About 23 results found for searched term "EF-24" (0.145 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M6127 | TD-4208 | AChR/AChE |
| Revefenacin; GSK1160724 | ||
| Revefenacin (TD-4208; GSK1160724) is a novel and potent muscarinic receptor antagonist that has a high affinity and long residence time at the M3 receptor, and demonstrates in vitro kinetic selectivity for M3 over M2 muscarinic receptor subtype and no meaningful off-target activity. | ||
| M7792 | EF-24 | ERK |
| EF24 | ||
| EF-24 is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. | ||
| M4708 | Herbacetin | Others |
| Herbacetin is a natural flavonoid found in flaxseed and has a variety of pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects. Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor that binds directly to Asp44, Asp243 and Glu384 on ODC. It is also an SGK1 inhibitor. | ||
| M8189 | STF-62247 | Autophagy |
| STF62247; STF 62247 | ||
| Stf-62247 is an autophagy inducer with selective cytotoxicity against VHL-deficient renal cell carcinoma, with IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively. Stf-62247 can trigger ADCD in glioblastoma cell lines (LN-229, MZ-54, GOS-3 and U343) by inducing dephosphorylation and inactivation of mTORC1. | ||
| M10645 | MS402 | Epigenetic Reader Domain |
| MS-402 | ||
| MS402 is a novel BD1-selective BET BrD inhibitor, inhibiting primarily Th17 cell differentiation with a little or almost no effect on Th1 or Th2 and Treg cells. MS402 has Ki values of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. | ||
| M10717 | JNJ-5207852 | Histamine Receptor |
| JNJ-5207852 IS HISTAMINE H3 RECEPTORS ARE SELECTIVELY EFFECTIVE ANTAGONISTS, WHICH ARE H AGAINST RATS AND HUMANS3 receptors pKi the values are 8.9 and 9.24, respectively. | ||
| M10824 | GSK2245035 | TLR |
| GSK2245035 is a highly potent, selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential stimulation of interferon type 1 (IFN). GSK2245035 for IFNα and TNFα pEC50 9.3 and 6.5, respectively. GSK2245035 effectively inhibits allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 has the potential for asthma. | ||
| M10851 | LY2922470 | Others |
| LY2922470 is an effective, selective, orally potent GPR40 agonist that acts on human GPR40, mouse GPR40, and rat GPR40 EC50 The values are 7 nM, 1 nM, and 3 nM, respectively. LY2922470 lowers blood glucose levels while significantly increasing insulin and GLP-1, potentially for use in the study of type 2 diabetes mellitus (T2DM). | ||
| M11180 | (+)-(3R,8S)-Falcarindiol | Antibiotic |
| (3R,8S)-Falcarindiol; 3(R),8(S),9(Z)-Falcarindiol | ||
| (+)-(3R, 8S)-Falcarindiol is polyacetylene obtained from carrots, has an antimycobacterial effect, the lowest inhibitory concentration of Mycobacterium tuberculosis H37Ra MIC and IC50 The values are 24 μM and 6 μM, respectively. Has anti-tumor and anti-inflammatory effects. | ||
| M11243 | CPI-169 | Histone Methyltransferase |
| CPI 169 R-enantiomer | ||
| Cpi-169 (CPI 169 R-Enantiomer) is a novel and effective EZH2 inhibitor, capable of inhibiting the activity of EZH2 WT, EZH2 Y641N and EZH1 with IC50 value of 0.24 nM, respectively. 0.51 nM and 6.1 nM. | ||
| M14493 | MSI-1436 lactate | Phosphatase |
| Trodusquemine lactate; Aminosterol-1436 lactate | ||
| MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM). | ||
| M21558 | ART812 | DNA/RNA Synthesis |
| ART812 is an orally effective DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 had an IC50 value of 240 nM for cell-based microhomologous mediated end-junction (MMEJ). | ||
| M24583 | Refanezumab | Others |
| GSK249320 | ||
| Refanezumab (GSK249320) is an IgG1-type humanized monoclonal antibody directed against myelin-associated glycoprotein (MAG). Refanezumab binds to MAG and blocks MAG-mediated inhibition of axonal regeneration. Refanezumab can cross the blood-brain barrier (BBB) in animal stroke models. Refanezumab has the potential for the enhancement of recovery of function poststroke. | ||
| M28156 | Samatasvir | Anti-infection |
| IDX719; IDX18719 | ||
| Samatasvir (IDX71) is a potent, orally active NS5A inhibitor of HCV replication. Samatasvir is effective and selective against infectious HCV and replicons, with EC50s falling within a tight range of 2 to 24 pM in genotype 1 through 5 replicons. | ||
| M29378 | MS177 | PROTAC |
| MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest. | ||
| M29388 | VB124 | Monocarboxylate Transporter (MCT) |
| VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism. | ||
| M30136 | 24-Methylenecholesterol | Transferase |
| Ostreasterol | ||
| 24-Methylenecholesterol (Ostreasterol), a natural marine sterol, stimulates cholesterol acyltransferase in human macrophages. 24-Methylenecholesterol possess anti-aging effects in yeast. 24-methylenecholesterol enhances honey bee longevity and improves nurse bee physiology. | ||
| M30137 | 24(S)-Hydroxycholesterol | Liver X Receptor |
| 24S-OHC; 24S-HC; Cerebrosterol | ||
| 24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators. | ||
| M30447 | RU 24969 hemisuccinate | 5-HT Receptor |
| RU 24969 hemisuccinate is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 hemisuccinate could decrease fluid consumption and increase forward locomotion. | ||
| M30511 | ABT-724 | Dopamine Receptor |
| ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile. | ||
| M30753 | LBW242 | IAP |
| LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells. | ||
| M30993 | Kazinol A | Others |
| Kazinol A induces cytotoxic effects in human bladder cancer cells, including the cisplatin-resistant T24R2. | ||
| M53535 | CEF14, EBV Rta Protein (28-37) | Anti-infection |
| CEF14, EBV Rta Protein (28-37) is the HLA A24-restricted epitope from Epstein-Barr Virus Rta protein (28-37). | ||
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