About 31 results found for searched term "Ar-V7-IN-1" (0.13 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M57285 | Ar-V7-IN-1 | Androgen Receptor |
| Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications such as prostate cancer. | ||
| M3405 | AR-42 | HDAC |
| OSU-HDAC42; HDAC-42 | ||
| AR-42 is an HDAC inhibitor with IC50 of 30 nM. AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. | ||
| M3970 | Scutellarin | STAT |
| Scutellarin, an active flavone isolated from Scutellaria baicalensis, is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively. Scutellarin inhibited caspase-11 activation and pyroptosis in macrophages at least partly via regulating the PKA signaling pathway. | ||
| M6457 | AR-C 118925XX | P2 Receptor |
| ARC118925XX | ||
| AR-C 118925XX is a selective, competitive P2Y2 receptor antagonist. AR-C 118925XX is inactive against a panel of 37 other receptors at a concentration of 10 μM. AR-C 118925XX inhibits ATP-γS-induced mucin secretion in bronchial epithelial cells (IC50 = 1 μM). AR-C 118925XX inhibits P2Y2 receptor-induced β-arrestin translocation in vitro (pA2 = 37.2-51.3 nM). | ||
| M7177 | Quinine hydrochloride | Potassium Channel |
| Quinine hydrochloride is the hydrochloride form of Quinine, an alkaloid extracted from the bark of the cinchona tree, with antimalarial and antitumor activities, and an IC50 value of 60 ng/mL against P. falciparum strains passou and 107.8 ng/mL against P. falciparum strain 3CD7, respectively, and an inhibitor of potassium channels. Quinine hydrochloride is also a potassium channel inhibitor that inhibits voltage pulse-induced MT mSlo3 (KCa5.1) channel +100 mV currents, with an IC50 value of 169 μM. In addition, Quinine hydrochloride binds to purine nucleoside phosphorylase (PfNP) and PfNP with low nanomolar affinity. nucleoside phosphorylase (PfPNP) with low nanomolar affinity. | ||
| M8125 | Quinalizarin | Casein Kinase |
| Quinalizarin is a potent (IC50 = 110 nM), ATP-competitive, and highly selective (IC50 > 1 μM for CK1 and 72 other kinases) inhibitor of casein kinase II (CK2), with a Ki value of approximately 50 nM and an IC50 of 110 nM.Quinalizarin induces apoptosis in some cancer cells. Quinalizarin can induce apoptosis in some cancer cells.) | ||
| 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. | ||
| M8488 | Ophiopogonin D' | Sirtuin |
| Ophiopogonin D', isolated from the tuber of Ophiopogon japonicus, is a rare naturally occurring C29 steroid glycoside. Ophiopogonin D' has cytotoxic activity against two human tumor cell lines mG-63 and SNU387. Ophiopogonin D' can induce necrotic apoptosis of prostate cancer LNCaP cells by activating RIPK1. IC50 were 3.09 μM and 3.63 μM, respectively. SIRT1 is activated in a dose-dependent manner by Ophiopogonin D'. | ||
| M8758 | GW806742X | Necroptosis |
| GW806742X is an ATP site-targeing kinase inhibitor (IC50 in nM = 2/VEGFR2, 15/SRC, 47/C-FMS, 851/GSK3, 9016/ERBB2, 9120/FGFR) with potent antiproliferation activity against cancer cultures (IC50 in nM = 5/HUVEC-v, 424/HUVEC-b, 81/HEF, 453/MDA468, 470/A375P, 693/HT29, 734/PC3), GW806742X is now better known as Compound 1 for its anti-necroptosis activity via affinity interaction with ML | ||
| 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. | ||
| M9400 | Firmonertinib mesylate | EGFR/HER2 |
| Alflutinib mesylate; AST2818 mesylate | ||
| Firmonertinib (Alflutinib) mesylate is a potent, third generation EGFR inhibitor that targets both EGFR activating mutations and T790M thus leading to tumor growth inhibition. Firmonertinib (AST2818) has the potential for the research of non-small cell lung cancer (NSCLC). | ||
| M9906 | Astragalus Polysacharin | Adjuvants |
| Astragalus polysaccharide; APS | ||
| Astragalus Polysacharin is a natural product from Astragalus membranaeus, used as adjuvant, attenuates TNF-α-induced insulin resistance by suppressing miR-721 and activating PPAR-γ and PI3K/Akt in 3T3-L1 adipocytes. | ||
| 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). | ||
| M10863 | NCGC00378430 | Others |
| NCGC00378430 is a potent inhibitor of the SIX1/EYA2 interaction. NCGC00378430 partially reverses SIX1 overexpression-mediated transcription and metabolic profiling, and reverses SIX1-induced TGF-β signaling and epithelial-interstitial transformation (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in mouse models. | ||
| M11167 | A-381393 | Dopamine Receptor |
| A-381393 IS AN EFFECTIVE, SELECTIVE, AND BLOOD-BRAIN BARRIER-PERMEABLE dopamine D4 receptor Antagonist, dopamine D for humans4.4，D4.2 AND D4.7 receptors Ki The values are 1.5, 1.9, and 1.6 nM, respectively, with selectivity being D1，D2，D3，D5 MORE THAN 2700 TIMES THE DOPAMINE RECEPTOR. A-381393 VS. 5-HT2A MODERATE SELECTIVITY, Ki The value is 370 nM. | ||
| M11229 | Miransertib hydrochloride | Akt |
| ARQ-092 hydrochloride | ||
| Miransertib hydrochloride (ARQ-092 Hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with an IC50 of 2.7 nM for Akt1, Akt2, and Akt3, respectively. 14 nM and 8.1 nM. Miransertib hydrochloride is an effective inhibitor of AKT1-E17K mutant protein, and can be used in the study of PI3K/ AkT-driven tumors and Proteus syndrome. Miransertib hydrochloride effectively inhibited Leishmania. | ||
| M13379 | Guggulsterone | Apoptosis |
| Z/E-Guggulsterone | ||
| Guggulsterone is a plant sterol from the gum fat of the Commiphora Wightii tree. Guggulsterone is a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. | ||
| M14208 | Endovion | Chloride Channel |
| NS3728 | ||
| Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor. | ||
| M20765 | Lavendustin B | Integrase |
| Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). Lavendustin B is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1). | ||
| M20983 | Barnidipine | Calcium Channel |
| Libradin, Mepirodipine, Vasexten, YM-09730-5, Cyress, Hypoca, Oldeca | ||
| Barnidipine (Libradin, Mepirodipine, Vasexten, YM-09730-5, Cyress, Hypoca, Oldeca) is an antihypertensive drug that belongs to the dihydropyridine (DHP) group of calcium antagonist (CaA) with Ki of 0.21 nM for [3H]nitrendipine binding sites. | ||
| M21084 | GA-017 | YAP |
| GA-017 is a potent and selective inhibitor of LATS1 and LATS2 (large tumor suppressor kinase 1/2) with IC50 values of 4.10 and 3.92 nM, respectively.GA-017 is a cell proliferation activator.GA-017 promotes YAP/TAZ activation and nuclear translocation.GA-017 promotes cell growth in 3D culture conditions.GA-017 Enhances the formation of mouse intestinal organoid isolates. | ||
| M21158 | Vepdegestrant (ARV-471) | PROTAC |
| ARV471; PF-07850327 | ||
| Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer.ARV-471 is a heterobifunctional molecule that promotes the interaction between estrogen receptor alpha and intracellular E3 ligase complexes.ARV-471 causes ubiquitination and subsequent degradation of the estrogen receptor via the proteasome.ARV-471 potently degrades ER-positive The ER in breast cancer cell lines is potently degraded by ARV-471 with a DC50 value of approximately 2 nM. | ||
| M21407 | Autogramin-2 | Autophagy |
| Autogramin-2 effectively inhibited autophagy induced by starvation with an IC50 of 0.27 μM. Autogramin-2 also inhibited autophagy induced by Rapamycin (by inhibiting mTORC1) with an IC50 of 0.14 μM. | ||
| M21446 | AZD-9574 | PPAR |
| AZD-9574 is a best-in-class, potent, blood-brain barrier permeable PARP1 inhibitor that exhibits >8000-fold selectivity for PARP1 over PARP2/3/5a/6.AZD-9574 selectively inhibits PARP1 at the SSB site.AZD-9574 is an anticancer AZD-9574 is an anticancer compound that can be used in HRD+ breast cancer and advanced solid malignant tumor studies. | ||
| M21755 | Barasertib | Aurora Kinase |
| AZD1152 | ||
| Barasertib (AZD1152), a precursor of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells. | ||
| M24782 | Relatlimab | Others |
| BMS-986016 | ||
| Relatlimab (BMS-986016) is a human monoclonal antibody anti-LAG-3 antibody generated by immunization of transgenic mice bearing human immunoglobulin miniloci with recombinant LAG-3 protein. Relatlimab blocks LAG-3/MHC II interaction with an IC50 value of 0.67 nM and LAG-3/FGL1 interaction with an IC50 value of 0.019 nM. Relatlimab can be used in research of cancer. | ||
| M27613 | Irdabisant hydrochloride | Histamine Receptor |
| CEP-26401 hydrochloride | ||
| Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. | ||
| M27614 | Irdabisant | Histamine Receptor |
| CEP-26401 | ||
| Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment. | ||
| M27648 | Zardaverine | PDE |
| Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma. | ||
| M27649 | Onalespib lactate | HSP |
| Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC). | ||
| M27681 | ARN14494 | Apoptosis |
| ARN14494 is a potent and selective serine palmitoyltransferase (SPT) inhibitor, with an IC50 of 27.3 nM. ARN14494 affects the CNS in terms of anti-inflammation and neuroprotection. ARN14494 protects neurons from β-amyloid 1-42-induced neurotoxicity through a variety of mechanisms, including anti-oxidation, anti-apoptosis, and anti-inflammation. ARN14494 can be used for Alzheimer’s disease research. | ||
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