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E1/E2/E3 Enzyme

Ubiquitin (UB) is a protein modifier that regulates many essential cellular processes. To initiate protein modification by UB, the E1 enzyme activates the C-terminal carboxylate of UB to launch its transfer through the E1-E2-E3 cascade onto target proteins. The E1 enzyme is the activating enzyme, to which ubiquitin is attached in an ATP-dependent reaction by a thioester bond. The E2 enzyme is the conjugating enzyme, to which the ubiquitin is transferred from the E1. The E3 is the ubiquitin ligase, which directly or indirectly catalyzes the transfer of the ubiquitin to the target protein (the substrate), with the formation of an isopeptide bond.
Cat. No. 製品名 CAS No. Purity Chemical Structure
T6629 PYR-41 418805-02-4 98%
PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
T6965 RG7112 939981-39-2 98%
RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
T4253 Skp2 Inhibitor C1 432001-69-9 98%
Skp2 Inhibitor C1 (SKPin C1)(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation.
T6023 Nutlin-3a 675576-98-4 98%
Nutlin-3a ((−)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
T16699 PYZD-4409 423148-78-1 98%
PYZD-4409 is a selective UBA1 inhibitor with an IC50 of 20 μM. PYZD-4409 induces cell death in malignant cells and is preferentially cytotoxic to malignant cells...
T17187 TZ9 1002789-86-7 98%
TZ9 is a selective and potent Rad6 inhibitor with anticancer and anti-tumor activity.TZ9 inhibits Rad6B-induced ubiquitination of histone H2A.TZ9 induces cell cy...
T14569 BI8626 1875036-75-1 98%
BI8626 is a ubiquitin ligase HUWE1 inhibitor with protective effects against spontaneous desiccation syndrome in NOD/ShiLtj mice.BI8626 inhibits intracellular ch...
T16974 TAK-243 1450833-55-2 98%
TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM). TAK-243 blocks ubiquitin binding and disrupts mono-ubiquitin signa...
T11980 MD-224 2136247-12-4 100%
MD-224 is a highly potent and efficacious MDM2 degrader based on the proteolysistargeting chimera (PROTAC) concept,and as a new class of anticancer agent.
T2947 Indole-3-carbinol 700-06-1 100%
Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activatio...
T3317 SZL P1-41 222716-34-9 100%
SZL P1-41, a skp2 inhibitor, can prevent assembly of Skp2-Skp1 complexes. It selectively suppresses Skp2 SCF E3 ligase activity but exhibits no effect on the act...
T7889 C25-140 1358099-18-9 100%
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
T5199 COH000 1534358-79-6 96.91%
COH000 is a covalent and irreversible inhibitor of small ubiquitin-like modifier (SUMO)-activating enzyme and inhibited SUMOylation (IC50: ~ 0.2 μM in vitro).
T2243 Serdemetan 881202-45-5 97.13%
Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
T9500 M435-1279 1359431-16-5 97.16%
M435-1279 is a UBE2T inhibitor. M435-1279 blocks UBE2T-mediated degradation of RACK1, leading to inhibit the hyperactivation of Wnt/β-catenin signaling pathway.
T10703 Mezigdomide 2259648-80-9 97.21%
Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that often acts as a molecular glue. Mezigdomide ...
T12261 NSC232003 1905453-18-0 97.72%
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
T5555 Siremadlin 1448867-41-1 97.77%
Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
T7379 2-D08 144707-18-6 98%
2-D08 is a synthetic flavone that inhibits sumoylation, also inhibits Axl with an IC50 of 0.49 nM.2-D08 showed anti-aggregatory and neuroprotective effect.
T6585 SAR405838 1303607-60-4 98.04%
MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
PYR-41
T6629
PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2.
RG7112
T6965
RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
Skp2 Inhibitor C1
T4253
Skp2 Inhibitor C1 (SKPin C1)(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation.
Nutlin-3a
T6023
Nutlin-3a ((−)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
PYZD-4409
T16699
PYZD-4409 is a selective UBA1 inhibitor with an IC50 of 20 μM. PYZD-4409 induces cell death in malignant cells and is preferentially cytotoxic to malignant cells...
TZ9
T17187
TZ9 is a selective and potent Rad6 inhibitor with anticancer and anti-tumor activity.TZ9 inhibits Rad6B-induced ubiquitination of histone H2A.TZ9 induces cell cy...
BI8626
T14569
BI8626 is a ubiquitin ligase HUWE1 inhibitor with protective effects against spontaneous desiccation syndrome in NOD/ShiLtj mice.BI8626 inhibits intracellular ch...
TAK-243
T16974
TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM). TAK-243 blocks ubiquitin binding and disrupts mono-ubiquitin signa...
MD-224
T11980
MD-224 is a highly potent and efficacious MDM2 degrader based on the proteolysistargeting chimera (PROTAC) concept,and as a new class of anticancer agent.
Indole-3-carbinol
T2947
Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activatio...
SZL P1-41
T3317
SZL P1-41, a skp2 inhibitor, can prevent assembly of Skp2-Skp1 complexes. It selectively suppresses Skp2 SCF E3 ligase activity but exhibits no effect on the act...
C25-140
T7889
C25-140 is a small-molecule inhibitor of TRAF6-Ubc13.
COH000
T5199
COH000 is a covalent and irreversible inhibitor of small ubiquitin-like modifier (SUMO)-activating enzyme and inhibited SUMOylation (IC50: ~ 0.2 μM in vitro).
Serdemetan
T2243
Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
M435-1279
T9500
M435-1279 is a UBE2T inhibitor. M435-1279 blocks UBE2T-mediated degradation of RACK1, leading to inhibit the hyperactivation of Wnt/β-catenin signaling pathway.
Mezigdomide
T10703
Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that often acts as a molecular glue. Mezigdomide ...
NSC232003
T12261
NSC232003 is a highly potent and cell-permeable inhibitor of UHRF1.
Siremadlin
T5555
Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
2-D08
T7379
2-D08 is a synthetic flavone that inhibits sumoylation, also inhibits Axl with an IC50 of 0.49 nM.2-D08 showed anti-aggregatory and neuroprotective effect.
SAR405838
T6585
MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
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