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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC77625 Naproxen Gilteritinib
Naproxen Gilteritinib is the active reference substance of Gilteritinib Gilteritinib is the target protein ligand of PROTAC degrader LWY713.
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DC77624 Nap-FF
Nap-FF is a cell-penetrating dipeptide that can be used in the preparation of hydrogel chemosensors and in the research of targeted drug delivery.
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DC77623 N-Acetyl-S-geranylgeranyl-L-cysteine
N-Acetyl-S-geranylgeranyl-L-cysteine is a Methyltransferase inhibitor. N-Acetyl-S-geranylgeranyl-L-cysteine inhibits beta 2 integrin-induced actin polymerization with an IC50 of 45 nM.
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DC77622 NA-17
NA-17 is a naphthalimide compound with anti-tumor activity and lower toxicity to normal cells like HL-7702 and WI-38. NA-17 exhibits a p53-dependent selective inhibition in various NSCLC cells, inducing the accumulation of active p53 in the mitochondria and nuclei of NSCLC cells. NA-17 can cause cell cycle arrest in the G1 phase, leading to apoptosis and cell death.
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DC77621 N-(3-Pyridyl)indomethacinamide
N-(3-Pyridyl)indomethacinamide is a derivative of Indomethacin hydrolysis in human FAAH-transfected HEK293 cells (IC50 of 360 nM).
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DC77620 MY-1576
MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo.
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DC77619 MU1920
MU1920 is an ATP-competitive, selective inhibitor for haspin with an IC50 of 6 nM. MU1920 exhibits good pharmacokinetic properties and metabolic stability in mouse plasma and microsomes without obvious anticancer effects, which can be used for development of chemical probes.
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DC77618 MU147
MU147 is an MRE11 nuclease inhibitor and chemical probe with anticancer activity, which is lethal to Ehrlich ascites tumor cells both in vitro and in vivo. MU147 also eliminates the double-strand break repair mechanism dependent on the MRE11 nuclease activity without impairing the activation of ATM. MU147 also impairs the degradation of nascent strands of stalled replication FOX and selectively affects brca2-deficient cells.
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DC77617 MU1409
MU1409 is an inhibitor of MRE11 nuclease with an IC50 of 12.1 μM. Additionally, MU1409 also inhibits FEN1 and EXO1, with IC50 values of 24.2 and 176.4 μM, respectively. MU1409 affects DNA repair in cells, preventing the degradation of stalled replication forks in BRCA2-deficient cells, making it a promising candidate for research on BRCA2 mutation-induced cancers.
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DC77616 MS9024
MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM.
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DC77615 MS8511 hydrochloride
MS8511 (hydrochloride) is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 (hydrochloride) reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 (hydrochloride) can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS).
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DC77614 MS7131
MS7131 is a USP1-recruiting DUBTACs. MS7131 effectively reduces histone H3 lysine 27 trimethylation and significantly suppresses the proliferation and clonogenicity of cancer cells.
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DC77613 MS1262-C3-amide-C10-amine
MS1262-C3-amide-C10-amine is a E3 Ligase Ligand-Linker Conjugates. MS1262-C3-amide-C10-amine incorporates a GLP ligand for the E3 ligase SPOP, and a PROTAC linker. MS1262-C3-amide-C10-amine can be used to design PROTACs such as MS479.
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DC77612 MS-073
MS-073 (CP162398) is a P-glycoprotein (P-gp) inhibitor. MS-073 reverses multidrug resistance in drug-resistant cells by competitively inhibiting drug binding to P-glycoprotein.
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DC77611 MRL828
MRL828 combines a Tau pathology-binding ligand and modified guanine moiety based on the ATTEC technology to selectively designate aggregated tau proteins for clearance via the ALP. MRL828 decreases intracellular Tau aggregates and promotes the secretion of Tau.
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DC77610 MRK-990
MRK-990 is the inhibitor for PRMT that inhibits PRMT5 and PRMT9 with IC50 of 30 nM and 10 nM.
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DC77609 MR44397
MR44397 is a WD40 repeat (WDR) 5 ligand, can be used for cancer research.
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DC77608 MP-010
MP-010 is a FKBP12 ligand that regulates cytosolic calcium by stabilizing RyR channel activity. MP-010 promotes functional improvement in SOD1G93A amyotrophic lateral sclerosis (ALS) mice, as evidenced by improved motor coordination, increased integrity of neuromuscular junctions, and significantly enhanced survival of spinal motor neurons. MP-010 can be used for research in the field of neurological diseases.
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DC77607 MNN-02-155
MNN-02-155 is a bivalent molecular glue with with dual binding to p300/CBP and BCL6. MNN-02-155 induces potent activation of the BCL6-target reporter gene and cell death. MNN-02-155 can be used for the study of diffuse large B cell lymphomas (DLBCLs).
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DC77606 MMB-4
MMB-4 is an oxime that can reactivate cholinesterases that have been inactivated by exposure to organophosphates such as Sarin or Soman.
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DC77605 MLS000389544
MLS000389544 is a selective and potent methylsulfonylnitrobenzoate thyroid hormone receptor β (TRβ) antagonist that blocks the association of TRβ with steroid receptor coactivator 2 (SRC2).
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DC77604 MI-888
MI-888 is an orally active MDM2 inhibitor with a Ki of 0.44 nM. MI-888 can inhibit the MDM2-p53 interaction. MI-888 has favorable pharmacokinetic properties and anti-tumor activity.
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DC77603 MI-883
MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC50=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC50=0.1 μM). MI-883 stimulates CAR LBD assembly (EC50=0.38 µM) and CAR3 variant activation (EC50=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC50=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models.
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DC77602 MI-1063
MI-1063 is an inhibitor for DMD-2, that blocks the MDM2-p53 interaction, and activates the tumor suppressor function of p53. MI-1063 inhibits the growth of cancer cell RS4-11 and MV4-11 with IC50 of 179 nM and 93 nM. MI-1063 can be used as target protein ligand in synthesis of PROTAC degrader MD-265.
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DC77601 MethADP trisodium
MethADP (Adenosine 5'-(α,β-methylene)diphosphate) trisodium is a CD73 inhibitor. MethADP trisodium can be used for the research of ATP-adenosine pathway.
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DC77600 Metamizole hemimagnesium
Metamizole (Dipyrone) hemimagnesium is an anti-inflammatory and antioxidant agent with the property of reducing body temperature. Metamizole hemimagnesium can decrease the levels of C-reactive protein (CRP) and interleukin 6 (IL-6). It is also an orally active cyclooxygenase (COX) inhibitor. Metamizole hemimagnesium can inhibit cell proliferation and promote apoptosis. It can be used in the research of inflammation and fever.
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DC77599 MEL23
MEL23 is a MDM2 E3 ligase inhibitor that blocks the E3 ligase activity of the MDM2-MDMX complex. MEL23 inhibits Mdm2 and p53 ubiquitination in cells, reduce viability of cells with wild-type p53. MEL23 stabilizes MDM2 via a mechanism independent of p53 transcription.
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DC77598 MeCY5-NHS ester
MeCY5-NHS estera is a reactive dye. MeCY5-NHS estera can be used for the labeling of proteins and nucleic acids.
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DC77597 Mebolazine
Mebolazine binds to the androgen receptor and produce androgenic and anabolic activity.
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DC77596 Me-(S,R,S)-AHPC-CO-C5-N3
Me-(S,R,S)-AHPC-CO-C5-N3 is an E3 ligase ligand-linker conjugate composed of a VHL ligand and a linker . Me-(S,R,S)-AHPC-CO-C5-N3 can be used for synthesis of PROTACs, such as PROTAC CG167.
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