About 30 results found for searched term "LE 300" (0.078 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M6901 | LE 300 | Others |
| LE 300 is a potent and selective dopamine D 1 antagonist. | ||
| M2482 | C646 | Histone Acetyltransferase |
| C 646 | ||
| C646 is a selective inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM. C646 preferentially selective for p300 versus other acetyltransferases. | ||
| M2504 | CFTR(inh)-172 | CFTR |
| CFTR inhibitor 172 | ||
| CFTR(inh)-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters. | ||
| M2667 | Empagliflozin | SGLT |
| BI 10773 | ||
| Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. | ||
| M2717 | Galeterone | Androgen Receptor |
| TOK-001 | ||
| Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. | ||
| M2735 | GSK2656157 | PERK |
| GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM, 500-fold greater against a panel of 300 kinases. | ||
| M2859 | ML347 | ALK |
| LDN 193719 | ||
| ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM. | ||
| M3309 | Bethanechol chloride | AChR/AChE |
| Carbamyl-β-methylcholine chloride | ||
| Bethanechol chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors. Bethanechol chloride (0.3-300 μM) significantly reduces ileal pacemaker potentials. | ||
| M3569 | AST-1306 (TsOH) | EGFR/HER2 |
| AST-6; Allitinib tosylate | ||
| AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases, | ||
| M3645 | MG149 | Histone Acetyltransferase |
| MG149 is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50= 47 uM); little potent for PCAF and p300 (IC50 >200 uM). | ||
| M3932 | NVP-TNKS656 | PARP |
| TNKS-656 | ||
| NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2. | ||
| M4606 | Phloridzin | SGLT |
| Floridzin; NSC 2833 | ||
| Phloridzin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor. | ||
| M5515 | Vitamin D3 | Vitamin |
| Cholecalciferol; Colecalciferol | ||
| Vitamin D3 (Cholecalciferol) is a form of vitamin D, binds and activates a H305F/H397Y mutant vitamin D receptor (VDR) with EC50 of 300 nM. *The compound is unstable in solutions, freshly prepared is recommended | ||
| M5809 | Nefazodone hydrochloride | 5-HT Receptor |
| BMY-13754; MJ-13754-1 | ||
| Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). | ||
| M5989 | Tandospirone | 5-HT Receptor |
| SM-3997 | ||
| Tandospirone(SM-3997) is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM). | ||
| M6154 | 2-PMPA tetrasodium | Others |
| PMPA tetrasodium salt; 2-(Phosphonomethyl)pentanedioic acid | ||
| 2-PMPA (PMPA tetrasodium salt) is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) with an IC50 of 300 pM. | ||
| M6176 | TMP195 | HDAC |
| TFMO 2 | ||
| TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays. | ||
| M10604 | Pirtobrutinib (LOXO-305) | BTK |
| LY 3527727; RXC-005 | ||
| Pirtobrutinib (LOXO-305; LY 3527727; RXC-005) is a first-in-class, highly selective, non-covalent, next-generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells.Pirtobrutinib's selectivity for BTK more than 300 times more selective than other 370 kinases. Pirtobrutinib can be used in studies related to chronic lymphocytic leukemia (CLL). | ||
| M6808 | I-CBP 112 | Histone Acetyltransferase |
| I-CBP 112 is a selective CBP/p300 BRD inhibitor. | ||
| M7065 | NU9056 | Histone Acetyltransferase |
| NU 9056 | ||
| NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor with an IC50 of 2 µM. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5. NU9056 induces apoptosis of prostate cancer cells. | ||
| M7126 | PF CBP1 | Epigenetic Reader Domain |
| PF CBP1 is a selective CBP/p300 bromodomain inhibitor. | ||
| M7509 | UNC0642 | Histone Methyltransferase |
| UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. | ||
| M7538 | Tenalisib | PI3K |
| RP6530 | ||
| Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively. | ||
| M7577 | ML-7 hydrochloride | Others |
| ML-7 HCl | ||
| ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM) and TRPC6 channel (IC50>10 μM). | ||
| M8328 | RBx-0597 | Others |
| RBx-0597 is a potent, competitive inhibitor of DPP-IV (IC50 = 30 nM), that displays selectivity or 150 and 300 fold over DDP-VIII and DDP-IX, respectively. | ||
| M8671 | UCPH-102 | Others |
| UCPH-102 is a selective inhibitor of the Excitatory Amino Acid Transporter subtype-1 (EAAT1, GLAST) with an IC50 value of 420 nM for EAAT1 and >300 μM for EAAT2-5. | ||
| M9141 | SGC-CBP30 | Epigenetic Reader Domain |
| Sgc-cbp30 is a potent and highly selective CBP/ P300 bromine domain inhibitor (Kd of 21 nM and 32 nM against CBP and P300, respectively), which is 40 times more selective than BRD4 [BRD4(1)]. Sgc-cbp30 strongly reduces the secretion of IL-17A in Th17 cells and has anti-inflammatory effects. | ||
| M9152 | CPI-637 | Epigenetic Reader Domain |
| CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively. | ||
| M9482 | PD-168077 maleate | Dopamine Receptor |
| PD-168077 maleate is a potent D4 dopamine receptor agonist (Ki = 8.7 nM), with > 400-fold and > 300-fold selectivity over D2 / D3 subtypes, respectively. | ||
| M9561 | A-485 | Histone Acetyltransferase |
| A-485 is a potent and selective HAT inhibitor of p300/CBP in vitro with an IC50 of 10 nM in a p300 TR-FRET assay and 3 nM in a CBP TR-FRET assay with selectivity > 1000-fold over closely related HATs. | ||
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