41 results for "Ubiquitin Ligase (E3) Inhibitors" in 产品
Ubiquitin Ligase (E3) Inhibitors
Ubiquitin E3 ligases (EC 6.3.2.19) attach ubiquitin molecules onto lysine residues of proteins in order to target the protein for a specific cellular process, such as proteasomal degradation or an alteration in subcellular localization. In addition to the specific ubiquitin ligases such as MDM2, E3A and anaphase-promoting complex (APC), many other proteins also contain domains that possess ubiquitin ligase activity. Almost all known ubiquitin E3 ligases contain one of three domains: a HECT, ...
MDM2 antagonist; inhibits MDM2-p53 interaction
| Chemical Name: | (±)-4-[4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one |
| Purity: | ≥98% |
(+)-JQ1 based Degrader (PROTAC®) that preferentially degrades BRD4
| Chemical Name: | (2S,4R)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)- 4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% |
Cdc20 inhibitor; inhibits Cdc20-substrate interaction
| Chemical Name: | 3-(2-Methyl-5-nitroimidazol-1-yl)-N-(2,2,2-trichloro-1-phenylaminoethyl)propionamide |
| Purity: | ≥98% |
MDM2 antagonist; active enantiomer of Nutlin-3 (Cat. No. 3984)
| Chemical Name: | 4-[[(4S,5R)-4,5-bis(4-Chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-2-piperazinone |
| Purity: | ≥97% |
Cereblon binder; induces ubiquitination and degradation of CK1α by E3 ubiquitin ligase
| Chemical Name: | 3-(4-Amino-1,3-dihydro-1-oxo-2H-isoindol-2-yl)-2,6-piperidinedione |
| Purity: | ≥98% |
Potent and selective CSN5 (COP9 signalosome) inhibitor
| Chemical Name: | 3-(Difluoromethyl)-N-(6-((5S,6S)-6-hydroxy-6,7,8,9-tetrahydro-5H-imidazo[1,5-a]azepin-5-yl)-[1,10-biphenyl]-3-yl)-1-isopropyl-1H-pyrazole-5-carboxamide |
| Purity: | ≥98% |
Hdm2 inhibitor; activates p53-dependent transcription
| Chemical Name: | 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dione dihydrochloride |
| Purity: | ≥98% |
Selective inhibitor of E3 ubiquitin ligase
| Chemical Name: | 9H-Indeno[1,2-e][1,2,5]oxadiazolo[3,4-b]pyrazin-9-one |
| Purity: | ≥98% |
Selective Skp2 inhibitor; suppresses E3 ligase activity
| Chemical Name: | 3-(2-Benzothiazolyl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-1-benzopyran-4-one |
| Purity: | ≥98% |
β-TrCP1 ligase inhibitor
| Chemical Name: | 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid |
| Purity: | ≥98% |
High-affinity inhibitor of VHL
| Chemical Name: | (2S,4R)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% |
Cereblon binder; also TNF-α inhibitor and antiangiogenic
| Chemical Name: | 4-Amino-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione |
| Purity: | ≥98% |
(+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
| Chemical Name: | (6S)-4-(4-Chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide |
| Purity: | ≥98% |
Molecular glue; pre-mRNA splicing modulator
| Chemical Name: | N1-(3-Chloro-1H-indol-7-yl)-1,4-benzenedisulfonamide |
| Purity: | ≥98% |
Potent and selective cereblon Degrader (PROTAC®); cell-permeable
| Chemical Name: | (2S,4R)-1-((2S)-2-(5-((5-((6-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)hexyl)oxy)pentyl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥96% |
MDM2-p53 interaction inhibitor
| Alternate Names: | NSC 652287 |
| Chemical Name: | 5,5'-(2,5-Furandiyl)bis-2-thiophenemethanol |
| Purity: | ≥97% |
Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination
| Chemical Name: | 2-(3-Pyridinylmethylene)-1H-Indene-1,3(2H)-dione |
| Purity: | ≥98% |
High affinity MDM2 inhibitor
| Chemical Name: | 6-Methoxy-1-(1-naphthalenyl)-9H-pyrido[3,4-b]indole |
| Purity: | ≥98% |
HECT E3 ubiquitin ligase inhibitor
| Chemical Name: | N-(4-Acetylphenyl)-3-(5-ethyl-2-furanyl)-2-propenamide |
| Purity: | ≥98% |
Negative control for VH 298
| Chemical Name: | (2S,4S)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% |
(+)-JQ1 based PROTAC® with selectivity for BRD4
| Chemical Name: | (2S,4R)-1-(2R)-2-Acetamido-3-[[6-[2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetamido]hexyl]thio]-3-methylbutanoyl]-4-hydroxy-N-[4-(4-methylthiazol-5-yl)benzyl)pyrrolidinine-2-carboxamide |
| Purity: | ≥98% |
Homo-PROTAC® for self-degradation of pVHL30
| Chemical Name: | N1,N20-bis((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,6,9,12,15,18-hexaoxaicosanediamide |
| Purity: | ≥98% |
Multikinase Degrader (PROTAC®)
| Chemical Name: | N-(2-(2-(2-(4-(4-((5-Chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)piperazin-1-yl)ethoxy)ethoxy)ethyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamide |
| Purity: | ≥98% |
Negative control for TL 12-186 (Cat. No. 6524)
| Chemical Name: | N-(2-(2-(2-(4-(4-((5-Chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)piperazin-1-yl)ethoxy)ethoxy)ethyl)-2-((1,3-dioxo-2-(2-oxopiperidin-3-yl)isoindolin-4-yl)amino)acetamide |
| Purity: | ≥98% |
Potent MDM2 inhibitor; inhibits MDM2-p53 interaction
| Chemical Name: | 4-[[[(2R,3S,4R,5S)-3-(3-Chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxybenzoic acid |
| Purity: | ≥98% |
