Ki = 160 pmol/L for all three isoforms) that interferes with mitotic progression and bipolar spindle formation.{26942,26944} It induces G2/M accumulation, defects in centrosome separation, and formation of either monopolar arrays or disorganized spindles.{26944} A-443654 has been reported to slow the progression of Akt-dependent tumors in in vivo mouse models.{26942} In response to an A-443654-induced decrease in phosphorylation of Akt targets, a concomitant increase in Thr308 and Ser473 phosphorylation of Akt has been observed in human cancer cell lines.{26943} A-443654 has been used to examine the mechanism of this rapid feedback reaction.
Brand:CaymanSKU:-Out of stock
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis. A-443654 is an inhibitor of Akt (Ki = 160 pmol/L for all three isoforms) that interferes with mitotic progression and bipolar spindle formation.{26942,26944} It induces G2/M accumulation, defects in centrosome separation, and formation of either monopolar arrays or disorganized spindles.{26944} A-443654 has been reported to slow the progression of Akt-dependent tumors in in vivo mouse models.{26942} In response to an A-443654-induced decrease in phosphorylation of Akt targets, a concomitant increase in Thr308 and Ser473 phosphorylation of Akt has been observed in human cancer cell lines.{26943} A-443654 has been used to examine the mechanism of this rapid feedback reaction.
Brand:CaymanSKU:-Out of stock
A-484954 is an ATP-competitive inhibitor of eukaryotic elongation factor-2 kinase (eEF-2K; IC50 = 420 nM).{51146} It reduces eEF-2K autophosphorylation in PC3, HeLa, H460, H1299, and MDA-MB-231 cancer cells when used at a concentration of 75 μM.
Brand:CaymanSKU:28279 - 1 mgAvailable on backorder
A-484954 is an ATP-competitive inhibitor of eukaryotic elongation factor-2 kinase (eEF-2K; IC50 = 420 nM).{51146} It reduces eEF-2K autophosphorylation in PC3, HeLa, H460, H1299, and MDA-MB-231 cancer cells when used at a concentration of 75 μM.
Brand:CaymanSKU:28279 - 10 mgAvailable on backorder
A-484954 is an ATP-competitive inhibitor of eukaryotic elongation factor-2 kinase (eEF-2K; IC50 = 420 nM).{51146} It reduces eEF-2K autophosphorylation in PC3, HeLa, H460, H1299, and MDA-MB-231 cancer cells when used at a concentration of 75 μM.
Brand:CaymanSKU:28279 - 25 mgAvailable on backorder
A-484954 is an ATP-competitive inhibitor of eukaryotic elongation factor-2 kinase (eEF-2K; IC50 = 420 nM).{51146} It reduces eEF-2K autophosphorylation in PC3, HeLa, H460, H1299, and MDA-MB-231 cancer cells when used at a concentration of 75 μM.
Brand:CaymanSKU:28279 - 5 mgAvailable on backorder
A-485 is an inhibitor of the histone acetyltransferase p300/CBP (IC50 = 60 nM).{40422} It decreases acetylated histone H3 lysine 27 (H3K27Ac), but not H3K9Ac, levels in PC3 cells in a concentration-dependent manner. A-485 reduces proliferation of non-small cell lung cancer (NSCLC), small cell lung cancer, triple-negative breast cancer, mantel cell lymphoma, multiple myeloma, non-Hodgkin’s, and acute myeloid leukemia cell lines. It inhibits expression of prostate specific antigen (PSA) and H3K27Ac occupancy at the PSA enhancer without inhibiting androgen receptor occupancy in LNCaP-FGC cells. A-485 reduces tumor volume in a LuCaP-77 mouse xenograft model of castration-resistant prostate cancer when administered at a dose of 100 mg twice per day for 21 days.
Brand:CaymanSKU:24119 - 1 mgAvailable on backorder
A-485 is an inhibitor of the histone acetyltransferase p300/CBP (IC50 = 60 nM).{40422} It decreases acetylated histone H3 lysine 27 (H3K27Ac), but not H3K9Ac, levels in PC3 cells in a concentration-dependent manner. A-485 reduces proliferation of non-small cell lung cancer (NSCLC), small cell lung cancer, triple-negative breast cancer, mantel cell lymphoma, multiple myeloma, non-Hodgkin’s, and acute myeloid leukemia cell lines. It inhibits expression of prostate specific antigen (PSA) and H3K27Ac occupancy at the PSA enhancer without inhibiting androgen receptor occupancy in LNCaP-FGC cells. A-485 reduces tumor volume in a LuCaP-77 mouse xenograft model of castration-resistant prostate cancer when administered at a dose of 100 mg twice per day for 21 days.
Brand:CaymanSKU:24119 - 10 mgAvailable on backorder
A-485 is an inhibitor of the histone acetyltransferase p300/CBP (IC50 = 60 nM).{40422} It decreases acetylated histone H3 lysine 27 (H3K27Ac), but not H3K9Ac, levels in PC3 cells in a concentration-dependent manner. A-485 reduces proliferation of non-small cell lung cancer (NSCLC), small cell lung cancer, triple-negative breast cancer, mantel cell lymphoma, multiple myeloma, non-Hodgkin’s, and acute myeloid leukemia cell lines. It inhibits expression of prostate specific antigen (PSA) and H3K27Ac occupancy at the PSA enhancer without inhibiting androgen receptor occupancy in LNCaP-FGC cells. A-485 reduces tumor volume in a LuCaP-77 mouse xenograft model of castration-resistant prostate cancer when administered at a dose of 100 mg twice per day for 21 days.
Brand:CaymanSKU:24119 - 25 mgAvailable on backorder
A-485 is an inhibitor of the histone acetyltransferase p300/CBP (IC50 = 60 nM).{40422} It decreases acetylated histone H3 lysine 27 (H3K27Ac), but not H3K9Ac, levels in PC3 cells in a concentration-dependent manner. A-485 reduces proliferation of non-small cell lung cancer (NSCLC), small cell lung cancer, triple-negative breast cancer, mantel cell lymphoma, multiple myeloma, non-Hodgkin’s, and acute myeloid leukemia cell lines. It inhibits expression of prostate specific antigen (PSA) and H3K27Ac occupancy at the PSA enhancer without inhibiting androgen receptor occupancy in LNCaP-FGC cells. A-485 reduces tumor volume in a LuCaP-77 mouse xenograft model of castration-resistant prostate cancer when administered at a dose of 100 mg twice per day for 21 days.
Brand:CaymanSKU:24119 - 5 mgAvailable on backorder
A-54556A is a natural acyldepsipeptide (ADEP) antibiotic isolated from the fermentation broth of S. hawaiiensis.{24688} Like other ADEP antibiotics, A-54556A binds to the ATP-dependent Clp protease proteolytic subunit ClpP, resulting in constitutive activation of this bacterial protease.{27768,27766,27765} This leads to uncontrolled proteolysis, inhibition of bacterial cell division, and, ultimately, cell death.{24688,27767} A-54556A preferentially targets Gram-positive bacteria, including staphylococci, streptococci, and enterococci, with minimum inhibitory concentration values in the submicrogram/milliliter range.{27767} ADEP antibiotics are effective against chronic infections as they are able to eradicate chronic biofilm infections, particularly when combined with rifampicin.{24689}
Brand:CaymanSKU:- A-54556A is a natural acyldepsipeptide (ADEP) antibiotic isolated from the fermentation broth of S. hawaiiensis.{24688} Like other ADEP antibiotics, A-54556A binds to the ATP-dependent Clp protease proteolytic subunit ClpP, resulting in constitutive activation of this bacterial protease.{27768,27766,27765} This leads to uncontrolled proteolysis, inhibition of bacterial cell division, and, ultimately, cell death.{24688,27767} A-54556A preferentially targets Gram-positive bacteria, including staphylococci, streptococci, and enterococci, with minimum inhibitory concentration values in the submicrogram/milliliter range.{27767} ADEP antibiotics are effective against chronic infections as they are able to eradicate chronic biofilm infections, particularly when combined with rifampicin.{24689}
Brand:CaymanSKU:-
A-54556B is a natural acyldepsipeptide (ADEP) antibiotic isolated from the fermentation broth of S. hawaiiensis.{27771} Like the closely related ADEP, A-54556A (Item No. 15305), A-54556B is effective against Gram-positive bacteria, including penicillin-resistant S. aureus.{27771} A-54556B is also effective against many strains of anaerobic bacteria.{27771}
Brand:CaymanSKU:-Out of stock
A-54556B is a natural acyldepsipeptide (ADEP) antibiotic isolated from the fermentation broth of S. hawaiiensis.{27771} Like the closely related ADEP, A-54556A (Item No. 15305), A-54556B is effective against Gram-positive bacteria, including penicillin-resistant S. aureus.{27771} A-54556B is also effective against many strains of anaerobic bacteria.{27771}
Brand:CaymanSKU:-Out of stock
The α1-adrenergic receptors are Gq protein-coupled receptors that play a key role in the modulation of sympathetic nervous system activity and are the site of action for therapeutic agents, such as antihypertensive drugs. A-61603 is a selective α1A-adrenergic receptor agonist that is at least 35-fold more potent at α1A receptor sites than at α1B or α1D.{28349} Activation of the α1A-adrenergic receptor by A-61603 has been reported to increase the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro (EC50 = 6.9 nM) much more potently than activation by phenylephrine (Item No. 17205; EC50 = 2.3 µM).{28350}
Brand:CaymanSKU:-Available on backorder
The α1-adrenergic receptors are Gq protein-coupled receptors that play a key role in the modulation of sympathetic nervous system activity and are the site of action for therapeutic agents, such as antihypertensive drugs. A-61603 is a selective α1A-adrenergic receptor agonist that is at least 35-fold more potent at α1A receptor sites than at α1B or α1D.{28349} Activation of the α1A-adrenergic receptor by A-61603 has been reported to increase the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro (EC50 = 6.9 nM) much more potently than activation by phenylephrine (Item No. 17205; EC50 = 2.3 µM).{28350}
Brand:CaymanSKU:-Available on backorder
The α1-adrenergic receptors are Gq protein-coupled receptors that play a key role in the modulation of sympathetic nervous system activity and are the site of action for therapeutic agents, such as antihypertensive drugs. A-61603 is a selective α1A-adrenergic receptor agonist that is at least 35-fold more potent at α1A receptor sites than at α1B or α1D.{28349} Activation of the α1A-adrenergic receptor by A-61603 has been reported to increase the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro (EC50 = 6.9 nM) much more potently than activation by phenylephrine (Item No. 17205; EC50 = 2.3 µM).{28350}
Brand:CaymanSKU:-Available on backorder
A-66 is a potent, selective inhibitor of the PI3K isoform p110α (IC50 = 32 nM in a cell-free assay).{32579} It displays over 100-fold selectivity for p110α over other isoforms. A-66 is effective in vivo, suppressing the growth of SK-OV-3 tumor xenografts in mice.{32579} It also impairs all measures of in vivo insulin action in mice.{32580} A-66 partially suppresses B cell receptor-dependent Akt activation and proliferation.{31648}
Brand:CaymanSKU:-Available on backorder
A-66 is a potent, selective inhibitor of the PI3K isoform p110α (IC50 = 32 nM in a cell-free assay).{32579} It displays over 100-fold selectivity for p110α over other isoforms. A-66 is effective in vivo, suppressing the growth of SK-OV-3 tumor xenografts in mice.{32579} It also impairs all measures of in vivo insulin action in mice.{32580} A-66 partially suppresses B cell receptor-dependent Akt activation and proliferation.{31648}
Brand:CaymanSKU:-Available on backorder
A-66 is a potent, selective inhibitor of the PI3K isoform p110α (IC50 = 32 nM in a cell-free assay).{32579} It displays over 100-fold selectivity for p110α over other isoforms. A-66 is effective in vivo, suppressing the growth of SK-OV-3 tumor xenografts in mice.{32579} It also impairs all measures of in vivo insulin action in mice.{32580} A-66 partially suppresses B cell receptor-dependent Akt activation and proliferation.{31648}
Brand:CaymanSKU:-Available on backorder
A-66 is a potent, selective inhibitor of the PI3K isoform p110α (IC50 = 32 nM in a cell-free assay).{32579} It displays over 100-fold selectivity for p110α over other isoforms. A-66 is effective in vivo, suppressing the growth of SK-OV-3 tumor xenografts in mice.{32579} It also impairs all measures of in vivo insulin action in mice.{32580} A-66 partially suppresses B cell receptor-dependent Akt activation and proliferation.{31648}
Brand:CaymanSKU:-Available on backorder
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival, as well as angiogenesis. A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki = 11 nM for Akt1).{26942} It shows inhibitory activity against PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively, but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families.{26942} A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4 µM.{26942} In vivo, 40 mg/kg/day A-674563 in combination with 15 mg/kg/day paclitaxel (Item No. 10461) was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model.{26942}
Brand:CaymanSKU:-Available on backorder
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival, as well as angiogenesis. A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki = 11 nM for Akt1).{26942} It shows inhibitory activity against PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively, but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families.{26942} A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4 µM.{26942} In vivo, 40 mg/kg/day A-674563 in combination with 15 mg/kg/day paclitaxel (Item No. 10461) was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model.{26942}
Brand:CaymanSKU:-Available on backorder
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival, as well as angiogenesis. A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki = 11 nM for Akt1).{26942} It shows inhibitory activity against PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively, but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families.{26942} A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4 µM.{26942} In vivo, 40 mg/kg/day A-674563 in combination with 15 mg/kg/day paclitaxel (Item No. 10461) was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model.{26942}
Brand:CaymanSKU:-Available on backorder
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival, as well as angiogenesis. A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki = 11 nM for Akt1).{26942} It shows inhibitory activity against PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively, but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families.{26942} A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4 µM.{26942} In vivo, 40 mg/kg/day A-674563 in combination with 15 mg/kg/day paclitaxel (Item No. 10461) was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model.{26942}
Brand:CaymanSKU:-Available on backorder
Calmodulin is a calcium-dependent protein that regulates the activity of a diverse array of enzymes, ion channels, and other proteins and thus has diverse roles in cell function.{23723,23722} A-7 is an analog of the napthalenesulfonamide W-7 (Item No. 14826) that has an acyl chain length of 10 carbons, rather than six. It is a potent cell-permeable antagonist of calmodulin that inhibits Ca2+/calmodulin cyclic nucleotide phosphodiesterase more potently than W-7 (IC50 = 3.2 and 26 µM, respectively).{26195,26194}
Brand:CaymanSKU:- Calmodulin is a calcium-dependent protein that regulates the activity of a diverse array of enzymes, ion channels, and other proteins and thus has diverse roles in cell function.{23723,23722} A-7 is an analog of the napthalenesulfonamide W-7 (Item No. 14826) that has an acyl chain length of 10 carbons, rather than six. It is a potent cell-permeable antagonist of calmodulin that inhibits Ca2+/calmodulin cyclic nucleotide phosphodiesterase more potently than W-7 (IC50 = 3.2 and 26 µM, respectively).{26195,26194}
Brand:CaymanSKU:- Calmodulin is a calcium-dependent protein that regulates the activity of a diverse array of enzymes, ion channels, and other proteins and thus has diverse roles in cell function.{23723,23722} A-7 is an analog of the napthalenesulfonamide W-7 (Item No. 14826) that has an acyl chain length of 10 carbons, rather than six. It is a potent cell-permeable antagonist of calmodulin that inhibits Ca2+/calmodulin cyclic nucleotide phosphodiesterase more potently than W-7 (IC50 = 3.2 and 26 µM, respectively).{26195,26194}
Brand:CaymanSKU:-
A-740003 is a competitive antagonist of the ATP-gated ionotropic P2X7 receptor (IC50s = 40 and 18 nM for human and rat receptors, respectively).{33388} It shows weak or no activity at other P2 receptors and other receptors and ion channels. A-740003 blocks agonist-induced IL-1β release and pore formation in differentiated THP-1 cells (IC50s = 156 and 92 nM, respectively).{33388} It is effective in vivo when administered intraperitoneally, reducing pain in several animal models.{33388} A-740003 is used in cell and animal studies to elucidate P2X7 roles and signaling pathways.{22913,33386,33387}
Brand:CaymanSKU:21256 -Out of stock
A-740003 is a competitive antagonist of the ATP-gated ionotropic P2X7 receptor (IC50s = 40 and 18 nM for human and rat receptors, respectively).{33388} It shows weak or no activity at other P2 receptors and other receptors and ion channels. A-740003 blocks agonist-induced IL-1β release and pore formation in differentiated THP-1 cells (IC50s = 156 and 92 nM, respectively).{33388} It is effective in vivo when administered intraperitoneally, reducing pain in several animal models.{33388} A-740003 is used in cell and animal studies to elucidate P2X7 roles and signaling pathways.{22913,33386,33387}
Brand:CaymanSKU:21256 -Out of stock
A-740003 is a competitive antagonist of the ATP-gated ionotropic P2X7 receptor (IC50s = 40 and 18 nM for human and rat receptors, respectively).{33388} It shows weak or no activity at other P2 receptors and other receptors and ion channels. A-740003 blocks agonist-induced IL-1β release and pore formation in differentiated THP-1 cells (IC50s = 156 and 92 nM, respectively).{33388} It is effective in vivo when administered intraperitoneally, reducing pain in several animal models.{33388} A-740003 is used in cell and animal studies to elucidate P2X7 roles and signaling pathways.{22913,33386,33387}
Brand:CaymanSKU:21256 -Out of stock
A-740003 is a competitive antagonist of the ATP-gated ionotropic P2X7 receptor (IC50s = 40 and 18 nM for human and rat receptors, respectively).{33388} It shows weak or no activity at other P2 receptors and other receptors and ion channels. A-740003 blocks agonist-induced IL-1β release and pore formation in differentiated THP-1 cells (IC50s = 156 and 92 nM, respectively).{33388} It is effective in vivo when administered intraperitoneally, reducing pain in several animal models.{33388} A-740003 is used in cell and animal studies to elucidate P2X7 roles and signaling pathways.{22913,33386,33387}
Brand:CaymanSKU:21256 -Out of stock
A-769662 is a small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172.{22445,22447} A-769662 specifically activates β1 subunit-containing AMPK heterotrimers, and its effects are independent of kinases upstream of AMPK.{22445,22448} A-769662 has been used to stimulate CYP450-mediated fatty acid oxidation, inhibit adipocyte differentiation, explore glucose uptake in skeletal muscle, and promote endothelial cell survival during metabolic stress.{22448,22444,22450,22449,22446}
Brand:CaymanSKU:11900 - 10 mgAvailable on backorder
A-769662 is a small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172.{22445,22447} A-769662 specifically activates β1 subunit-containing AMPK heterotrimers, and its effects are independent of kinases upstream of AMPK.{22445,22448} A-769662 has been used to stimulate CYP450-mediated fatty acid oxidation, inhibit adipocyte differentiation, explore glucose uptake in skeletal muscle, and promote endothelial cell survival during metabolic stress.{22448,22444,22450,22449,22446}
Brand:CaymanSKU:11900 - 5 mgAvailable on backorder
A-769662 is a small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172.{22445,22447} A-769662 specifically activates β1 subunit-containing AMPK heterotrimers, and its effects are independent of kinases upstream of AMPK.{22445,22448} A-769662 has been used to stimulate CYP450-mediated fatty acid oxidation, inhibit adipocyte differentiation, explore glucose uptake in skeletal muscle, and promote endothelial cell survival during metabolic stress.{22448,22444,22450,22449,22446}
Brand:CaymanSKU:11900 - 50 mgAvailable on backorder
A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC50 = 25 nM).{31358} It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells.{31358} It completely blocks phosphorylation of SMAD2 by TGF-β in human keratinocyte HaCaT cells at 1 µM. A-77-01 prevents morphological and gene expression changes characteristic of epithelial-to-mesenchymal transition in NMuMG cells treated with TGF-β.{31358}
Brand:CaymanSKU:-Available on backorder
A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC50 = 25 nM).{31358} It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells.{31358} It completely blocks phosphorylation of SMAD2 by TGF-β in human keratinocyte HaCaT cells at 1 µM. A-77-01 prevents morphological and gene expression changes characteristic of epithelial-to-mesenchymal transition in NMuMG cells treated with TGF-β.{31358}
Brand:CaymanSKU:-Available on backorder
A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC50 = 25 nM).{31358} It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells.{31358} It completely blocks phosphorylation of SMAD2 by TGF-β in human keratinocyte HaCaT cells at 1 µM. A-77-01 prevents morphological and gene expression changes characteristic of epithelial-to-mesenchymal transition in NMuMG cells treated with TGF-β.{31358}
Brand:CaymanSKU:-Available on backorder
A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC50 = 25 nM).{31358} It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells.{31358} It completely blocks phosphorylation of SMAD2 by TGF-β in human keratinocyte HaCaT cells at 1 µM. A-77-01 prevents morphological and gene expression changes characteristic of epithelial-to-mesenchymal transition in NMuMG cells treated with TGF-β.{31358}
Brand:CaymanSKU:-Available on backorder
A-771726 is the active metabolite of leflunomide, a prodrug approved by the FDA for treatment of rheumatoid arthritis. A-771726 reversibly inhibits dihydroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines. It prevents activated lymphocytes from accumulating sufficient pyrimidines to support DNA synthesis (IC50s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively).{22723} At higher doses, A-771726 inhibits tyrosine kinases responsible for early T cell and B cell signaling in the G0/G1 phase of the cell cycle.{22723} A-771726 has also been shown to inhibit the production of prostaglandin E2 in synoviocytes activated by TNF-α and IL-1α (IC50s = 7 and 3 μM, respectively) as well as inhibit MMP-1 and IL-6 production at concentrations >10 μM.{22722}
Brand:CaymanSKU:- A-771726 is the active metabolite of leflunomide, a prodrug approved by the FDA for treatment of rheumatoid arthritis. A-771726 reversibly inhibits dihydroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines. It prevents activated lymphocytes from accumulating sufficient pyrimidines to support DNA synthesis (IC50s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively).{22723} At higher doses, A-771726 inhibits tyrosine kinases responsible for early T cell and B cell signaling in the G0/G1 phase of the cell cycle.{22723} A-771726 has also been shown to inhibit the production of prostaglandin E2 in synoviocytes activated by TNF-α and IL-1α (IC50s = 7 and 3 μM, respectively) as well as inhibit MMP-1 and IL-6 production at concentrations >10 μM.{22722}
Brand:CaymanSKU:- A-771726 is the active metabolite of leflunomide, a prodrug approved by the FDA for treatment of rheumatoid arthritis. A-771726 reversibly inhibits dihydroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines. It prevents activated lymphocytes from accumulating sufficient pyrimidines to support DNA synthesis (IC50s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively).{22723} At higher doses, A-771726 inhibits tyrosine kinases responsible for early T cell and B cell signaling in the G0/G1 phase of the cell cycle.{22723} A-771726 has also been shown to inhibit the production of prostaglandin E2 in synoviocytes activated by TNF-α and IL-1α (IC50s = 7 and 3 μM, respectively) as well as inhibit MMP-1 and IL-6 production at concentrations >10 μM.{22722}
Brand:CaymanSKU:-
A-77636 is a dopamine D1 receptor agonist (Ki = 40 nM).{40976} It induces activity equal to or greater than dopamine (Item No. 21992) in an adenylate cyclase assay of D1 receptor activity in fish retina and rat caudate putamen (EC50s = 7.4 and 1.1 nM, respectively) but does not show agonist activity at D2 receptors expressed in MMQ cells when used at concentrations up to 10 μM. A-77636 (10 μM) induces desensitization of dopamine-stimulated cAMP accumulation and downregulation of D1 receptors, reducing D1 receptor expression by 79% in C-6 glioma cells expressing monkey D1A receptors.{40977} In a marmoset model of Parkinson’s disease induced by MPTP, A-77636 (3 μmol/kg, s.c.) increases locomotor activity 5.3-fold and reduces disease severity.{40976} Subcutaneous administration of A-77636 elicits cortical acetylcholine release at a dose of 1 μmol/kg.{40978} It also elicits over a 230% increase in cortical and hippocampal acetylcholine release when administered at a dose of 4 μmol/kg, an effect that is blocked by the D1 antagonist SCH 23390 (Item No. 15631).
Brand:CaymanSKU:24316 - 1 mgAvailable on backorder
A-77636 is a dopamine D1 receptor agonist (Ki = 40 nM).{40976} It induces activity equal to or greater than dopamine (Item No. 21992) in an adenylate cyclase assay of D1 receptor activity in fish retina and rat caudate putamen (EC50s = 7.4 and 1.1 nM, respectively) but does not show agonist activity at D2 receptors expressed in MMQ cells when used at concentrations up to 10 μM. A-77636 (10 μM) induces desensitization of dopamine-stimulated cAMP accumulation and downregulation of D1 receptors, reducing D1 receptor expression by 79% in C-6 glioma cells expressing monkey D1A receptors.{40977} In a marmoset model of Parkinson’s disease induced by MPTP, A-77636 (3 μmol/kg, s.c.) increases locomotor activity 5.3-fold and reduces disease severity.{40976} Subcutaneous administration of A-77636 elicits cortical acetylcholine release at a dose of 1 μmol/kg.{40978} It also elicits over a 230% increase in cortical and hippocampal acetylcholine release when administered at a dose of 4 μmol/kg, an effect that is blocked by the D1 antagonist SCH 23390 (Item No. 15631).
Brand:CaymanSKU:24316 - 10 mgAvailable on backorder
A-77636 is a dopamine D1 receptor agonist (Ki = 40 nM).{40976} It induces activity equal to or greater than dopamine (Item No. 21992) in an adenylate cyclase assay of D1 receptor activity in fish retina and rat caudate putamen (EC50s = 7.4 and 1.1 nM, respectively) but does not show agonist activity at D2 receptors expressed in MMQ cells when used at concentrations up to 10 μM. A-77636 (10 μM) induces desensitization of dopamine-stimulated cAMP accumulation and downregulation of D1 receptors, reducing D1 receptor expression by 79% in C-6 glioma cells expressing monkey D1A receptors.{40977} In a marmoset model of Parkinson’s disease induced by MPTP, A-77636 (3 μmol/kg, s.c.) increases locomotor activity 5.3-fold and reduces disease severity.{40976} Subcutaneous administration of A-77636 elicits cortical acetylcholine release at a dose of 1 μmol/kg.{40978} It also elicits over a 230% increase in cortical and hippocampal acetylcholine release when administered at a dose of 4 μmol/kg, an effect that is blocked by the D1 antagonist SCH 23390 (Item No. 15631).
Brand:CaymanSKU:24316 - 5 mgAvailable on backorder
A-796260 is a synthetic cannabinoid (CB) that shows high selectivity for the CB2 receptor (Ki = 0.77 nM) over the CB1 receptor (Ki = 2,100 nM).{21031} It also shows efficacy in vivo in models of inflammatory, post-operative, neuropathic, and osteoarthritic pain, activities which are selectively blocked by CB2 receptor-selective antagonists.{21542} This product is intended for research and forensic uses.
Brand:CaymanSKU:11606 - 1 mgAvailable on backorder
A-796260 is a synthetic cannabinoid (CB) that shows high selectivity for the CB2 receptor (Ki = 0.77 nM) over the CB1 receptor (Ki = 2,100 nM).{21031} It also shows efficacy in vivo in models of inflammatory, post-operative, neuropathic, and osteoarthritic pain, activities which are selectively blocked by CB2 receptor-selective antagonists.{21542} This product is intended for research and forensic uses.
Brand:CaymanSKU:11606 - 10 mgAvailable on backorder
A-796260 is a synthetic cannabinoid (CB) that shows high selectivity for the CB2 receptor (Ki = 0.77 nM) over the CB1 receptor (Ki = 2,100 nM).{21031} It also shows efficacy in vivo in models of inflammatory, post-operative, neuropathic, and osteoarthritic pain, activities which are selectively blocked by CB2 receptor-selective antagonists.{21542} This product is intended for research and forensic uses.
Brand:CaymanSKU:11606 - 5 mgAvailable on backorder
A-796260 (Item No. 11606) is a synthetic cannabinoid (CB) that shows high selectivity for the CB2 receptor (Ki = 0.77 nM) over the CB1 receptor (Ki = 2,100 nM).{21031} It also shows efficacy in vivo in models of inflammatory, post-operative, neuropathic, and osteoarthritic pain, activities which are selectively blocked by CB2 receptor-selective antagonists.{21542} A-796260 degradant is an impurity that may be produced in the synthesis of A-796260. The physiological and toxicological properties of this compound are not known. This product is intended for forensic and research applications.
Brand:CaymanSKU:-Available on backorder
A-796260 (Item No. 11606) is a synthetic cannabinoid (CB) that shows high selectivity for the CB2 receptor (Ki = 0.77 nM) over the CB1 receptor (Ki = 2,100 nM).{21031} It also shows efficacy in vivo in models of inflammatory, post-operative, neuropathic, and osteoarthritic pain, activities which are selectively blocked by CB2 receptor-selective antagonists.{21542} A-796260 degradant is an impurity that may be produced in the synthesis of A-796260. The physiological and toxicological properties of this compound are not known. This product is intended for forensic and research applications.
Brand:CaymanSKU:-Available on backorder