About 33 results found for searched term "MR-L2" (0.087 seconds)
Cat.No. | Name | Target |
---|---|---|
M1710 | Flavopiridol | CDK |
HMR-1275; Alvocidib; L86-8275 | ||
Flavopiridol (Alvocidib) is a competitive broad-spectrum CDK inhibitor with IC50 of 30,170,100 nM against CDK1, CDK2 and CDK4, respectively. | ||
M22466 | Emraclidine (CVL-231) | AChR/AChE |
CVL-231 | ||
Emraclidine (CVL-231) is a potential best-in-class, muscarinic M4 receptor-positive modulator (PAM) that crosses the blood-brain barrier.Emraclidine can be used in studies related to neurological disorders. | ||
M50194 | MRGPRX4 modulator-2 | MRGPR |
MRGPRX4 modulator-2 is a potent MRGPR X4 modulator with antagonistic activity against MRGPRX4 and an IC50 < 100 nM.MRGPRX4 modulator-2 can be used in studies related to autoimmune diseases. | ||
M58458 | MR-L2 | PDE |
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM. | ||
M2328 | Pirfenidone | TGF-beta/Smad |
AMR69; S-7701 | ||
Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone inhibits TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β in CCL-64 cells. Pirfenidone (AMR69) attenuates CCL2 and CCL12 production in fibrocyte cells. | ||
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. | ||
M4787 | Euphorbia-factor-L1 | Others |
Euphorbia Factor L1, a diterpenoid compound, can reduce the protein and mRNA levels of Bcl-2, PI3K, AKT and mTOR, and up-regulate the protein levels of Caspase-9 and Caspase-3. There was no effect on caspase-9 and caspase-3 protease. Euphorbia Factor L1 can induce autophagy and has anti-cancer, anti-adipogenesis, anti-osteoclast formation and multiple drug resistance regulation effects. | ||
M10593 | MRTX1133 | Ras |
MRTX-1133 | ||
MRTX1133 is a first-in-class, potent and highly selective KRAS G12D inhibitor. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. | ||
M6999 | MRS 1706 | Adenosine Receptor |
MRS 1706 is a potent and selective A 2B inverse agonist. | ||
M7000 | MRS 2179 tetrasodium salt | P2 Receptor |
MRS 2179 tetrasodium salt is a selective P2Y 1 antagonist. | ||
M7002 | MRS 2279 | Others |
MRS 2279 is a selective, high affinity P2Y 1 antagonist. | ||
M7003 | MRS 2500 tetraammonium salt | Others |
MRS 2500 tetraammonium salt is a extremely potent and selective P2Y 1 antagonist. | ||
M8533 | CCG-203971 | Ras |
CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. | ||
M8679 | IMR-1 | Notch |
IMR-1 is a first-in-class, cell-permeable inhibitor of the Notch transcription activation complex, with an IC50 of 26 μM. IMR-1 prevents Maml1 from recruiting to the Notch ternary complex (NTC) in chromatin, inhibits transcription of Notch target genes, and has antitumor activity. | ||
M11331 | UC2288 | Mdm2 |
UC2288 is a novel p21 attenuator with cellular permeability and oral activity (relatively selective activity for P21), based on the structural synthesis of sorafenib. UC2288 down-regulated the expression of P21 mRNA and reduced the level of P21 protein independently of p53, and had little effect on the stability of P21 protein. UC2288 did not inhibit VEGFR2 and Raf kinases, even at 10 μM. | ||
M8769 | Tasimelteon | Melatonin Receptor |
BMS-214778; VEC-162 | ||
Tasimelteon (BMS-214778) is a Dual Melatonin Receptor Agonist (DMRA) recently approved (Hetlioz) for the treatment of Non-24-hour sleep–wake disorder, a disorder primarily found in the totally blind, where a lack of normal synchronization between the 24-hour light–dark cycle and the endogenous circadian rhythm causes it to drift out of alignment with conventional sleep–wake schedules. | ||
M9428 | MRTX849 (Adagrasib) | Ras |
Adagrasib; MRTX-849 | ||
MRTX849 (Adagrasib) is a potent, highly selective, oral available KRAS G12C inhibitor. | ||
M9542 | TMRM Perchlorate | Fluorescent Dye |
T668 | ||
TMRM Perchlorate is a cell-permeant cationic lipophilic red fluorescent dye (λex=530 nm, λem=592 nm). | ||
M9957 | Finerenone | Mineralocorticoid Receptor |
BAY94-8862 | ||
Finerenone (BAY 94-8862) is a third generation selective, oral active, non-steroidal halocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone showed good selectivity (>500-fold) compared to glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (AR). Finerenone has potential applications in the study of heart and kidney diseases, such as type 2 diabetes and chronic kidney disease. | ||
M11021 | (rel)-AR234960 | ERK |
(rel)-AR234960 is the relatively active configuration of AR234960. AR234960 is a non-peptide MAS (a G protein coupling receptor) agonist that upregulates CTGF mRNA and protein levels through the ERK1/2 signaling pathway in HEK293-MAS cells and adult myocardial fibroblasts. | ||
M13577 | MRT68921 dihydrochloride | ULK |
MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. | ||
M13884 | MRS 1754 | Adenosine Receptor |
MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats. | ||
M14052 | CCG-100602 | Ras |
CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF. | ||
M14054 | MRTX-1257 | Ras |
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. | ||
M15037 | Recombinant Mouse IP-10/CXCL10 (E. coli) | Cytokines and Growth Factors |
Small inducible cytokine B10; CXCL10 | ||
Interferon inducible protein 10 (IP-10)/CXCL10 was originally thought to be an IFN-γ- inducible gene in monocytes, fibroblasts, and endothelial cells. LPS, IL-1β, TNF-α, IL-12 and virus can also induce the expression of IP-10 mRNA. Protein structure: CXCL10 (ILE22-PRO98), Accession # :Q548V9. | ||
M14590 | MRT67307 | IκB/IKK |
MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells. | ||
M15038 | Recombinant Human IP-10/CXCL10 (E. coli) | Cytokines and Growth Factors |
Small inducible cytokine B10; CXCL10 | ||
IP-10 /CXCL10, also known as CXCL10, was originally thought to be an IFN-γ- induced gene in monocytes, fibroblasts, and endothelial cells. LPS, IL-1β, TNF-α, IL-12 and virus can also induce the expression of IP-10 mRNA. Expressed with an N-terminal Met. CXCL10 (VAL22-PRO98), Accession # :P02778. | ||
M19411 | Cafestol | ERK |
Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activatio䲧瓰Ỵ瓱��㧀 | ||
M20998 | PMX-53 | Complement System |
3D53; PMX53; Ac-Phe-[Orn-Pro-dCha-Trp-Arg] | ||
PMX-53 is a potent CD88 (C5aR) antagonist with an IC50 of 20 nM, it inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC50 values of 22 nM and 75 nM, respectively. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. | ||
M21029 | MRE-269 | Immunology/Inflammation |
ACT-333679 | ||
MRE-269 (ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor. | ||
M21503 | MRTX849 acid | Ras |
MRTX849 acid can be used to synthesize PROTAC LC-2. LC-2 is a potent, first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50, between 0.25 and 0.76 μM). | ||
M21518 | MRTX849 ethoxypropanoic acid | PROTAC Linker |
MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2. | ||
M21722 | Felezonexor (CBS9106) | CRM1 |
CBS9106; SL-801 | ||
Felezonexor (CBS9106; SL-801) is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity without affecting CRM1 mRNA levels. Felezonexor is also a reversible inhibitor of XPO1, inhibits nuclear export by covalently binding to Cys528 as well as by inducing the degradation of XPO1. |
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