E1/E2/E3 Enzyme(E1/E2/E3泛素酶)

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.

Products for E1/E2/E3 Enzyme

Cat.No. 产品名称 Information
GC33039 COH000
(1R,4S)-二甲基1-((R)-1-(苯基氨基)-2-(对甲苯基)乙基)-7-氧杂二环[2.2.1]庚-2,5-二烯-2,3-二羧酸
An inhibitor of SUMO-activating enzyme
GC32911 CTX1
CTX1是一种新型小分子p53激活剂。
GC32881 Milademetan (DS-3032)
DS-3032
Milademetan (DS-3032) (DS-3032) 是一种特异性的、具有口服活性的 MDM2 抑制剂，用于研究急性髓性白血病 (AML) 或实体瘤。 Milademetan (DS-3032) (DS-3032) 诱导 G1 细胞周期停滞、衰老和凋亡。
GC32814 DKM 2-93 DKM2-93是相对选择性的UBA5抑制剂，IC50值为430μM。
GC32737 TAK-243 (MLN7243)
MLN7243
A UAE inhibitor
GC32721 NSC232003
NSC232003是一种高效的可渗透细胞的UHRF1抑制剂，可抑制DNA甲基化，并破坏DNMT1/UHRF1相互作用。
GC19312 RO8994 An inhibitor of MDM2-p53 interaction
GC19268 NVP-HDM201
NVP-HDM201; HDM201
NVP-HDM201 (NVP-HDM201) 是一种有效的、口服生物利用度高且高度特异性的 p53-MDM2 相互作用抑制剂。
GC19257 MX69 An inhibitor of the MDM2 protein and XIAP RNA interaction
GC19088 CC122
Avadomide
A pleiotropic pathway modifier with anticancer activity
GC18561 TZ9 A Rad6B inhibitor
GC10408 2-D08 An inhibitor of sumoylation
GC10134 Ginkgolic Acid C15:1
银杏酸; Ginkgolic acid (15
An inhibitor of SUMOylation
GC18136 BH3I-1
BHI1; BH 3I1
An inhibitor of anti-apoptotic Bcl-2 proteins
GC11547 MI-773 (SAR405838)
MI-77301
An inhibitor of MDM2-p53 protein-protein interactions
GC11445 YH239-EE A prodrug form of YH 239
GC10940 PRT 4165
NSC600157
An inhibitor of PRC1 ubiquitin ligases
GC11869 SZL P1-41 SZL P1-41是一种特异性S期激酶相关蛋白2（Skp2）抑制剂。
GC12647 NVP-CGM097
CGM097
An inhibitor of the MDM2-p53 interaction
GC16368 Indole-3-carbinol
3-吲哚甲醇; I3C; 3-Indolemethanol
A natural phytochemical
GC17801 PYZD-4409 PYZD-4409 是泛素激活酶 UBA1 的特异性抑制剂，IC50 为 20 μM（无细胞酶测定）。 PYZD-4409 在恶性细胞中诱导细胞死亡并优先抑制原发性急性髓细胞白血病细胞的克隆形成。
GC16296 MI-773
(2'R,3S,4'S,5'R)-6-氯-4'-(3-氯-2-氟苯基)-2'-(2,2-二甲基丙基)-1,2-二氢-N-(反式-4-羟基环己基)-2-氧代螺[3H-吲哚-3,3'-吡咯烷]-5'-甲酰胺
MI-773 是一种有效的 MDM2-p53 蛋白-蛋白相互作用 (PPI) 抑制剂，对 MDM2 具有高结合亲和力 (Kd=8.2 nM)。 MI-773 具有抗肿瘤活性。
GC15771 PYR-41 An irreversible inhibitor of ubiquitin-activating enzyme
GC15828 AMG232
2-((3R,5R,6S)-5-(3-氯苯基)-6-(4-氯苯基)-1-((S)-1-(异丙基磺酰基)-3-甲基丁烷-2-基)-3-甲基-2-氧代哌啶-3-基)乙酸,AMG 232;AMG-232
An inhibitor of the MDM2 and p53 interaction
GC12508 Nutlin-3b
4-[[(4R,5S)-4,5-双(4-氯苯基)-4,5-二氢-2-[4-甲氧基-2-(1-甲基乙氧基)苯基]-1H-咪唑-1-基]羰基]-2-哌嗪酮
The less active enantiomer of (–)-nutlin-3
GC13590 SJ 172550
MDMX Inhibitor II
A small molecule inhibitor of MDMX
GC16371 Solasodine
澳洲茄铵,Purapuridine;Solancarpidine;Solasodin
An alkaloid with diverse biological activities
GC16055 SMIP004
N-(4-丁基-2-甲基苯基)乙酰胺,SMIP 004;SMIP-004
SMIP004 是一种 SKP2 E3 连接酶抑制剂，可下调 SKP2 并稳定 p27。 SMIP004 是人前列腺癌细胞的癌细胞选择性凋亡诱导剂。
GC11594 RG7388
RG 7388; RG-7388; ldasanutlin; Ro 5503781
An inhibitor of the MDM2-p53 interaction
GC13019 RG7112
[(4R,5S)-4,5-双(4-氯苯基)-2-[4-(1,1-二甲基乙基)-2-乙氧基苯基]-4,5-二氢-4,5-二甲基-1H-咪唑-1-基][4-[3-(甲磺酰基)丙基]-1-哌嗪基]甲酮,RG-7112;RG 7112
An inhibitor of the MDM2-p53 interaction
GC10470 Nutlin-3a chiral
Nutlin-3a;Nutlin 3a
Nutlin-3a 手性是 Nutlin-3 的活性异构体，是鼠类双微体 2 (MDM2) 拮抗剂，IC50 值为 0.09μM。
GC12117 JNJ-26854165 (Serdemetan)
N-[2-(1H-吲哚-3-基)乙基]-N'-(4-吡啶基)-1,4-苯二胺,JNJ 26854165
An antagonist of MDM2 action
GC16051 Nutlin-3
4-[[4,5-双(4-氯苯基)-4,5-二氢-2-[4-甲氧基-2-(1-甲基乙氧基)苯基]-1H-咪唑-1-基]羰基]-2-哌嗪酮,Nutlin 3,MDM2 Antagonist
A racemic mixture of (?)-nutlin-3 and (+)-nutlin-3