About 30 results found for searched term "PT-S58" (0.192 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M8332 | PT-S58 | Others |
| PT-S58 is a PPAR β/δ full antagonist, and a derivative of GSK0660. | ||
| M2623 | Desvenlafaxine | 5-HT Receptor |
| O-Desmethylvenlafaxine | ||
| Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively. | ||
| M2624 | Desvenlafaxine Succinate | 5-HT Receptor |
| O-Desmethylvenlafaxine succinate hydrate | ||
| Desvenlafaxine Succinate is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively. | ||
| M2838 | Meptazinol hydrochloride | Opioid Receptor |
| IL-22811 hydrochloride; WY-22811 hydrochloride | ||
| Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM. | ||
| M3457 | Naftopidil | Adrenergic Receptor |
| KT-611; BM-15275 | ||
| Naftopidil is a selective α1-adrenergic receptor antagonist or alpha blocker with a Ki of 58.3 nM. | ||
| M4075 | Ginsenoside-Rd | NF-κB |
| Gypenoside VIII | ||
| Ginsenoside Rd inhibited NF-κB transcriptional activity induced by TNFα with IC50 of 12.05±0.82 μM. Ginsenoside Rd inhibited the expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibited CYP2D6, CYP1A2, CYP3A4 and CYP2C9 with IC50 of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM and 85.1±9.1 μM, respectively. | ||
| M7191 | RF9 | Neuropeptide Receptor |
| RF-9; RF 9 | ||
| RF9 is a selective NPFF receptor antagonist (Ki values are 58 and 75 nM at hNPFF1 and hNPFF2 receptors respectively). | ||
| M8408 | CU-CPT22 | TLR |
| CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM. | ||
| M11210 | MN58b | Apoptosis |
| MN58b is a selective inhibitor of choline kinase α (CHKα) and inhibits phosphocholine synthesis. MN58b induces apoptosis to reduce cell growth. MN58b also has antitumoral activity. | ||
| M11264 | KI-7 | Adenosine Receptor |
| Ki-7 is an A2B adenosine receptor positive allosteric regulator. Ki-7 enhances cAMP accumulation induced by NECA, a non-selective A2B adenosine receptor agonist (EC50=445.8 nM). Ki-7 also enhanced selective A2B adenosine receptor agonist BAY 60-6583 and adenosine-induced cAMP accumulation with EC50 of 2390 nM and 2550 nM, respectively. | ||
| M11287 | JNJ-39758979 | Histamine Receptor |
| Jnj-39758979 is a selective, orally active, high-affinity histamine H4 receptor antagonist with Ki values of 12.5, 5.3 and 25 nM for human, mouse and monkey histamine H4 receptor, respectively. Jnj-39758979 antagonized histamine-induced cAMP inhibition with a pA2 of 7.9. Jnj-39758979 has good anti-inflammatory and antipruritic effects. | ||
| M11420 | MYCi975 | c-Myc |
| NUCC-0200975 | ||
| MYCi975 (Nuc-0200975) is an orally active MYC inhibitor that disrupts MYC/MAX interactions, promotes MYC T58 phosphorylation and MYC degradation, and impairs myC-driven gene expression. MYCi975 (NUC-0200975) has strong anti-tumor effect and good tolerance, increasing tumor immune cell infiltration and enhancing tumor sensitivity against PD1 immune studies. | ||
| M11530 | Guvacine | GABA Receptor |
| Guvacine, an alkaloid found in areca nut, is an effective inhibitor of GABA uptake. Guvacine inhibited rat GAT-1 with IC50 values of 39 μM, 58 μM and 378 μM, respectively. | ||
| M25541 | SKF-82958 hydrobromide | Dopamine Receptor |
| (±)-SKF-82958 hydrobromide; Chloro-APB hydrobromide | ||
| SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM). | ||
| M13762 | 5(6)-TAMRA | Fluorescent Dye |
| 5(6)-Carboxytetramethylrhodamine | ||
| 5(6)-TAMRA contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid; bright, orange-fluorescent dye produces conjugates with absorption/emission maxima of ~555/580 nm. | ||
| M14935 | YB-0158 | Wnt/beta-catenin |
| Wnt pathway inhibitor 2 | ||
| YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities. | ||
| M27798 | SNT-207858 | Melanocortin Receptor |
| SNT207858 is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor. | ||
| M27800 | SNT-207858 free base | Melanocortin Receptor |
| SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor. | ||
| M27880 | L-745870 hydrochloride | Dopamine Receptor |
| L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors. | ||
| M27932 | SRTCX1002 | Sirtuin |
| SRTCX1002 is a potent activator of SIRT1 (STAC), suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB Activity. SRTCX1002 suppresses stimuli-induced NF-κB transcriptional activation and LPS-induced TNFα secretion with IC50s of 0.71 and 7.58 µM, respectively. | ||
| M28243 | RP 67580 | Neurokinin Receptor |
| RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation. | ||
| M28632 | CMF019 | Others |
| CMF019 is a potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. | ||
| M28637 | L-745870 | Dopamine Receptor |
| L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors. | ||
| M29325 | ABDP 581/591 C11 | Fluorescent Dye |
| ABDP C11 | ||
| ABDP 581/591 C11 (same as BODIPY 581/591 C11) is a BODIPY borofluoroprene derivative with good light stability and low fluorescence artifacts. ABDP 581/591 C11 (same as BODIPY 581/591 C11) can be used for study lipid peroxidation and antioxidant properties in living cells, or detect ferroptosis by reaction with hydroxyl radicals. ABDP 581/591 C11 is emitted at 591 nm (reduced prototype), or redshifted to 510 nm (oxidized type). The excitation wavelengths were 581 nm (reduced prototype) and 500 nm (oxidized type). | ||
| M29495 | PD 102807 | AChR/AChE |
| PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively. Antidyskinetic effect. | ||
| M30084 | PPI-2458 | Others |
| PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research. | ||
| M30365 | AS604872 | Prostaglandin Receptor |
| AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour. | ||
| M30560 | JNJ10191584 | Histamine Receptor |
| VUF6002 | ||
| JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively. | ||
| M30747 | L-745870 trihydrochloride | Dopamine Receptor |
| L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors. | ||
| M30826 | EAI001 | EGFR/HER2 |
| EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer. | ||
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