E1/E2/E3 Enzyme Inhibitor

Heclin (Standard) is the analytical standard of Heclin (HY-110204). This product is intended for research and analytical applications. Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits Smurf2, Nedd4, WWP1 (IC₅₀ values are 6.8, 6.3, 6.9 μM) and can be used for the research of gastric cancer.

Milademetan (Standard) is the analytical standard of Milademetan (HY-101266). This product is intended for research and analytical applications. Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.

DKM 2-93 (Standard) is the analytical standard of DKM 2-93 (HY-101836). This product is intended for research and analytical applications. DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC₅₀ of 430 μM.

TAK-243 (Standard) is the analytical standard of TAK-243 (HY-100487). This product is intended for research and analytical applications. TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.

GS143 (Standard) is the analytical standard of GS143 (HY-110261). This product is intended for research and analytical applications. GS143 is a selec-tive IκBα ubiquitination inhibitor with an IC₅₀ of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup-presses NF-κB acti-va-tion and tran-scrip-tion of tar-get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.

ML-792 (Standard) is the analytical standard of ML-792 (HY-108702). This product is intended for research and analytical applications. ML-792 is a potent and selective inhibitor of SAE/SUMO1 and SAE/SUMO2 in enzymatic assays (IC₅₀ values of 3 and 11 nM, respectively) compared with NAE/NEDD8 and UAE/ubiquitin (IC₅₀> values of 32 μM and >100 μM, respectively).

HLI98C is a ubiquitin ligase inhibitor. HLI98C inhibits p53 ubiquitylation. HLI98C inhibits HDM2 auto-ubiquitylation.

Alrizomadlin (Standard) is the analytical standard of Alrizomadlin (HY-101518). This product is intended for research and analytical applications. Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.

RG7112 (Standard) is the analytical standard of RG7112 (HY-10959). This product is intended for research and analytical applications. RG7112 is a potent, selective, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC₅₀ of 18 nM and a K_d of 11 nM for binding to MDM2.

Nutlin-3 (Standard) is the analytical standard of Nutlin-3. This product is intended for research and analytical applications. Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.

NAcM-OPT (Standard) is the analytical standard of NAcM-OPT (HY-111505). This product is intended for research and analytical applications. NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.

Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity.

NX-1607 (Cbl-b-IN-3) (GMP) is a GMP-grade NX-1607 (HY-141432). GMP-grade small molecules can be used as adjuvant agents in cell therapy. NX-1607 (GMP) enhances antigen recall, reduces T cell exhaustion and increases cytokine production. NX-1607 is an inhibitor of Cbl-b (an E3 enzyme).

SMER3 (Standard) is the analytical standard of SMER3 (HY-10949). This product is intended for research and analytical applications. SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCFMet30.

Idasanutlin (Standard) (RG7388 (Standard)) is the analytical standard of Idasanutlin (HY-15676). This product is intended for research and analytical applications. Idasanutlin (RG7388) is an orally bioavailable MDM2 inhibitor with an IC₅₀ of 6 nM. Idasanutlin disrupts MDM2-p53 binding, stabilizes and activates p53, triggering cell cycle arrest, apoptosis, and reduced cancer cell viability. Idasanutlin reduces EGFR protein expression and phosphorylation, suppresses downstream SHP2, MEK1/2, ERK1/2, AKT, mTOR, p70(S6K1), and S6 signaling. Idasanutlin induces mitochondrial ROS production, drives p38 MAPK phosphorylation, upregulates NOXA, and mediates caspase-3-dependent apoptosis and gasdermin E-mediated pyroptosis. Idasanutlin can be used for the research of TP53-mutant non-small cell lung cancer, T-cell acute lymphoblastic leukemia, colorectal carcinoma, melanoma, diffuse large B-cell lymphoma, mantle cell lymphoma, non-Hodgkin lymphoma, severe fever with thrombocytopenia syndrome, neuroblastoma, acute lymphoblastic leukemia, relapsed or refractory acute myeloid leukemia, osteosarcoma, solid tumors, and hematological tumors.

VHL Ligand 38 (Compound 1) is a competitive E3 ubiquitin-protein ligase VHL inhibitor with IC₅₀s of 4.1 and 7.0 μM in 1% and 10% DMSO, respectively. VHL Ligand 38 contains a hydroxyproline residue and an isoxazolylacetamide fragment. VHL Ligand 38 significantly inhibits the binding of a fluorescent peptide derived from HIF1α (FAM-DEALA-Hyp-YIPD) (HY-P5908F) to VHL.

Subasumstat (Standard) is the analytical standard of Subasumstat (HY-111789). This product is intended for research and analytical applications. Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.

Mezigdomide (Standard) is the analytical standard of Mezigdomide (HY-129395). This product is intended for research and analytical applications. Mezigdomide (CC-92480), a cereblon E3 ubiquitin ligase modulating agent (CELMoD), acts as a molecular glue. Mezigdomide shows high affinity to cereblon, resulting in potent antimyeloma activity.

SZL P1-41 (Standard) is the analytical standard of SZL P1-41 (HY-100237). This product is intended for research and analytical applications. SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.

Teslexivir hydrochloride (Standard) is the analytical standard of Teslexivir (hydrochloride) (HY-109045A). This product is intended for research and analytical applications. Teslexivir (BTA074) hydrochloride is a potent antiviral agent. Teslexivir hydrochloride is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir hydrochloride can be used for condyloma research.