About 30 results found for searched term "COTI-2" (0.094 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M13551 | COTI-2 | p53 |
| COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. | ||
| M1784 | Icotinib | EGFR/HER2 |
| BPI-2009H | ||
| Icotinib (BPI-2009H) is a potent and novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC50 of 5 nM. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. | ||
| M2077 | Detomidine hydrochloride | Adrenergic Receptor |
| Detomidine hydrochloride is a nonnarcotic, synthetic alpha-2 adrenoreceptor agonist. | ||
| M2256 | Ivermectin (MK-933) | Autophagy |
| Stromectol; MK-933; CD-5024; K-237 | ||
| Ivermectin (MK-933) is a positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor and the purinergic P2X4 receptor. Importin α5 inhibitor ivermectin effectively abrogates STAT1-importin α5 interactions. | ||
| M3710 | MK-3697 | OX Receptor |
| MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM. | ||
| M4594 | Cytisine | AChR/AChE |
| Cytisine; Sophorine; Baptitoxine | ||
| Cytisinicline (Cytisine) is an alkaloid that can be extracted from Laburnum and Cytisus. Cytisinicline (Cytisine) is a partial agonist of α4β2 nicotinic acetylcholinergic receptors (α4β2 nAChRs), and also a partial agonist of α4β2 and α7 receptors. It has been used medically to help people quit smoking. | ||
| M58539 | AT 1001 | AChR/AChE |
| AT1001 | ||
| AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) with Ki of 2.64 nM. | ||
| M5750 | Lobeline HCl | AChR/AChE |
| α-Lobeline hydrochloride; L-Lobeline hydrochloride | ||
| Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes. | ||
| M8553 | ABT-089 dihydrochloride | Others |
| ABT-089 (Pozanicline) is a subtype-selective neuronal nicotinic receptor partial agonist binding primarily to the α4β2 and also α6β2 subtypes. | ||
| M9058 | Varenicline hydrochloride | AChR/AChE |
| CP 526555 hcl; Chantix; Champix | ||
| Varenicline hydrochloride is a potent partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR, with EC50s of 2.3 μM and 55 μM, respectively. In addition, Varenicline hydrochloride is also a potent full agonist of α7 nAChRs. In addition, Varenicline hydrochloride is a potent full α7 nAChRs agonist with an EC50 of 18 μM. | ||
| M9077 | STAT5-IN-1 | STAT |
| STAT5 Inhibitor | ||
| STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform. STAT5-IN-1 is a cell permeable nonpetidic nicotinoyl hydrazone which suppresses Stat5 via binding to the SH2 domain. | ||
| M9681 | JBSNF-000088 (6-Methoxynicotinamide) | Others |
| 6-Methoxynicotinamide | ||
| Jbsnf-000088 (6-methoxynicotinamide) is a niacinamide (NA) analogue, which is a potent NNMT inhibitor. Jbsnf-000088 (6-methoxynicotinamide) is a niacinamide n-methyl transferase (NNMT) inhibitor. The IC50 of monkey NNMT and mouse NNMT were 1.8 µM, 2.8 µM and 5.0 µM, respectively. In animal models of metabolic diseases, JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization and regulates glucose. | ||
| M10654 | Ajmalicine (Raubasine) | Adrenergic Receptor |
| Raubasine | ||
| Ajmalicine (Raubasine) is an adrenolytic agent which preferentially blocks alpha 1-adrenoceptor than alpha 2-adrenoceptor. Ajmalicine (Raubasine) is an reversible non-competitive nicotine receptor antagonist with an IC50 of 72.3 μM. | ||
| M10937 | Edicotinib | CSF-1R (c-Fms) |
| JNJ-40346527; JNJ-527 | ||
| Edicotinib (JNJ-40346527) is a potent, selective, blood-brain permeable and orally active CSF-1R inhibitor.IC50 3.2 nM. Edicotinib has less inhibitory effect on KIT and FLT3,IC50 The values are 20 nM and 190 nM, respectively. Edicotinib inhibits the expansion of microglia, weakens the proliferation of microglia and neurodegenerative degeneration. Edicotinib can be used in the study of Alzheimer's disease and rheumatoid arthritis. | ||
| M11322 | JBSNF-000088 | Others |
| 6-Methoxynicotinamide | ||
| Jbsnf-000088 (6-methoxynicotinamide) is an analogue of Nicotinamide (NA), and is an effective inhibitor of Nicotinamide n-methyltransferase (NNMT). The IC50 values for human NNMT(hNNMT), Monkey NNMT(mkNNMT) and mouse NNMT(mNNMT) were 1.8 µM, 2.8 µM and 5.0 µM. | ||
| M13378 | Antide | LHRH/GnRH |
| Sequence：Ac-D2Nal-DCpa-DPal-Ser-Lys(nicotinoyl)-DLys(nicotinoyl)-Leu-Lys(isopropyl)-Pro-DAla-NH2 | ||
| M13406 | Deacetylase Inhibitor Cocktail (100X) | Inhibitor Cocktails |
| AbMole Deacetylase Inhibitor Cocktail is a synergistic combination of chemicals designed to preserve the acetylation state of proteins. AbMole Deacetylase Inhibitor Cocktail (100X) is provided as 1 mL vial. Each vial contains 1 mL 70% DMSO with the following components: Trichostatin A (40 μM), EX-527 (1 mM), Nicotinamide (400 mM), and Sodium Butyrate (200 mM). | ||
| M13986 | MK-6892 | Others |
| MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively. | ||
| M14539 | Dabigatran ethyl ester hydrochloride | Thrombopoietin/Thrombin |
| Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and a thrombin inhibitor. | ||
| M20823 | OT-82 | NAMPT |
| OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03 nM in non-HP cancer cells and 2.89 nM in HP cancer cells, respectively. | ||
| M20843 | NNMTi | Transferase |
| Compound 1k, NNMT inhibitor | ||
| NNMTi (Compound 1k, NNMT inhibitor) is a potent nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 of 1.2 μM. | ||
| M20984 | Varenicline dihydrochloride | AChR/AChE |
| Chantix, Champix | ||
| Varenicline (CP 526555, Chantix, Champix) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation. | ||
| M27881 | 2-Hydroxysaclofen | GABA Receptor |
| 2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats. | ||
| M28597 | Rivanicline | AChR/AChE |
| RJR-2403; (E)-Metanicotine | ||
| Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM). | ||
| M29318 | NS3861 | AChR/AChE |
| NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively. | ||
| M29319 | NS3861 fumarate | AChR/AChE |
| NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively. | ||
| M29351 | Rivanicline oxalate | AChR/AChE |
| RJR-2403 oxalate; (E)-Metanicotine oxalate | ||
| Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM). | ||
| M29693 | Ispronicline | AChR/AChE |
| TC-1734; ACD3480 | ||
| Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR. | ||
| M29978 | CP-601927 | AChR/AChE |
| CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties. | ||
| M30160 | Anagyrine | AChR/AChE |
| (-)-Anagyrine; Monolupine; Rhombinine | ||
| Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR. | ||
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