About 31 results found for searched term "EAD1" (0.123 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M10224 | YAP-TEAD-IN-1 TFA | YAP |
| YAP-TEAD-IN-1 TFA is a competitive inhibitor of YAP-TEAD interaction with IC50 of 25 nM. | ||
| M11552 | DREADD agonist 21 | AChR/AChE |
| DREADD Agonist 21 is an effective agonist for human muscarinic acetylcholine M3 receptor (hM3Dq) (EC50=1.7 nM). | ||
| M20628 | EAD1 | Autophagy |
| EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells. | ||
| M50386 | YAP-TEAD-IN-1 | YAP |
| YAP-TEAD-IN-1 is a potent and competitive inhibitor of YAP–TEAD interaction (IC50=25 nM). | ||
| M2215 | Niraparib (MK-4827) | PARP |
| MK-4827 | ||
| MK-4827 (Niraparib) is a selective PARP1/2 inhibitor with an IC50 value of 3.8 nM/2.1 nM that increases the formation of PARP-DNA complexes through inhibition of PARPase activity, leading to DNA damage, apoptosis, PARP-1-dependent cell death (parthanatos) and cell death. Strong effector activity when acting on cancer cells harboring mutant BRCA-1 and BRCA-2. It is more than 330-fold more selective than PARP3, V-PARP and Tank1. | ||
| M2403 | Apoptosis Activator 2 | Caspase |
| 1-(3,4-Dichlorobenzyl)-1H-indole-2,3-dione | ||
| Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells. | ||
| M2557 | Ezatiostat | Apoptosis |
| TER199, TLK199 | ||
| Ezatiostat (TER199, TLK199) is a glutathione analog inhibitor of glutathione S-transferase (GST) P1-1. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. | ||
| M3892 | BMH-21 | DNA/RNA Synthesis |
| BMH-21 is a first-in-class DNA intercalator that binds to high-frequency GC-rich sequences in ribosomal DNA genes and can effectively and rapidly inhibit the transcription of RNA polymerase I (Pol I), leading to degradation of the Pol I catalytic subunit RPA194 and non-phosphorylation of histone H2AX. H2AX is not phosphorylated.BMH-21 has broad and potent antitumor activity in NCI60 cancer cell line and inhibits tumor growth in vivo. | ||
| M7504 | CIL56 (CA3) | Ferroptosis |
| CIL56 (CA3) is a potent and selective ferroptosis inducer, it has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. | ||
| M8199 | SR11237 | RAR/RXR |
| SR11237 is a retinoid X receptor (RXR) selective agonist without any RAR activity that leads to the formation of RXR/RXR homodimers and activation of reporter genes containing RXR response elements. In addition, SR11237 significantly promotes reprogramming. | ||
| M8686 | CCF642 | Apoptosis |
| CCF642 is a cell-permeable protein disulfide isomerase (PDI) inhibitor that exhibits 100-fold higher potency than PACMA 31 (by di-E-GSSG assay) via an alternative mode of action that most likely involves PDI active-site CGHCK motifs instead of cysteine known to be targeted by PACMA 31. | ||
| M10782 | APG-1387 | IAP |
| APG-1387 is a divalent SMAC mimetic that is an IAP antagonist that blocks the activity of the IAP family of proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins as well as caspase-3 activation and PARP lysis, leading to apoptosis. APG-1387 can be used for the study of hepatocellular carcinoma, ovarian cancer and nasopharyngeal carcinoma. | ||
| M11354 | INCB086550 | PD-1/PD-L1 |
| PD-1/PD-L1-IN-8 | ||
| INCB086550 selectively inhibited PD-L1 with IC50 of 3.1 nM, 4.9 nM and 1.9 nM for human, rhesus monkey and rat pD-L1, respectively. INCB086550 could not inhibit the binding of PD-L2 to PD-1 at 10 μM. INCB086550 significantly inhibits the PD-1/PD-L1 signaling axis by binding to PD-L1 protein, leading to PD-L1 dimerization and internalization, and has good tumor suppressive effect in a variety of mouse tumor models. | ||
| M14889 | GNF4877 | DYRK |
| GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells). | ||
| M14911 | CH6953755 | Src-bcr-Abl |
| CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo. | ||
| M14937 | TED-347 | YAP |
| TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. | ||
| M20724 | RCM-1 | IL Receptor/Related |
| Robert Costa Memorial drug-1 | ||
| RCM-1 is a nontoxic inhibitor of Forkhead box M1 (FOXM1) that suppresses goblet cell metaplasia and prevents IL-13 and STAT6 signaling in allergen-exposed mice. RCM-1 decreases carcinogenesis and nuclear β-catenin. | ||
| M21087 | VT103 | YAP |
| VT103, a VT101 analog, is a selective and orally active TEAD1 protein palmitoylation inhibitor that can be used in cancer research. VT103 inhibits the transcription of YAP/TAZ-TEAD promoted gene, blocks the auto-palmitoylation of TEAD, and interferes with the interaction between YAP/TAZ and TEAD. | ||
| M21088 | K-975 | YAP |
| K-975 is a potent, selective and orally active TEAD inhibitor that strongly inhibits protein-protein interactions between YAP1/TAZ and TEAD. | ||
| M21133 | VT107 | Others |
| The pan-TEAD transcription factor inhibitor VT-104 binds to a lipid pocket on TEAD, preventing its auto-palmitoylation, similar to the previously highlighted TEAD inhibitors. | ||
| M21662 | MGH-CP1 | Apoptosis |
| MGH-CP1 is a potent and orally active TEAD2 and TEAD4 auto-palmitoylation inhibitor with IC50s of 710 nM and 672 nM, respectively. MGH-CP1 can decrease the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. | ||
| M22501 | SM-102 | Liposome |
| SM102 | ||
| ALC-0159 is a lipid conjugate of polyethylene glycol that can be used as an immunosuppressant SM-102 is an ionizable aminolipid with a terminal hydroxyl group in the head group, which reduces the hydration of the head group and improves hydrogen bonding interactions with nucleic acids, thus enhancing transfection.SM-102 can be used for the preparation of lipid nanoparticles (LNPs), as well as for the lipid nanoparticle delivery of | ||
| M24552 | Gevokizumab | IL Receptor/Related |
| Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II). | ||
| M25436 | EGR240 | Transferase |
| ERG240 is a selective inhibitor of branched-chain aminotransferase 1 (BCAT1) with an IC50 of 0.1-1nM. ERG240 leads to decreased oxygen consumption and glycolysis through the down regulation of IRG1 expression, which leads to decrease itaconate production in human macrophages. | ||
| M27726 | Clitocine | Apoptosis |
| Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity. | ||
| M28586 | LML134 | Histamine Receptor |
| LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders. | ||
| M28641 | Tesirine | Drug-Linker Conjugates for ADC |
| SG3249 | ||
| Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity. | ||
| M28703 | TL4-12 | MAPKAPK2/MAP3K/MAP4K |
| TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM). | ||
| M28775 | UNC-2170 | Others |
| UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC50=29 µM; Kd=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB). | ||
| M28781 | Trimetrexate trihydrochloride | Dihydrofolate reductase |
| CI-898 trihydrochloride | ||
| Trimetrexate (CI-898) trihydrochloride is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. | ||
| M29144 | Claficapavir | HIV Protease |
| A1752 | ||
| Claficapavir (A1752) is a specific nucleocapsid protein (NC) inhibitor with an IC50 around 1 μM. Claficapavir strongly binds the HIV-1 NC (Kd=20 nM) thereby inhibiting the chaperone properties of NC and leading to good antiviral activity against the HIV-1. | ||
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