Chemicals
Showing 27151–27300 of 41137 results
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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
ML-226 is an inhibitor of α/β hydrolase domain-containing protein 11 (ABHD11) that inhibits ABHD11 in vitro and in situ (IC50s = 15 and 0.68 nM, respectively).{45078} It is 100-fold selective for ABHD11 over approximately 20 other serine hydrolases. ML-226 covalently carbamoylates the active site serine of ABHD11. It can be used as an anti-probe for ML-211 (Item No. 17630), an inhibitor of the protein palmitoyl thioesterases lysophospholipase 1 (LYPLA1) and LYPA2.{28662}
Brand:CaymanSKU:25681 - 1 mgAvailable on backorder
ML-226 is an inhibitor of α/β hydrolase domain-containing protein 11 (ABHD11) that inhibits ABHD11 in vitro and in situ (IC50s = 15 and 0.68 nM, respectively).{45078} It is 100-fold selective for ABHD11 over approximately 20 other serine hydrolases. ML-226 covalently carbamoylates the active site serine of ABHD11. It can be used as an anti-probe for ML-211 (Item No. 17630), an inhibitor of the protein palmitoyl thioesterases lysophospholipase 1 (LYPLA1) and LYPA2.{28662}
Brand:CaymanSKU:25681 - 10 mgAvailable on backorder
ML-226 is an inhibitor of α/β hydrolase domain-containing protein 11 (ABHD11) that inhibits ABHD11 in vitro and in situ (IC50s = 15 and 0.68 nM, respectively).{45078} It is 100-fold selective for ABHD11 over approximately 20 other serine hydrolases. ML-226 covalently carbamoylates the active site serine of ABHD11. It can be used as an anti-probe for ML-211 (Item No. 17630), an inhibitor of the protein palmitoyl thioesterases lysophospholipase 1 (LYPLA1) and LYPA2.{28662}
Brand:CaymanSKU:25681 - 5 mgAvailable on backorder
The hypoxia-inducible factor (HIF) transcription factors are members of the basic-helix-loop-helix (bHLH) family of transcription factors and play important roles in maintaining cellular oxygen homeostasis.{11044,12428} HIF-1α has emerged as an important drug target in breast and prostate cancer, cardiovascular disease, and ischemia.{10724,11835} ML-228 is an activator of the HIF signaling pathway, as demonstrated by HIF response element (HRE) reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM).{23099} Its activity in the HRE assay is blocked by excess iron, suggesting that ML-228 can chelate iron.{23099} Molecular modeling indicates that ML-228 does not modulate HIF signaling by binding to prolyl hydroxyases.{23099} ML-228 also significantly inhibits ligand binding to several channels, receptors, and transporters, including ERG potassium channel, 5-HT2B and A3 adenosine receptors, and dopamine transporter.{23099}
Brand:CaymanSKU:- The hypoxia-inducible factor (HIF) transcription factors are members of the basic-helix-loop-helix (bHLH) family of transcription factors and play important roles in maintaining cellular oxygen homeostasis.{11044,12428} HIF-1α has emerged as an important drug target in breast and prostate cancer, cardiovascular disease, and ischemia.{10724,11835} ML-228 is an activator of the HIF signaling pathway, as demonstrated by HIF response element (HRE) reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM).{23099} Its activity in the HRE assay is blocked by excess iron, suggesting that ML-228 can chelate iron.{23099} Molecular modeling indicates that ML-228 does not modulate HIF signaling by binding to prolyl hydroxyases.{23099} ML-228 also significantly inhibits ligand binding to several channels, receptors, and transporters, including ERG potassium channel, 5-HT2B and A3 adenosine receptors, and dopamine transporter.{23099}
Brand:CaymanSKU:- The hypoxia-inducible factor (HIF) transcription factors are members of the basic-helix-loop-helix (bHLH) family of transcription factors and play important roles in maintaining cellular oxygen homeostasis.{11044,12428} HIF-1α has emerged as an important drug target in breast and prostate cancer, cardiovascular disease, and ischemia.{10724,11835} ML-228 is an activator of the HIF signaling pathway, as demonstrated by HIF response element (HRE) reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM).{23099} Its activity in the HRE assay is blocked by excess iron, suggesting that ML-228 can chelate iron.{23099} Molecular modeling indicates that ML-228 does not modulate HIF signaling by binding to prolyl hydroxyases.{23099} ML-228 also significantly inhibits ligand binding to several channels, receptors, and transporters, including ERG potassium channel, 5-HT2B and A3 adenosine receptors, and dopamine transporter.{23099}
Brand:CaymanSKU:- The hypoxia-inducible factor (HIF) transcription factors are members of the basic-helix-loop-helix (bHLH) family of transcription factors and play important roles in maintaining cellular oxygen homeostasis.{11044,12428} HIF-1α has emerged as an important drug target in breast and prostate cancer, cardiovascular disease, and ischemia.{10724,11835} ML-228 is an activator of the HIF signaling pathway, as demonstrated by HIF response element (HRE) reporter assay (EC50 = 1.2 µM), HIF-1α nuclear translocation assay (EC50 = 1.3 µM), and increased VEGF expression (EC50 = 1.6 µM).{23099} Its activity in the HRE assay is blocked by excess iron, suggesting that ML-228 can chelate iron.{23099} Molecular modeling indicates that ML-228 does not modulate HIF signaling by binding to prolyl hydroxyases.{23099} ML-228 also significantly inhibits ligand binding to several channels, receptors, and transporters, including ERG potassium channel, 5-HT2B and A3 adenosine receptors, and dopamine transporter.{23099}
Brand:CaymanSKU:-
ML-230 is an inhibitor of ATP-binding cassette family G member 2 (ABCG2).{61128} It selectively inhibits JC-1 efflux in Ig-MXP3 cells overexpressing ABCG2 over Jurkat cells overexpressing ABCB1 (IC50s = 0.13 and 4.65 µM, respectively). ML-230 enhances inhibition of IGROV-1/T8 ovarian cancer cell colony formation induced by topotecan (Item No. 14129).{61129} Intratumoral injection of ML-230 (100 nM) and topotecan reduces tumor size in an IGROV-1/T8 mouse xenograft model.
Brand:CaymanSKU:32552 - 1 mgAvailable on backorder
ML-230 is an inhibitor of ATP-binding cassette family G member 2 (ABCG2).{61128} It selectively inhibits JC-1 efflux in Ig-MXP3 cells overexpressing ABCG2 over Jurkat cells overexpressing ABCB1 (IC50s = 0.13 and 4.65 µM, respectively). ML-230 enhances inhibition of IGROV-1/T8 ovarian cancer cell colony formation induced by topotecan (Item No. 14129).{61129} Intratumoral injection of ML-230 (100 nM) and topotecan reduces tumor size in an IGROV-1/T8 mouse xenograft model.
Brand:CaymanSKU:32552 - 10 mgAvailable on backorder
ML-230 is an inhibitor of ATP-binding cassette family G member 2 (ABCG2).{61128} It selectively inhibits JC-1 efflux in Ig-MXP3 cells overexpressing ABCG2 over Jurkat cells overexpressing ABCB1 (IC50s = 0.13 and 4.65 µM, respectively). ML-230 enhances inhibition of IGROV-1/T8 ovarian cancer cell colony formation induced by topotecan (Item No. 14129).{61129} Intratumoral injection of ML-230 (100 nM) and topotecan reduces tumor size in an IGROV-1/T8 mouse xenograft model.
Brand:CaymanSKU:32552 - 5 mgAvailable on backorder
ML-239 is an inhibitor of cancer stem cells, displaying greater than 23-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 1.18 µM) over an isogenic control cell line (EC50 = 27.6 µM).{24522,24523,24524} It is also toxic to the breast carcinoma cell line MDA-MB-231.{24522} ML-239 alters the expression of genes in the MAPK, NF-κB, and inflammatory cytokine pathways.{24522,24524} It is stable in saline and modestly stable in human plasma.{24523}
Brand:CaymanSKU:- ML-239 is an inhibitor of cancer stem cells, displaying greater than 23-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 1.18 µM) over an isogenic control cell line (EC50 = 27.6 µM).{24522,24523,24524} It is also toxic to the breast carcinoma cell line MDA-MB-231.{24522} ML-239 alters the expression of genes in the MAPK, NF-κB, and inflammatory cytokine pathways.{24522,24524} It is stable in saline and modestly stable in human plasma.{24523}
Brand:CaymanSKU:- ML-239 is an inhibitor of cancer stem cells, displaying greater than 23-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 1.18 µM) over an isogenic control cell line (EC50 = 27.6 µM).{24522,24523,24524} It is also toxic to the breast carcinoma cell line MDA-MB-231.{24522} ML-239 alters the expression of genes in the MAPK, NF-κB, and inflammatory cytokine pathways.{24522,24524} It is stable in saline and modestly stable in human plasma.{24523}
Brand:CaymanSKU:- ML-239 is an inhibitor of cancer stem cells, displaying greater than 23-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 1.18 µM) over an isogenic control cell line (EC50 = 27.6 µM).{24522,24523,24524} It is also toxic to the breast carcinoma cell line MDA-MB-231.{24522} ML-239 alters the expression of genes in the MAPK, NF-κB, and inflammatory cytokine pathways.{24522,24524} It is stable in saline and modestly stable in human plasma.{24523}
Brand:CaymanSKU:-
ML-240 is an ATP-competitive inhibitor of the D2 domain of the ATPase p97 (IC50 = 0.11 µM; Ki = 0.22 µM).{28269,28270} It disrupts the endoplasmic reticulum-associated degradation (ERAD) and autophagy pathways, preventing the degradation of p97-dependent proteasome substrates (IC50 = 0.9 µM) and causing accumulation of ubiquitin conjugates in nuclear membrane and cytosolic compartments at 5-10 µM.{28269} ML-240 has also been shown to block proliferation of HCT15 and SW403 colon cancer cell lines (GI50s = 0.76 and 0.5 µM, respectively) and to rapidly mobilize caspase-3 and -7, inducing apoptosis.{28269}
Brand:CaymanSKU:-Available on backorder
ML-240 is an ATP-competitive inhibitor of the D2 domain of the ATPase p97 (IC50 = 0.11 µM; Ki = 0.22 µM).{28269,28270} It disrupts the endoplasmic reticulum-associated degradation (ERAD) and autophagy pathways, preventing the degradation of p97-dependent proteasome substrates (IC50 = 0.9 µM) and causing accumulation of ubiquitin conjugates in nuclear membrane and cytosolic compartments at 5-10 µM.{28269} ML-240 has also been shown to block proliferation of HCT15 and SW403 colon cancer cell lines (GI50s = 0.76 and 0.5 µM, respectively) and to rapidly mobilize caspase-3 and -7, inducing apoptosis.{28269}
Brand:CaymanSKU:-Available on backorder
ML-240 is an ATP-competitive inhibitor of the D2 domain of the ATPase p97 (IC50 = 0.11 µM; Ki = 0.22 µM).{28269,28270} It disrupts the endoplasmic reticulum-associated degradation (ERAD) and autophagy pathways, preventing the degradation of p97-dependent proteasome substrates (IC50 = 0.9 µM) and causing accumulation of ubiquitin conjugates in nuclear membrane and cytosolic compartments at 5-10 µM.{28269} ML-240 has also been shown to block proliferation of HCT15 and SW403 colon cancer cell lines (GI50s = 0.76 and 0.5 µM, respectively) and to rapidly mobilize caspase-3 and -7, inducing apoptosis.{28269}
Brand:CaymanSKU:-Available on backorder
ML-240 is an ATP-competitive inhibitor of the D2 domain of the ATPase p97 (IC50 = 0.11 µM; Ki = 0.22 µM).{28269,28270} It disrupts the endoplasmic reticulum-associated degradation (ERAD) and autophagy pathways, preventing the degradation of p97-dependent proteasome substrates (IC50 = 0.9 µM) and causing accumulation of ubiquitin conjugates in nuclear membrane and cytosolic compartments at 5-10 µM.{28269} ML-240 has also been shown to block proliferation of HCT15 and SW403 colon cancer cell lines (GI50s = 0.76 and 0.5 µM, respectively) and to rapidly mobilize caspase-3 and -7, inducing apoptosis.{28269}
Brand:CaymanSKU:-Available on backorder
ML-243 is an inhibitor of cancer stem cells, displaying 32-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 2.0 µM) over a control (mammary epithelial) cell line (EC50 = 64 µM).{24541} It weakly antagonizes the adenosine A2A receptor (IC50 = 10 µM) and has no effect on 68 other targets commonly used in drug discovery for lead profiling.{24541}
Brand:CaymanSKU:- ML-243 is an inhibitor of cancer stem cells, displaying 32-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 2.0 µM) over a control (mammary epithelial) cell line (EC50 = 64 µM).{24541} It weakly antagonizes the adenosine A2A receptor (IC50 = 10 µM) and has no effect on 68 other targets commonly used in drug discovery for lead profiling.{24541}
Brand:CaymanSKU:- ML-243 is an inhibitor of cancer stem cells, displaying 32-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 2.0 µM) over a control (mammary epithelial) cell line (EC50 = 64 µM).{24541} It weakly antagonizes the adenosine A2A receptor (IC50 = 10 µM) and has no effect on 68 other targets commonly used in drug discovery for lead profiling.{24541}
Brand:CaymanSKU:- ML-243 is an inhibitor of cancer stem cells, displaying 32-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 2.0 µM) over a control (mammary epithelial) cell line (EC50 = 64 µM).{24541} It weakly antagonizes the adenosine A2A receptor (IC50 = 10 µM) and has no effect on 68 other targets commonly used in drug discovery for lead profiling.{24541}
Brand:CaymanSKU:-
ML-261 is a thienopyrrole-5-carboxamide that inhibits lipid droplet formation in murine AML12 hepatocytes (IC50 = 69.7 nM) but not in human Huh7 hepatocellular carcinoma or primary hepatocyte cells.{24552}
Brand:CaymanSKU:- ML-261 is a thienopyrrole-5-carboxamide that inhibits lipid droplet formation in murine AML12 hepatocytes (IC50 = 69.7 nM) but not in human Huh7 hepatocellular carcinoma or primary hepatocyte cells.{24552}
Brand:CaymanSKU:- ML-261 is a thienopyrrole-5-carboxamide that inhibits lipid droplet formation in murine AML12 hepatocytes (IC50 = 69.7 nM) but not in human Huh7 hepatocellular carcinoma or primary hepatocyte cells.{24552}
Brand:CaymanSKU:- ML-261 is a thienopyrrole-5-carboxamide that inhibits lipid droplet formation in murine AML12 hepatocytes (IC50 = 69.7 nM) but not in human Huh7 hepatocellular carcinoma or primary hepatocyte cells.{24552}
Brand:CaymanSKU:-
ML-262 is an inhibitor of hepatic lipid droplet formation (IC50 = 6.4 nM in murine AML-12 cells), which is associated with non-alcoholic fatty liver disease.{24552} ML-262 does not induce cytotoxicity (up to 33 µM) or inhibit fatty acid uptake (up to 50 µM).
Brand:CaymanSKU:21902 -Out of stock
ML-262 is an inhibitor of hepatic lipid droplet formation (IC50 = 6.4 nM in murine AML-12 cells), which is associated with non-alcoholic fatty liver disease.{24552} ML-262 does not induce cytotoxicity (up to 33 µM) or inhibit fatty acid uptake (up to 50 µM).
Brand:CaymanSKU:21902 -Out of stock
ML-262 is an inhibitor of hepatic lipid droplet formation (IC50 = 6.4 nM in murine AML-12 cells), which is associated with non-alcoholic fatty liver disease.{24552} ML-262 does not induce cytotoxicity (up to 33 µM) or inhibit fatty acid uptake (up to 50 µM).
Brand:CaymanSKU:21902 -Out of stock