About 32 results found for searched term "ATIC-IN-1" (0.259 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M42871 | ATIC-IN-1 acetate | Others |
| ATIC-IN-1 acetate is an inhibitor targeting to Aminoimidazole carboxamide ribonucleotide transformylase/inosine monophosphate cyclohydrolase (ATIC) dimerization with a Ki value of 685 nM. | ||
| M42875 | ATIC-IN-1 | Others |
| ATIC-IN-1is an inhibitor targeting to Aminoimidazole carboxamide ribonucleotide transformylase/inosine monophosphate cyclohydrolase (ATIC) dimerization with a Ki value of 685 nM. | ||
| M2241 | Adapalene | RAR/RXR |
| CD271; Differin; ADA | ||
| Adapalene is a third-generation topical retinoid, it is a potent RAR agonist, with AC50 values of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene is also an MST1 agonist. | ||
| M2370 | Adrenalone hydrochloride | Adrenergic Receptor |
| Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors. | ||
| M4083 | Ginsenoside-F1 | Cytochrome P450 (e.g. CYP17) |
| 20(S)-Ginsenoside F1 | ||
| Ginsenoside F1 is an enzymatically modified derivative of Ginsenoside Rg1. Ginsenoside F1 competently inhibits CYP3A4 and has a weak inhibitory effect on CYP2D6. | ||
| M4507 | Scopolin | Sirtuin |
| Scopolin is a coumarin isolated from the roots of Arabidopsis. Scopolin mitigated hepatic steatosis by activating sirT1-mediated signaling cascades. | ||
| M4510 | Madecassic-acid | NO Synthase |
| Madecassic acid was isolated from Centella asiatica (umbelliferae). Madecassic acid showed inhibition of iNOS, COX-2, TNF-α, IL-1beta and IL-6, and had anti-inflammatory effect by down-regulation of NF-κB activation in RAW 264.7 macrophages. | ||
| M4886 | Selamectin | Parasite |
| Selamectin is an antiparasitic agent and insect repellent that activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent filariasis, lymphatic filariasis and nematode infection. Selamectin is also an effective p-glycoprotein substrate and inhibitor with IC50 of 120 nM. | ||
| M6255 | JPH203 | Autophagy |
| KYT-0353 | ||
| JPH203, a selective L-type amino acid transporter 1 (LAT1) inhibitor, shows a dramatic inhibition of leucine uptake (IC50=0.06 µM) and cell growth (IC50=4.1 µM) in human colon cancer cells (HT-29), human oral cancer cells (YD-38) and leukemic cells. | ||
| M6466 | AS 1269574 | GPR/FFAR |
| AS1269574 is a potent, orally active GPR119 agonist with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates the TRPA1 cation channel and stimulates glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induced pancreatic β cells to secrete glucose-dependent insulin only under high glucose conditions. AS1269574 has potential for type 2 diabetes research. | ||
| M7305 | SKPin C1 | Others |
| SKPin-C1 | ||
| SKPin C1 is a inhibitor of Skp2-mediated p27 degradation. SKPin C1 induces p27 accumulation in metastatic melanoma cell lines. SKPin C1 promotes G1/S cell cycle arrest in T47D cells and LNCaP cells. SKPin C1 induces G2/M cell cycle arrest in MCF-7 cells. | ||
| M8594 | BRD3308 | HDAC |
| BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23 times more selective to HDAC3 than HDAC1 (IC50:1.26 μM) or HDAC2 (IC50:1.34 μM). BRD3308 inhibits pancreatic β cell apoptosis induced by inflammatory cytokines or glucolipid toxic stress and increases functional insulin release. BRD3308 also activates HIV-1 transcription and disrupts HIV-1 latency. | ||
| M8666 | Urolithin A | ERK |
| Urolithin A is a naturally occurring compound produced by the metabolism in the body of vegetable tannins (ellagic acid and ellagitannins) found in food. It is also a mitochondrial modulator, regulating mitochondrial function in hematopoietic stem cells, as well as restoring blood regeneration in aging hematopoietic stem cells. In addition, Urolithin A is a ligand for the Aromatic Hydrocarbon Receptor (AhR), which promotes the anti-tumor function of CD8+ cytotoxic T-lymphocytes (CTLs) in an AhR-independent manner. Moreover, Urolithin A directly binds to ERK1/2 kinase, enhances its activation, and subsequently phosphorylates and activates the autophagy initiation factor ULK1, thereby promoting autophagy. | ||
| M10590 | Alofanib (RPT835) | FGFR |
| RPT835 | ||
| Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. | ||
| M10727 | Pulrodemstat benzenesulfonate | Histone demethylase |
| CC-90011 benzenesulfonate | ||
| CC-90011 (Pulrodemstat) benzenesulfonate is a potent, selective, reversible and orally active lysine-specific demethylase-1 (LSD1) inhibitor,IC50 0.25 nM. CC-90011 benzenesulfonate has less enzymatic inhibition of LSD2, MOA-A and MAO-B. CC-90011 benzenesulfonate induces differentiation of acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells and has potent anti-cancer activity. | ||
| M10848 | LP-922761 | Others |
| LP-922761 is a potent, selective, orally active AAK1 inhibitor in enzymatic and cell analysis IC50 4.8 nM and 7.6 nM, respectively. LP-922761 also inhibits BMP-2-induced protein kinase (BIKE),IC50 24 nM. LP-922761 has no significant activity against cell GAK, opioids, epinephrine alpha2, or GABAa receptors. | ||
| M13400 | Recombinant Human UBA5 (E.coli, N-6His) | Cytokines and Growth Factors |
| Ubiquitin-like modifier-activating enzyme 5 | ||
| UBA5 is a member of the ubiquitin activated E1 family and UBA5 subfamily. Ubiquitin and ubiquitin-like proteins are identified as covalently binding to a variety of cellular substrates through a three-step enzymatic pathway. Ubiquitin activase (E1) plays a crucial role in the first step of activating ubiquitin or ubiquitin-like proteins in the ubiquitination pathway. | ||
| M13672 | AES-135 | HDAC |
| AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM. | ||
| M14051 | 1A-116 | Ras |
| 1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer. 1A-116 prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes . | ||
| M14195 | Dehydronitrosonisoldipine | Calcium Channel |
| Dehydronitrosonisoldipine is a calcium channel antagonist. Dehydronitrosonisoldipine acts mainly by blocking SARM1 activation but not its enzymatic activities. Dehydronitrosonisoldipine inhibits SARM1 and axon degenration (AxD) by covalently modifying cysteines, also inhibits the Vincristine-activated cADPR production in neurons. | ||
| M14480 | Toddalolactone | PAI-1 |
| Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM. | ||
| M21185 | BMS-986318 | Farnesoid X Receptor |
| BMS-986318 is a potent non-bile acid FXR agonist with an EC50 of 53 and 350 nM in FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has suitable ADME properties and is effective in a mouse model of hepatic cholestasis and fibrosis with bile duct ligation.BMS-986318 can be used in nonalcoholic steato BMS-986318 can be used in non-alcoholic steatohepatitis (NASH) studies. | ||
| M21564 | RIPK1-IN-7 | RIPK |
| Ripk1-in-7 is a receptor interacting protein kinase 1 (RIPK1) inhibitor with Kd value of 4 nM and IC50 value of 11 nM. RIPK1-IN-7 showed good antimetastatic activity in experimental B16 melanoma lung metastasis model. | ||
| M21638 | Recombinant Human GPNMB (HEK293, C-6His) | Cytokines and Growth Factors |
| Glycoprotein Non-Metastatic Melanoma Protein B | ||
| Recombinant Human GPNMB (Glycoprotein Non-Metastatic Melanoma Protein B) is produced by Mammalian expression system and the target gene encoding Ala22-Pro486 is expressed with a 6His tag at the C-terminus. Osteoactivin is an intracellular glycoprotein belongs to the NMB/pMEL-17 family, which is asscociated with cell endosomal/lysomal compartments. | ||
| M21645 | Tipranavir | HIV Protease |
| PNU-140690 | ||
| Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. | ||
| M21671 | Recombinant Mouse/Rat VEGF-C Protein (HEK293, aa 108-223, His Tag) | Cytokines and Growth Factors |
| Vascular endothelial growth factor C | ||
| Recombinant Mouse/Rat VEGF-C Protein is a dimeric glycoprotein, as a ligand for two receptors, VEGFR-3 (Flt4), and VEGFR-2. VEGF-C may function in angiogenesis of the venous and lymphatic vascular systems during embryogenesis. Measured in a cell proliferation assay using human umbilical vein endothelial cells (HUVEC), the ED50 for this effect is typically 0.1-0.8 μg/mL. | ||
| M27600 | TH10785 | Others |
| TH10785 is a DNA glycosylase 1 (OGG1) activator, TH10785 can interact with the phenylalanine-319 and glycine-42 amino acids of OGG1 and increase the enzyme activity, generates β, δ-lyase enzymatic function. TH10785 can control the catalytic activity mediated by a nitrogen base within its molecular structure. TH10785 can be used for the research of various diseases and aging connected with DNA oxidative lesions. | ||
| M27608 | BMS-593214 | Others |
| BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT). | ||
| M28196 | 12-Hydroxynevirapine | Metabolite/Endogenous Metabolite |
| 12-hydroxy-NVP; 12-OH-NVP | ||
| 12-Hydroxynevirapine (12-hydroxy-NVP; 12-OH-NVP) is a major oxidative metabolite of Nevirapine. Nevirapine is a non-nucleoside reverse transcriptase inhibitor indicated for the HIV-1 infections. Nevirapine causes idiosyncratic hepatotoxicity and mild-to-severe skin rashes. 12-Hydroxynevirapine, a non-reactive metabolite, can be bioactivated by sulphotransferases (SULTs) in the liver and skin, yielding the reactive species 12-Sulphoxy-nevirapine. | ||
| M28249 | AMG-1694 | Glucokinase (GK) |
| AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals. | ||
| M28363 | EVT801 | VEGFR/PDGFR |
| EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models. | ||
| M28373 | (±)-BI-D | HIV Protease |
| (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site. IC50 value: 2.4–2.9 μM(HIV-Luc infection of WT and Hdgfrp2 KO cells) [1] Target: integrase inhibitor in vitro: Approximately 2.4–2.9 μM of BI-D was required to inhibit 50% of HIV-Luc infection of WT and Hdgfrp2 KO cells, while the IC50 decreased dramatically, to 160–200 nM, in Psip1 and double-KO cells . | ||
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