About 33 results found for searched term "Antagonist G" (0.11 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M9082 | ISO-1 | NLR |
| MIF Antagonist; Macrophage Migration Inhibitory Factor | ||
| ISO-1, also known as MIF Antagonist, is a MIF inhibitor with an IC50 of 7 uM. ISO-1 exerts anti-cancer effects on PANC-1 cell proliferation, migration and invasion in vitro, and inhibited PANC-1 cell-induced tumour growth in xenograft mice in vivo. | ||
| M10242 | Antagonist G | Vasopressin Receptor |
| ARG-D-TRP-N-ME-PHE-D-TRP-LEU-MET-NH2 | ||
| Antagonist G is an anticancer peptide and it is also a potent vasopressin antagonist. | ||
| M41342 | FKBP51F67V-selective antagonist Ligand2 | FKBP (FK506-binding protein) |
| FKBP51F67V-selective antagonist Ligand2 is a potent FKBP51 F67V-selective antagonist ligand. | ||
| M1712 | FTY720 hydrochloride | S1P Receptor |
| Fingolimod hydrochloride | ||
| Fingolimod (FTY720) HCl is a 1-phospho-neuraminol S1P receptor antagonist with an IC50 of 0.33 nM. , FTY720 can dephosphorylate AMPK by activating PP2A and reduce the expression level of phosphorylated eEF2K, ultimately leading to ADCD and iron death in human multiple myeloma cells. | ||
| M1812 | GANT58 | Gli |
| NSC75503 | ||
| GANT58 (NSC75503) is a potent GLI antagonist that inhibits GLI1-induced transcription with an IC50 of 5 μM. | ||
| M1917 | Mozavaptan | Vasopressin Receptor |
| OPC-31260 | ||
| Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. | ||
| M1966 | Fulvestrant | Estrogen Receptor |
| ICI 182780; ZD 9238; ZM 182780 | ||
| Fulvestrant is a Estrogen receptor (ER) antagonist with IC50 of 0.094 nM. Fulvestrant can also induce autophagy and apoptosis, and has anti-tumor effect. | ||
| M1971 | Maraviroc | CCR |
| Selzentry, Celsentri, UK-427857 | ||
| Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties. | ||
| M2026 | AT-406 | IAP |
| SM-406; Xevinapant; Debio 1143 | ||
| Xevinapant (Debio1143,AT-406, SM-406) is a potentially first-in-class, highly potent oral antagonist of inhibitor of apoptosis protein (IAP), which not only promotes cancer cell death by inhibiting IAP, but also It can enhance the anti-tumor immune response by inhibiting IAP. | ||
| M2041 | WZ 811 | CXCR |
| WZ811 is a highly competitive CXCR4 antagonist with oral activity. WZ811 effectively inhibited CXCR4/SDF-1 (also known as CXCL12) -mediated regulation of cAMP level (EC50=1.2 nM) and SDF-1-induced matrix glue invasion (EC50=5.2 nM) in cells. | ||
| M2051 | CP 945598 hydrochloride | Cannabinoid |
| Otenabant HCl; Otenabant hydrochloride | ||
| CP 945598 hydrochloride is a selective and high affinity CB1 antagonist (Ki values are 0.7 and 0.12 nM in binding and functional assays respectively). | ||
| M2106 | Azilsartan | Angiotensin Receptor |
| TAK-536 | ||
| Azilsartan (TAK-536) is an angiotensin II type 1 (AT1) receptor antagonist with IC50 of 2.6 nM. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. | ||
| M2134 | Vortioxetine hydrobromide | 5-HT Receptor |
| Lu AA21004 | ||
| Vortioxetine hydrobromide (Lu AA21004) is a 5-HT3, 5-HT7 and 5-HT1D receptor antagonist, a 5-HT1B receptor partial agonist, a 5-HT1A receptor agonist and a 5-HT transporter (5-HTT) inhibitor in vitro. | ||
| M2161 | Navarixin | CXCR |
| SCH 527123; MK-7123 | ||
| Navarixin (SCH 527123) is a novel, selective CXCR2 receptor antagonist with IC50 of 3 nM. Navarixin (SCH 527123) has Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly. | ||
| M2166 | Birinapant | IAP |
| TL32711 | ||
| Birinapant (TL32711) is a bivalent Smac analogue, which is a potent antagonist of XIAP and cIAP1 with Kd values of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces autoubiquitination and proteasome degradation of cIAP1 and cIAP2 in intact cells, resulting in the formation of RIPK1: Caspase-8 complex, which activates and induces tumor cell death. | ||
| M2347 | (+)-Bicuculline | GABA Receptor |
| d-Bicuculline | ||
| (+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels. | ||
| M2266 | Pizotifen malate | 5-HT Receptor |
| Sandomigran, pizotyline | ||
| Pizotifen malate is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site. | ||
| M2280 | Tamoxifen Citrate (ICI 46474) | Estrogen Receptor |
| ICI 46474; Istubal; Nolvadex | ||
| Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding. | ||
| M2344 | RU 58841 | Androgen Receptor |
| RU 58841 is a specific androgen receptor antagonist or anti-androgen. | ||
| M2365 | Acebutolol hydrochloride | Adrenergic Receptor |
| Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. | ||
| M2372 | Alizapride hydrochloride | Dopamine Receptor |
| Alizapride hydrochloride is a dopamine receptor antagonist used for the theropy of nausea and vomiting. | ||
| M2381 | AMD3465 hexahydrobromide (AMD3465 ) | CXCR |
| GENZ-644494 hexahydrobromide | ||
| AMD3465 hexahydrobromide（AMD3465 ) is an effective CXCR4 antagonist that inhibits 12G5 mAb in SupT1 cells. The IC50 values of CXCL12AF647 and CXCR4 were 0.75 nM and 18 nM, respectively. AMD 3465 also effectively inhibited X4 HIV replication (IC50, 1-10 nM), but not R5 HIV replication. | ||
| M2383 | AMG-517 | TRP Channel |
| AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. | ||
| M2393 | Amprolium hydrochloride | Parasite |
| Amprolium chloride is a thiamin antagonist, which prevents carbohydrate synthesis by blocking thiamine uptake. | ||
| M2418 | AZD1981 | GPR/FFAR |
| AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. | ||
| M2420 | Labetalol hydrochloride | Adrenergic Receptor |
| Labetalol HCl | ||
| Labetalol hydrochloride is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors. | ||
| M2445 | Benztropine mesylate | Dopamine Receptor |
| Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate | ||
| Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM. Benztropine mesylate is a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects. Benztropine mesylate is also an anti-histamine agent and a dopamine re-uptake inhibitor. | ||
| M2447 | PF-5274857 | Hedgehog |
| PF-5274857 is a novel Smoothened antagonist, inhibits Hedgehog signaling with IC50 and Ki values of 5.8 nM and 4.6 nM, respectively. | ||
| M2468 | Brimonidine Tartrate | Adrenergic Receptor |
| Brimonidine tartrate; AGN190342 tartrate; UK14304 tartrate | ||
| Brimonidine Tartrate is a highly selective α-adrenergic receptor antagonist with an EC50 of 0.45 nM for α2A adrenoreceptor, and has been used to study open-angle glaucoma or ocular hypertension. | ||
| M2542 | CTEP | GluR |
| mGluR5 inhibitor | ||
| CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors. | ||
| M2558 | DMOG | HIF |
| Dimethyloxallyl Glycine | ||
| DMOG (Dimethyloxaloyl glycine) is an antagonist of α-ketoglutarate cofactor and a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy. | ||
| M2584 | MDL-29951 | GluR |
| MDL-29951 is a novel glycine antagonist of NMDA receptor activation (Ki=0.14 mM, [3H]glycine binding) in vitro and in vivo with IC50 value of 0.14 mM ([3H]glycine binding). | ||
| M2650 | Doxepin hydrochloride | Histamine Receptor |
| Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. | ||
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