E1/E2/E3 Enzyme Inhibitor

E1/E2/E3 Enzyme Inhibitors (118):

Cat. No.	Product Name	Effect	Purity

HY-100487

TAK-243	Inhibitor	98.38%
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.

HY-10029

Nutlin-3a	Inhibitor	98.89%
Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC₅₀=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.

HY-111789

Subasumstat	Inhibitor	98.56%
Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.

HY-15676

Idasanutlin	Inhibitor	99.93%
Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC₅₀ of 6 nM.

HY-50696

Nutlin-3	Inhibitor	99.06%
Nutlin-3 is a commercial available p53-MDM2 inhibitor, with K_i of 90 nM.

HY-157435

PELI1-IN-1	Inhibitor
PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumor effect.

HY-158171

Cbl-b-IN-17	Inhibitor
Cbl-b-IN-17 (Example-40) is an inhibitor of Cbl-b with an IC₅₀ value <100 nM.

HY-156382

SPOP-IN-1	Inhibitor
SPOP-IN-1 is a selective SPOP E3 ubiquitin ligase inhibitor. SPOP-IN-1 leads to the accumulation of tumor suppressors PTEN and DUSP7 and decreased levels of phosphorylated AKT and ERK in clear-cell renal cell carcinoma.

HY-12296

Navtemadlin	Inhibitor	99.61%
Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC₅₀ of 0.6 nM. Navtemadlin binds to MDM2 with a K_d of 0.045 nM.

HY-129395

Mezigdomide	Inhibitor	98.62%
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.

HY-108702

ML-792	Inhibitor	99.90%
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).

HY-13296

PYR-41	Inhibitor	≥98.0%
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC₅₀ of < 10 μM, with little activity at E2 and E3.

HY-114166

2-D08	Inhibitor	98.44%
2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC₅₀ of 0.49 nM.

HY-114312

MD-224	Inhibitor	98.47%
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC₅₀ value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent. MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-18658

Siremadlin	Inhibitor	99.87%
Siremadlin (NVP-HDM201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.

HY-136339

Cbl-b-IN-1	Inhibitor	99.68%
Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC₅₀ <100 nM.

HY-10959

RG7112	Inhibitor	99.91%
RG7112 is a potent, selective, first clinical, 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.

HY-139514

RB-3	Inhibitor	99.42%
RB-3, a polycomb repressive complex 1 (PRC1) inhibitor, binds to RING1B-BMI1f, with a K_d of 2.8 μM.

HY-N0170

Indole-3-carbinol	Inhibitor	98.87%
Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).

HY-N0077

Ginkgolic Acid	Inhibitor	99.92%
Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC₅₀ of 3.0 μM in in vitro assay.

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