Cayman
Showing 29701–29850 of 45550 results
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The Ras family of GTPases, including the Arf, Rho, Ras, and Rab GTPase subfamilies, regulates various cellular processes ranging from membrane trafficking to the control of cell proliferation. They regulate cell physiology by switching between active and inactive conformational states by binding either GTP or GDP. Alterations in GTPase function are a known hallmark of certain cancers and genetic diseases. ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM) that demonstrates selectivity against the related GTPases cdc42, Ras, Rab-2A, and Rac1 (EC50s = 588.8, 346.7, 158.5, and 794.3 nM, respectively).{24525} It has been shown to function by increasing the affinity of the GTPase for guanine nucleotides.{24525}
Brand:CaymanSKU:- The Ras family of GTPases, including the Arf, Rho, Ras, and Rab GTPase subfamilies, regulates various cellular processes ranging from membrane trafficking to the control of cell proliferation. They regulate cell physiology by switching between active and inactive conformational states by binding either GTP or GDP. Alterations in GTPase function are a known hallmark of certain cancers and genetic diseases. ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM) that demonstrates selectivity against the related GTPases cdc42, Ras, Rab-2A, and Rac1 (EC50s = 588.8, 346.7, 158.5, and 794.3 nM, respectively).{24525} It has been shown to function by increasing the affinity of the GTPase for guanine nucleotides.{24525}
Brand:CaymanSKU:- The Ras family of GTPases, including the Arf, Rho, Ras, and Rab GTPase subfamilies, regulates various cellular processes ranging from membrane trafficking to the control of cell proliferation. They regulate cell physiology by switching between active and inactive conformational states by binding either GTP or GDP. Alterations in GTPase function are a known hallmark of certain cancers and genetic diseases. ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM) that demonstrates selectivity against the related GTPases cdc42, Ras, Rab-2A, and Rac1 (EC50s = 588.8, 346.7, 158.5, and 794.3 nM, respectively).{24525} It has been shown to function by increasing the affinity of the GTPase for guanine nucleotides.{24525}
Brand:CaymanSKU:- The Ras family of GTPases, including the Arf, Rho, Ras, and Rab GTPase subfamilies, regulates various cellular processes ranging from membrane trafficking to the control of cell proliferation. They regulate cell physiology by switching between active and inactive conformational states by binding either GTP or GDP. Alterations in GTPase function are a known hallmark of certain cancers and genetic diseases. ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM) that demonstrates selectivity against the related GTPases cdc42, Ras, Rab-2A, and Rac1 (EC50s = 588.8, 346.7, 158.5, and 794.3 nM, respectively).{24525} It has been shown to function by increasing the affinity of the GTPase for guanine nucleotides.{24525}
Brand:CaymanSKU:-
ML-099 is a small molecule pan activator of Ras-related GTPases, activating Rac1, cell division cycle 42, Ras, and Rab-2A with EC50 values of 20, 100, 141, and 355 nM, respectively.{24525}
Brand:CaymanSKU:- ML-099 is a small molecule pan activator of Ras-related GTPases, activating Rac1, cell division cycle 42, Ras, and Rab-2A with EC50 values of 20, 100, 141, and 355 nM, respectively.{24525}
Brand:CaymanSKU:- ML-099 is a small molecule pan activator of Ras-related GTPases, activating Rac1, cell division cycle 42, Ras, and Rab-2A with EC50 values of 20, 100, 141, and 355 nM, respectively.{24525}
Brand:CaymanSKU:- ML-099 is a small molecule pan activator of Ras-related GTPases, activating Rac1, cell division cycle 42, Ras, and Rab-2A with EC50 values of 20, 100, 141, and 355 nM, respectively.{24525}
Brand:CaymanSKU:-
ML-133 is an inward-rectifier potassium channel 2 (Kir2) inhibitor (IC50s = 1.8, 2.8, 2,9, and 2.6 µM for Kir2.1, Kir2.2, Kir2.3, and Kir2.6, respectively).{61043} It is selective for Kir2 channels over Kir1.1 and Kir4.1 channels (IC50s = 33 and 76 µM, respectively). ML-133 (10 and 30 nmol/animal) prevents the development of dynamic, but not punctate, mechanical allodynia in a mouse model of spared nerve injury.{61040}
Brand:CaymanSKU:31232 - 10 mgAvailable on backorder
ML-133 is an inward-rectifier potassium channel 2 (Kir2) inhibitor (IC50s = 1.8, 2.8, 2,9, and 2.6 µM for Kir2.1, Kir2.2, Kir2.3, and Kir2.6, respectively).{61043} It is selective for Kir2 channels over Kir1.1 and Kir4.1 channels (IC50s = 33 and 76 µM, respectively). ML-133 (10 and 30 nmol/animal) prevents the development of dynamic, but not punctate, mechanical allodynia in a mouse model of spared nerve injury.{61040}
Brand:CaymanSKU:31232 - 25 mgAvailable on backorder
ML-133 is an inward-rectifier potassium channel 2 (Kir2) inhibitor (IC50s = 1.8, 2.8, 2,9, and 2.6 µM for Kir2.1, Kir2.2, Kir2.3, and Kir2.6, respectively).{61043} It is selective for Kir2 channels over Kir1.1 and Kir4.1 channels (IC50s = 33 and 76 µM, respectively). ML-133 (10 and 30 nmol/animal) prevents the development of dynamic, but not punctate, mechanical allodynia in a mouse model of spared nerve injury.{61040}
Brand:CaymanSKU:31232 - 5 mgAvailable on backorder
ML-133 is an inward-rectifier potassium channel 2 (Kir2) inhibitor (IC50s = 1.8, 2.8, 2,9, and 2.6 µM for Kir2.1, Kir2.2, Kir2.3, and Kir2.6, respectively).{61043} It is selective for Kir2 channels over Kir1.1 and Kir4.1 channels (IC50s = 33 and 76 µM, respectively). ML-133 (10 and 30 nmol/animal) prevents the development of dynamic, but not punctate, mechanical allodynia in a mouse model of spared nerve injury.{61040}
Brand:CaymanSKU:31232 - 50 mgAvailable on backorder
ML-148 is an inhibitor of 15-hydroxy prostaglandin dehydrogenase (15-PGDH) with an IC50 value of 56 nM.{21861} It demonstrates selectivity for 15-PGDH when profiled across a panel of related dehydrogenase or reductase enzymes.{21861}
Brand:CaymanSKU:20475 -Available on backorder
ML-148 is an inhibitor of 15-hydroxy prostaglandin dehydrogenase (15-PGDH) with an IC50 value of 56 nM.{21861} It demonstrates selectivity for 15-PGDH when profiled across a panel of related dehydrogenase or reductase enzymes.{21861}
Brand:CaymanSKU:20475 -Available on backorder
ML-148 is an inhibitor of 15-hydroxy prostaglandin dehydrogenase (15-PGDH) with an IC50 value of 56 nM.{21861} It demonstrates selectivity for 15-PGDH when profiled across a panel of related dehydrogenase or reductase enzymes.{21861}
Brand:CaymanSKU:20475 -Available on backorder
ML-161 is an allosteric, reversible inhibitor of proteinase-activated receptor 1 (PAR1) on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC50 value of 0.26 µM.{24559} It blocks platelet activation induced by thrombin as well as by SFLLRN but not by PMA (Item No. 10008014), U-46619 (Item No. 16450), or collagen.{24559}
Brand:CaymanSKU:- ML-161 is an allosteric, reversible inhibitor of proteinase-activated receptor 1 (PAR1) on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC50 value of 0.26 µM.{24559} It blocks platelet activation induced by thrombin as well as by SFLLRN but not by PMA (Item No. 10008014), U-46619 (Item No. 16450), or collagen.{24559}
Brand:CaymanSKU:- ML-161 is an allosteric, reversible inhibitor of proteinase-activated receptor 1 (PAR1) on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC50 value of 0.26 µM.{24559} It blocks platelet activation induced by thrombin as well as by SFLLRN but not by PMA (Item No. 10008014), U-46619 (Item No. 16450), or collagen.{24559}
Brand:CaymanSKU:- ML-161 is an allosteric, reversible inhibitor of proteinase-activated receptor 1 (PAR1) on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC50 value of 0.26 µM.{24559} It blocks platelet activation induced by thrombin as well as by SFLLRN but not by PMA (Item No. 10008014), U-46619 (Item No. 16450), or collagen.{24559}
Brand:CaymanSKU:-
ML-162 is a GPX4 inhibitor that is selectively lethal to mutant RAS oncogene-expressing cell lines (IC50s = 25 and 578 nM for HRASG12V-expressing and wild-type BJ fibroblasts, respectively).{30722,33150} It shares a similar structure but is more potent and selective than (1S,3R)-RSL3 (Item No. 19288), a previously reported inhibitor of RAS oncogene-expressing cells.{33150}
Brand:CaymanSKU:20455 -Available on backorder
ML-162 is a GPX4 inhibitor that is selectively lethal to mutant RAS oncogene-expressing cell lines (IC50s = 25 and 578 nM for HRASG12V-expressing and wild-type BJ fibroblasts, respectively).{30722,33150} It shares a similar structure but is more potent and selective than (1S,3R)-RSL3 (Item No. 19288), a previously reported inhibitor of RAS oncogene-expressing cells.{33150}
Brand:CaymanSKU:20455 -Available on backorder
ML-162 is a GPX4 inhibitor that is selectively lethal to mutant RAS oncogene-expressing cell lines (IC50s = 25 and 578 nM for HRASG12V-expressing and wild-type BJ fibroblasts, respectively).{30722,33150} It shares a similar structure but is more potent and selective than (1S,3R)-RSL3 (Item No. 19288), a previously reported inhibitor of RAS oncogene-expressing cells.{33150}
Brand:CaymanSKU:20455 -Available on backorder
ML-162 is a GPX4 inhibitor that is selectively lethal to mutant RAS oncogene-expressing cell lines (IC50s = 25 and 578 nM for HRASG12V-expressing and wild-type BJ fibroblasts, respectively).{30722,33150} It shares a similar structure but is more potent and selective than (1S,3R)-RSL3 (Item No. 19288), a previously reported inhibitor of RAS oncogene-expressing cells.{33150}
Brand:CaymanSKU:20455 -Available on backorder
Sphingosine-1-phosphate (S1P) is an extracellular lipid mediator whose major effects are mediated through four of the S1P receptors (S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8). Binding of S1P to S1P4 activates ERK, MAPK, and PLC downstream signal transduction pathways. ML-178 activates S1P4 with an EC50 value of 46.3 nM and is inactive against S1P1, S1P2, S1P3, and S1P5 (EC50s = >50 µM) and has no effect against a panel of additional receptors, transporters, and ion channels.{29786}
Brand:CaymanSKU:-Available on backorder
Sphingosine-1-phosphate (S1P) is an extracellular lipid mediator whose major effects are mediated through four of the S1P receptors (S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8). Binding of S1P to S1P4 activates ERK, MAPK, and PLC downstream signal transduction pathways. ML-178 activates S1P4 with an EC50 value of 46.3 nM and is inactive against S1P1, S1P2, S1P3, and S1P5 (EC50s = >50 µM) and has no effect against a panel of additional receptors, transporters, and ion channels.{29786}
Brand:CaymanSKU:-Available on backorder
Sphingosine-1-phosphate (S1P) is an extracellular lipid mediator whose major effects are mediated through four of the S1P receptors (S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8). Binding of S1P to S1P4 activates ERK, MAPK, and PLC downstream signal transduction pathways. ML-178 activates S1P4 with an EC50 value of 46.3 nM and is inactive against S1P1, S1P2, S1P3, and S1P5 (EC50s = >50 µM) and has no effect against a panel of additional receptors, transporters, and ion channels.{29786}
Brand:CaymanSKU:-Available on backorder
Sphingosine-1-phosphate (S1P) is an extracellular lipid mediator whose major effects are mediated through four of the S1P receptors (S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8). Binding of S1P to S1P4 activates ERK, MAPK, and PLC downstream signal transduction pathways. ML-178 activates S1P4 with an EC50 value of 46.3 nM and is inactive against S1P1, S1P2, S1P3, and S1P5 (EC50s = >50 µM) and has no effect against a panel of additional receptors, transporters, and ion channels.{29786}
Brand:CaymanSKU:-Available on backorder
ML-179 is a potent inverse agonist of liver receptor homolog-1 (LRH-1) (IC50 = 320 nM) with maximum efficacy of 40% repression.{24526} It is inactive at the related steroidogenic factor-1 transcriptional activator.{24526} Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the death of estrogen-receptor negative MDA-MB-231 breast cancer cells, and inhibits the steroidogenic acute regulatory promoter (IC50 = 2.12 µM).{24526}
Brand:CaymanSKU:- ML-179 is a potent inverse agonist of liver receptor homolog-1 (LRH-1) (IC50 = 320 nM) with maximum efficacy of 40% repression.{24526} It is inactive at the related steroidogenic factor-1 transcriptional activator.{24526} Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the death of estrogen-receptor negative MDA-MB-231 breast cancer cells, and inhibits the steroidogenic acute regulatory promoter (IC50 = 2.12 µM).{24526}
Brand:CaymanSKU:- ML-179 is a potent inverse agonist of liver receptor homolog-1 (LRH-1) (IC50 = 320 nM) with maximum efficacy of 40% repression.{24526} It is inactive at the related steroidogenic factor-1 transcriptional activator.{24526} Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the death of estrogen-receptor negative MDA-MB-231 breast cancer cells, and inhibits the steroidogenic acute regulatory promoter (IC50 = 2.12 µM).{24526}
Brand:CaymanSKU:- ML-179 is a potent inverse agonist of liver receptor homolog-1 (LRH-1) (IC50 = 320 nM) with maximum efficacy of 40% repression.{24526} It is inactive at the related steroidogenic factor-1 transcriptional activator.{24526} Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the death of estrogen-receptor negative MDA-MB-231 breast cancer cells, and inhibits the steroidogenic acute regulatory promoter (IC50 = 2.12 µM).{24526}
Brand:CaymanSKU:-![A BB3 receptor antagonist; inhibits [125I]BA1 binding to NCI-H1299 lung cancer cells transfected with human BB3 receptors (IC50 = 4.8 μM); selective for BB3 over GRPR and NMBR (IC50s = 16 and >100 μM](https://interpriseusa.com/wp-content/uploads/2021/06/27319.png)
ML-18 is a non-peptide bombesin receptor subtype 3 (BB3) antagonist that inhibits [125I]BA1 binding to NCI-H1299 lung cancer cells transfected with human BB3 receptors (IC50 = 4.8 μM).{47246} It is selective for BB3 over the gastrin releasing peptide receptor (GRPR) and the neuromedin B receptor (NMBR) with IC50 values of 16 and >100 μM, respectively, in a radioligand binding assay. ML-18 (16 μM) reversibly inhibits BA1-induced increases in cytosolic calcium in NCI-H1299 cells. It also inhibits BA1-induced phosphorylation of ERK and EGFR and reduces proliferation of NCI-H1299 cells.
Brand:CaymanSKU:27319 - 1 mgAvailable on backorder
ML-18 is a non-peptide bombesin receptor subtype 3 (BB3) antagonist that inhibits [125I]BA1 binding to NCI-H1299 lung cancer cells transfected with human BB3 receptors (IC50 = 4.8 μM).{47246} It is selective for BB3 over the gastrin releasing peptide receptor (GRPR) and the neuromedin B receptor (NMBR) with IC50 values of 16 and >100 μM, respectively, in a radioligand binding assay. ML-18 (16 μM) reversibly inhibits BA1-induced increases in cytosolic calcium in NCI-H1299 cells. It also inhibits BA1-induced phosphorylation of ERK and EGFR and reduces proliferation of NCI-H1299 cells.
Brand:CaymanSKU:27319 - 10 mgAvailable on backorder
ML-18 is a non-peptide bombesin receptor subtype 3 (BB3) antagonist that inhibits [125I]BA1 binding to NCI-H1299 lung cancer cells transfected with human BB3 receptors (IC50 = 4.8 μM).{47246} It is selective for BB3 over the gastrin releasing peptide receptor (GRPR) and the neuromedin B receptor (NMBR) with IC50 values of 16 and >100 μM, respectively, in a radioligand binding assay. ML-18 (16 μM) reversibly inhibits BA1-induced increases in cytosolic calcium in NCI-H1299 cells. It also inhibits BA1-induced phosphorylation of ERK and EGFR and reduces proliferation of NCI-H1299 cells.
Brand:CaymanSKU:27319 - 5 mgAvailable on backorder
ML-18 is a non-peptide bombesin receptor subtype 3 (BB3) antagonist that inhibits [125I]BA1 binding to NCI-H1299 lung cancer cells transfected with human BB3 receptors (IC50 = 4.8 μM).{47246} It is selective for BB3 over the gastrin releasing peptide receptor (GRPR) and the neuromedin B receptor (NMBR) with IC50 values of 16 and >100 μM, respectively, in a radioligand binding assay. ML-18 (16 μM) reversibly inhibits BA1-induced increases in cytosolic calcium in NCI-H1299 cells. It also inhibits BA1-induced phosphorylation of ERK and EGFR and reduces proliferation of NCI-H1299 cells.
Brand:CaymanSKU:27319 - 500 µgAvailable on backorder
ML-180 is an inverse agonist of liver receptor homolog-1 (LRH-1, IC50 = 3.7 µM) with maximum efficacy of 64% repression.{24526} It is inactive at the related steroidogenic factor-1 transcriptional activator.{24526} Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the death of estrogen-receptor negative MDA-MB-231 breast cancer cells, and inhibits the steroidogenic acute regulatory promoter (IC50 = 2.05 µM).{24526}
Brand:CaymanSKU:- ML-180 is an inverse agonist of liver receptor homolog-1 (LRH-1, IC50 = 3.7 µM) with maximum efficacy of 64% repression.{24526} It is inactive at the related steroidogenic factor-1 transcriptional activator.{24526} Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the death of estrogen-receptor negative MDA-MB-231 breast cancer cells, and inhibits the steroidogenic acute regulatory promoter (IC50 = 2.05 µM).{24526}
Brand:CaymanSKU:- ML-180 is an inverse agonist of liver receptor homolog-1 (LRH-1, IC50 = 3.7 µM) with maximum efficacy of 64% repression.{24526} It is inactive at the related steroidogenic factor-1 transcriptional activator.{24526} Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the death of estrogen-receptor negative MDA-MB-231 breast cancer cells, and inhibits the steroidogenic acute regulatory promoter (IC50 = 2.05 µM).{24526}
Brand:CaymanSKU:- ML-180 is an inverse agonist of liver receptor homolog-1 (LRH-1, IC50 = 3.7 µM) with maximum efficacy of 64% repression.{24526} It is inactive at the related steroidogenic factor-1 transcriptional activator.{24526} Through LRH-1, ML-180 alters the expression of haptoglobin and serum amyloid proteins A1 and A4, induces the death of estrogen-receptor negative MDA-MB-231 breast cancer cells, and inhibits the steroidogenic acute regulatory promoter (IC50 = 2.05 µM).{24526}
Brand:CaymanSKU:-
GPR55 is a G protein-coupled receptor that is weakly activated by some cannabinoids (CBs) at nM concentrations but displays a 5- to 10-fold greater stimulation in response to 1 µM lysophosphatidylinositol (LPI).{17583,15021} ML-184 is a potent synthetic agonist of GPR55 (EC50 = 0.26 µM).{28660} It does not act at the related kynurenic acid receptor GPR35 and is a weak antagonist of CB1 and CB2 (IC50s = 21.8 and 15.1 µM, respectively).{28660} Like LPI, ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55.{28660}
Brand:CaymanSKU:-Available on backorder
GPR55 is a G protein-coupled receptor that is weakly activated by some cannabinoids (CBs) at nM concentrations but displays a 5- to 10-fold greater stimulation in response to 1 µM lysophosphatidylinositol (LPI).{17583,15021} ML-184 is a potent synthetic agonist of GPR55 (EC50 = 0.26 µM).{28660} It does not act at the related kynurenic acid receptor GPR35 and is a weak antagonist of CB1 and CB2 (IC50s = 21.8 and 15.1 µM, respectively).{28660} Like LPI, ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55.{28660}
Brand:CaymanSKU:-Available on backorder
GPR55 is a G protein-coupled receptor that is weakly activated by some cannabinoids (CBs) at nM concentrations but displays a 5- to 10-fold greater stimulation in response to 1 µM lysophosphatidylinositol (LPI).{17583,15021} ML-184 is a potent synthetic agonist of GPR55 (EC50 = 0.26 µM).{28660} It does not act at the related kynurenic acid receptor GPR35 and is a weak antagonist of CB1 and CB2 (IC50s = 21.8 and 15.1 µM, respectively).{28660} Like LPI, ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55.{28660}
Brand:CaymanSKU:-Available on backorder
GPR55 is a G protein-coupled receptor that is weakly activated by some cannabinoids (CBs) at nM concentrations but displays a 5- to 10-fold greater stimulation in response to 1 µM lysophosphatidylinositol (LPI).{17583,15021} ML-184 is a potent synthetic agonist of GPR55 (EC50 = 0.26 µM).{28660} It does not act at the related kynurenic acid receptor GPR35 and is a weak antagonist of CB1 and CB2 (IC50s = 21.8 and 15.1 µM, respectively).{28660} Like LPI, ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55.{28660}
Brand:CaymanSKU:-Available on backorder
ML-191 is an antagonist of GPR55.{24561} It inhibits GPR55 signaling induced by lysophosphatidylinositol (LPI; EC50 = 1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50 = 328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM.{24561}
Brand:CaymanSKU:- ML-191 is an antagonist of GPR55.{24561} It inhibits GPR55 signaling induced by lysophosphatidylinositol (LPI; EC50 = 1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50 = 328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM.{24561}
Brand:CaymanSKU:- ML-191 is an antagonist of GPR55.{24561} It inhibits GPR55 signaling induced by lysophosphatidylinositol (LPI; EC50 = 1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50 = 328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM.{24561}
Brand:CaymanSKU:- ML-191 is an antagonist of GPR55.{24561} It inhibits GPR55 signaling induced by lysophosphatidylinositol (LPI; EC50 = 1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50 = 328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM.{24561}
Brand:CaymanSKU:-
ML-192 is an antagonist of GPR55 (IC50 = 702 nM).{24561} It is selective for GPR55 over the cannabinoid (CB) receptors CB1 and CB2, as well as GPR35 (IC50s = >32 μM).
Brand:CaymanSKU:- ML-192 is an antagonist of GPR55 (IC50 = 702 nM).{24561} It is selective for GPR55 over the cannabinoid (CB) receptors CB1 and CB2, as well as GPR35 (IC50s = >32 μM).
Brand:CaymanSKU:- ML-192 is an antagonist of GPR55 (IC50 = 702 nM).{24561} It is selective for GPR55 over the cannabinoid (CB) receptors CB1 and CB2, as well as GPR35 (IC50s = >32 μM).
Brand:CaymanSKU:-
ML-193 is a potent antagonist of GPR55 (IC50 = 221 nM).{31914,31915} It displays selectivity for GPR55 over CB1, CB2, and GPR35. ML-193 inhibits GPR55-dependent ERK phosphorylation (IC50 = 65 nM) and blocks translocation of PKCβII.{31914} ML-193 blocks increases in intracellular calcium levels induced by lysophosphatidylinositol (LPI) in dissociated rat periaqueductal gray neurons and modulates pain perception in LPI-treated rats.{31913}
Brand:CaymanSKU:- ML-193 is a potent antagonist of GPR55 (IC50 = 221 nM).{31914,31915} It displays selectivity for GPR55 over CB1, CB2, and GPR35. ML-193 inhibits GPR55-dependent ERK phosphorylation (IC50 = 65 nM) and blocks translocation of PKCβII.{31914} ML-193 blocks increases in intracellular calcium levels induced by lysophosphatidylinositol (LPI) in dissociated rat periaqueductal gray neurons and modulates pain perception in LPI-treated rats.{31913}
Brand:CaymanSKU:- ML-193 is a potent antagonist of GPR55 (IC50 = 221 nM).{31914,31915} It displays selectivity for GPR55 over CB1, CB2, and GPR35. ML-193 inhibits GPR55-dependent ERK phosphorylation (IC50 = 65 nM) and blocks translocation of PKCβII.{31914} ML-193 blocks increases in intracellular calcium levels induced by lysophosphatidylinositol (LPI) in dissociated rat periaqueductal gray neurons and modulates pain perception in LPI-treated rats.{31913}
Brand:CaymanSKU:- ML-193 is a potent antagonist of GPR55 (IC50 = 221 nM).{31914,31915} It displays selectivity for GPR55 over CB1, CB2, and GPR35. ML-193 inhibits GPR55-dependent ERK phosphorylation (IC50 = 65 nM) and blocks translocation of PKCβII.{31914} ML-193 blocks increases in intracellular calcium levels induced by lysophosphatidylinositol (LPI) in dissociated rat periaqueductal gray neurons and modulates pain perception in LPI-treated rats.{31913}
Brand:CaymanSKU:-
ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC50s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively).{15626} It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1, TRPV3, TRPA1, or TRPM8 channels at concentrations up to 22 μM.{15626}
Brand:CaymanSKU:- ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC50s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively).{15626} It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1, TRPV3, TRPA1, or TRPM8 channels at concentrations up to 22 μM.{15626}
Brand:CaymanSKU:- ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC50s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively).{15626} It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1, TRPV3, TRPA1, or TRPM8 channels at concentrations up to 22 μM.{15626}
Brand:CaymanSKU:- ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC50s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively).{15626} It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1, TRPV3, TRPA1, or TRPM8 channels at concentrations up to 22 μM.{15626}
Brand:CaymanSKU:-
ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50 = 1.1 µM in a reporter assay).{53859} It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50 = 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated naïve cord blood human CD4+ T cells into Th17 T helper cells.
Brand:CaymanSKU:30164 - 1 mgAvailable on backorder
ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50 = 1.1 µM in a reporter assay).{53859} It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50 = 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated naïve cord blood human CD4+ T cells into Th17 T helper cells.
Brand:CaymanSKU:30164 - 5 mgAvailable on backorder
ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50 = 1.1 µM in a reporter assay).{53859} It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50 = 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated naïve cord blood human CD4+ T cells into Th17 T helper cells.
Brand:CaymanSKU:30164 - 500 µgAvailable on backorder
ML-210 is an inhibitor of glutathione peroxidase 4 (GPX4).{43393} It reduces viability of mesenchymal-state KP4 cells, an effect that can be blocked by the arachidonic acid lipoxygenase inhibitors PD 146176 (Item No. 10010518) and zileuton (Item No. 10006967). It is also selectively lethal to mutant RAS oncogene-expressing cells (IC50s = 71 and 272 nM in HRASG12V-expressing and wild-type RAS-expressing BJeH cells, respectively).{33150}
Brand:CaymanSKU:23282 - 1 mgAvailable on backorder
ML-210 is an inhibitor of glutathione peroxidase 4 (GPX4).{43393} It reduces viability of mesenchymal-state KP4 cells, an effect that can be blocked by the arachidonic acid lipoxygenase inhibitors PD 146176 (Item No. 10010518) and zileuton (Item No. 10006967). It is also selectively lethal to mutant RAS oncogene-expressing cells (IC50s = 71 and 272 nM in HRASG12V-expressing and wild-type RAS-expressing BJeH cells, respectively).{33150}
Brand:CaymanSKU:23282 - 10 mgAvailable on backorder
ML-210 is an inhibitor of glutathione peroxidase 4 (GPX4).{43393} It reduces viability of mesenchymal-state KP4 cells, an effect that can be blocked by the arachidonic acid lipoxygenase inhibitors PD 146176 (Item No. 10010518) and zileuton (Item No. 10006967). It is also selectively lethal to mutant RAS oncogene-expressing cells (IC50s = 71 and 272 nM in HRASG12V-expressing and wild-type RAS-expressing BJeH cells, respectively).{33150}
Brand:CaymanSKU:23282 - 25 mgAvailable on backorder
ML-210 is an inhibitor of glutathione peroxidase 4 (GPX4).{43393} It reduces viability of mesenchymal-state KP4 cells, an effect that can be blocked by the arachidonic acid lipoxygenase inhibitors PD 146176 (Item No. 10010518) and zileuton (Item No. 10006967). It is also selectively lethal to mutant RAS oncogene-expressing cells (IC50s = 71 and 272 nM in HRASG12V-expressing and wild-type RAS-expressing BJeH cells, respectively).{33150}
Brand:CaymanSKU:23282 - 5 mgAvailable on backorder
Lysophospholipase 1 (LYPLA1) is a protein palmitoyl thioesterase responsible for depalmitoylation of the oncogene HRas.{17771,28661} Palmitoylation of such oncogenes is thought to be required for trafficking and malignant transformation, making LYPLA1 a target for downregulating oncogenic signaling.{17771,28661} ML-211 is a carbamate-based dual inhibitor of LYPLA1 (IC50 = 17 nM) and the related LYPLA2 (IC50 = 30 nM).{28662} It can also inhibit the serine hydrolase ABHD11 with an IC50 value of 10 nM but is ≥ 50-fold selective for LYPLA in a panel of 20 additional serine hydrolases.{28662}
Brand:CaymanSKU:-Available on backorder
Lysophospholipase 1 (LYPLA1) is a protein palmitoyl thioesterase responsible for depalmitoylation of the oncogene HRas.{17771,28661} Palmitoylation of such oncogenes is thought to be required for trafficking and malignant transformation, making LYPLA1 a target for downregulating oncogenic signaling.{17771,28661} ML-211 is a carbamate-based dual inhibitor of LYPLA1 (IC50 = 17 nM) and the related LYPLA2 (IC50 = 30 nM).{28662} It can also inhibit the serine hydrolase ABHD11 with an IC50 value of 10 nM but is ≥ 50-fold selective for LYPLA in a panel of 20 additional serine hydrolases.{28662}
Brand:CaymanSKU:-Available on backorder
Lysophospholipase 1 (LYPLA1) is a protein palmitoyl thioesterase responsible for depalmitoylation of the oncogene HRas.{17771,28661} Palmitoylation of such oncogenes is thought to be required for trafficking and malignant transformation, making LYPLA1 a target for downregulating oncogenic signaling.{17771,28661} ML-211 is a carbamate-based dual inhibitor of LYPLA1 (IC50 = 17 nM) and the related LYPLA2 (IC50 = 30 nM).{28662} It can also inhibit the serine hydrolase ABHD11 with an IC50 value of 10 nM but is ≥ 50-fold selective for LYPLA in a panel of 20 additional serine hydrolases.{28662}
Brand:CaymanSKU:-Available on backorder
Lysophospholipase 1 (LYPLA1) is a protein palmitoyl thioesterase responsible for depalmitoylation of the oncogene HRas.{17771,28661} Palmitoylation of such oncogenes is thought to be required for trafficking and malignant transformation, making LYPLA1 a target for downregulating oncogenic signaling.{17771,28661} ML-211 is a carbamate-based dual inhibitor of LYPLA1 (IC50 = 17 nM) and the related LYPLA2 (IC50 = 30 nM).{28662} It can also inhibit the serine hydrolase ABHD11 with an IC50 value of 10 nM but is ≥ 50-fold selective for LYPLA in a panel of 20 additional serine hydrolases.{28662}
Brand:CaymanSKU:-Available on backorder
The KCNQ (Kv7) family of voltage-gated potassium (K+) channels consists of five members, KCNQ1-KCNQ5. KCNQ1-KCNQ5 are critical for setting up the excitation threshold of action potentials. KCNQ1 is expressed mainly in cardiac tissue, peripheral epithelial cells, and smooth muscle cells, while KCNQ2-KCNQ5 are predominantly expressed in the peripheral and central nervous system, including hippocampal cells, cortical cells, and dorsal root ganglion. ML-213 is a selective activator of KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) channels (EC50s = 230 and 510 nM for KCNQ2 and KCNQ4, respectively) that demonstrates > 80-fold selectivity against other related K+ channels.{24549}
Brand:CaymanSKU:- The KCNQ (Kv7) family of voltage-gated potassium (K+) channels consists of five members, KCNQ1-KCNQ5. KCNQ1-KCNQ5 are critical for setting up the excitation threshold of action potentials. KCNQ1 is expressed mainly in cardiac tissue, peripheral epithelial cells, and smooth muscle cells, while KCNQ2-KCNQ5 are predominantly expressed in the peripheral and central nervous system, including hippocampal cells, cortical cells, and dorsal root ganglion. ML-213 is a selective activator of KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) channels (EC50s = 230 and 510 nM for KCNQ2 and KCNQ4, respectively) that demonstrates > 80-fold selectivity against other related K+ channels.{24549}
Brand:CaymanSKU:- The KCNQ (Kv7) family of voltage-gated potassium (K+) channels consists of five members, KCNQ1-KCNQ5. KCNQ1-KCNQ5 are critical for setting up the excitation threshold of action potentials. KCNQ1 is expressed mainly in cardiac tissue, peripheral epithelial cells, and smooth muscle cells, while KCNQ2-KCNQ5 are predominantly expressed in the peripheral and central nervous system, including hippocampal cells, cortical cells, and dorsal root ganglion. ML-213 is a selective activator of KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) channels (EC50s = 230 and 510 nM for KCNQ2 and KCNQ4, respectively) that demonstrates > 80-fold selectivity against other related K+ channels.{24549}
Brand:CaymanSKU:- The KCNQ (Kv7) family of voltage-gated potassium (K+) channels consists of five members, KCNQ1-KCNQ5. KCNQ1-KCNQ5 are critical for setting up the excitation threshold of action potentials. KCNQ1 is expressed mainly in cardiac tissue, peripheral epithelial cells, and smooth muscle cells, while KCNQ2-KCNQ5 are predominantly expressed in the peripheral and central nervous system, including hippocampal cells, cortical cells, and dorsal root ganglion. ML-213 is a selective activator of KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) channels (EC50s = 230 and 510 nM for KCNQ2 and KCNQ4, respectively) that demonstrates > 80-fold selectivity against other related K+ channels.{24549}
Brand:CaymanSKU:-
Bloom (BLM) helicase is a DNA unwinding enzyme important for DNA repair in the homologous recombination pathway. Mutations of the BLM gene result in reduced BLM helicase activity that is associated with the rare genetic disorder, Bloom’s Syndrome, and a predisposition to developing cancer. ML-216 is the first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 50 μM).{24550} At 25-50 μM, ML-216 has been shown to dose-dependently inhibit the proliferation of BLM-expressing PSNF5 fibroblast cells but not BLM-deficient PSNG13 fibroblast cells.{24550}
Brand:CaymanSKU:- Bloom (BLM) helicase is a DNA unwinding enzyme important for DNA repair in the homologous recombination pathway. Mutations of the BLM gene result in reduced BLM helicase activity that is associated with the rare genetic disorder, Bloom’s Syndrome, and a predisposition to developing cancer. ML-216 is the first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 50 μM).{24550} At 25-50 μM, ML-216 has been shown to dose-dependently inhibit the proliferation of BLM-expressing PSNF5 fibroblast cells but not BLM-deficient PSNG13 fibroblast cells.{24550}
Brand:CaymanSKU:- Bloom (BLM) helicase is a DNA unwinding enzyme important for DNA repair in the homologous recombination pathway. Mutations of the BLM gene result in reduced BLM helicase activity that is associated with the rare genetic disorder, Bloom’s Syndrome, and a predisposition to developing cancer. ML-216 is the first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 50 μM).{24550} At 25-50 μM, ML-216 has been shown to dose-dependently inhibit the proliferation of BLM-expressing PSNF5 fibroblast cells but not BLM-deficient PSNG13 fibroblast cells.{24550}
Brand:CaymanSKU:- Bloom (BLM) helicase is a DNA unwinding enzyme important for DNA repair in the homologous recombination pathway. Mutations of the BLM gene result in reduced BLM helicase activity that is associated with the rare genetic disorder, Bloom’s Syndrome, and a predisposition to developing cancer. ML-216 is the first identified small molecule inhibitor of BLM helicase (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 50 μM).{24550} At 25-50 μM, ML-216 has been shown to dose-dependently inhibit the proliferation of BLM-expressing PSNF5 fibroblast cells but not BLM-deficient PSNG13 fibroblast cells.{24550}
Brand:CaymanSKU:-
ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 μM).{48358} It is selective for APJ over the angiotensin II type 1 (AT1) receptor (IC50 = >78 μM). ML-221 antagonizes apelin 13-induced activation of APJ in cAMP and β-arrestin recruitment assays (IC50s = 0.7 and 1.75 μM, respectively). It inhibits proliferation and angiogenesis in Mz-ChA-1 cholangiocarcinoma cells when used at concentrations ranging from 5 to 15 μM.{48359} In vivo, ML-221 (150 μg/kg) reduces tumor growth in a Mz-ChA-1 mouse xenograft model. Intrathecal injection of ML-221 (10 μg per animal) reduces mechanical allodynia and heat hyperalgesia induced by chronic constriction injury (CCI) of the sciatic nerve in rats.{48360} ML-221 also inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy.{48361}
Brand:CaymanSKU:27313 - 10 mgAvailable on backorder
ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 μM).{48358} It is selective for APJ over the angiotensin II type 1 (AT1) receptor (IC50 = >78 μM). ML-221 antagonizes apelin 13-induced activation of APJ in cAMP and β-arrestin recruitment assays (IC50s = 0.7 and 1.75 μM, respectively). It inhibits proliferation and angiogenesis in Mz-ChA-1 cholangiocarcinoma cells when used at concentrations ranging from 5 to 15 μM.{48359} In vivo, ML-221 (150 μg/kg) reduces tumor growth in a Mz-ChA-1 mouse xenograft model. Intrathecal injection of ML-221 (10 μg per animal) reduces mechanical allodynia and heat hyperalgesia induced by chronic constriction injury (CCI) of the sciatic nerve in rats.{48360} ML-221 also inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy.{48361}
Brand:CaymanSKU:27313 - 25 mgAvailable on backorder
ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 μM).{48358} It is selective for APJ over the angiotensin II type 1 (AT1) receptor (IC50 = >78 μM). ML-221 antagonizes apelin 13-induced activation of APJ in cAMP and β-arrestin recruitment assays (IC50s = 0.7 and 1.75 μM, respectively). It inhibits proliferation and angiogenesis in Mz-ChA-1 cholangiocarcinoma cells when used at concentrations ranging from 5 to 15 μM.{48359} In vivo, ML-221 (150 μg/kg) reduces tumor growth in a Mz-ChA-1 mouse xenograft model. Intrathecal injection of ML-221 (10 μg per animal) reduces mechanical allodynia and heat hyperalgesia induced by chronic constriction injury (CCI) of the sciatic nerve in rats.{48360} ML-221 also inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy.{48361}
Brand:CaymanSKU:27313 - 5 mgAvailable on backorder
ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 μM).{48358} It is selective for APJ over the angiotensin II type 1 (AT1) receptor (IC50 = >78 μM). ML-221 antagonizes apelin 13-induced activation of APJ in cAMP and β-arrestin recruitment assays (IC50s = 0.7 and 1.75 μM, respectively). It inhibits proliferation and angiogenesis in Mz-ChA-1 cholangiocarcinoma cells when used at concentrations ranging from 5 to 15 μM.{48359} In vivo, ML-221 (150 μg/kg) reduces tumor growth in a Mz-ChA-1 mouse xenograft model. Intrathecal injection of ML-221 (10 μg per animal) reduces mechanical allodynia and heat hyperalgesia induced by chronic constriction injury (CCI) of the sciatic nerve in rats.{48360} ML-221 also inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy.{48361}
Brand:CaymanSKU:27313 - 50 mgAvailable on backorder