Ubiquitin E3 Ligase Inhibitors |
|
Cat. No. |
Product |
Activity |
0652 |
Thalidomide |
Binds
cereblon; also TNF-α synthesis inhibitor |
2443 |
RITA |
MDM2-p53 interaction inhibitor |
3503 |
HLI 373 |
Hdm2 inhibitor; activates p53-dependent transcription |
3984 |
Nutlin-3 |
MDM2 antagonist; inhibits MDM2-p53 interaction |
4375 |
SMER 3 |
Selective inhibitor of E3 ubiquitin ligase |
5047 |
PRT 4165 |
Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination |
5076 |
SZL P1-41 |
Selective Skp2 inhibitor; suppresses E3 ligase activity |
5191 |
PTC 209 |
Bmi-1 inhibitor; antitumor |
5332 |
SP 141 |
High affinity MDM2 inhibitor |
5397 |
A01 |
High affinity Smurf1 inhibitor; enhances BMP signaling |
5433 |
Heclin |
HECT E3 ubiquitin ligase inhibitor |
5636 |
GS 143 |
β-TrCP1 ligase inhibitor |
5747 |
Apcin |
Cdc20 inhibitor; inhibits Cdc20-substrate interaction |
6075 |
Nutlin 3a |
MDM2 antagonist; active enantiomer of Nutlin-3 (Cat.
No. 3984) |
6156 |
VH 298 |
High-affinity inhibitor of VHL |
6719 |
YH 239-EE |
MDM2 inhibitor; disrupts MDM2-p53 interaction |
6904 |
Idasanutlin |
Potent MDM2 inhibitor; inhibits MDM2-p53 interaction |
7055 |
WS 383 |
Potent, selective and reversible DCN1-UBC12 interaction
inhibitor |
7089 |
CSN5i-3 |
Potent and selective CSN5 (COP9 signalosome) inhibitor |
7192 |
SMIP 004 |
SKP2 (S-phase kinase-associated protein 2) inhibitor;
upregulates p27 and arrests cell cycle in G1 phase |
7289 |
Nimbolide |
RNF114 inhibitor |
7498 |
SPOP-i-6lc |
SPOP E3 ubiquitin ligase inhibitor |
7542 |
SJ 1008066 |
MAGE-A11 inhibitor disrupts MAGE-A11:PCF11 interaction |
|
|
|
Ligands |
|
|
Cat. No. |
Product |
Activity |
7476 |
EN 219 |
Covalent
RNF114 ligand |
|
|
|
Degraders |
|
|
Cat. No. |
Product |
Activity |
6416 |
CM 11 |
Homo-PROTAC® for
self-degradation of pVHL30 |
7219 |
CRBN PROTAC® 14a |
Cereblon Degrader (PROTAC®) |
6948 |
CRBN-6-5-5-VHL |
Potent and selective cereblon Degrader; cell-permeable |
|
|
|
Controls |
|
|
Cat. No. |
Product |
Activity |
6157 |
cis VH
298 |
Negative
control for VH 298 |
7532 |
CSN5i-3-NEG |
Negative control for CSN5i-3 (Cat. No. 7089) |
7716 |
N-methylated pomalidomide |
Pomalidomide negative control; also functionalized cereblon
ligand for generating Degrader negative controls |
|
|
|
Others |
|
|
Cat. No. |
Product |
Activity |
7662 |
Azurin p28 peptide |
Binds p53 and
inhibits COP1-mediated ubiquitination of p53 |
7483 |
BDY FL VH032 |
High-affinity VHL fluorescent probe for TR-FRET and FP assays |
7287 |
FAM-DEALA-Hyp-YIPD |
Fluorescent HIF-1α peptide; can be used to evaluate the effect
of VHL binding on degradation activity |
7452 |
FAM-DEALAHypYIPMDDDFQLRSF |
Fluorescent HIF-1α peptide; can be used to evaluate the effect
of VHL binding on degradation activity |
7627 |
FITC-labelled Keap1-Nrf2
probe |
Fluorescent Keap1-Nrf2 peptide |
6782 |
Indisulam |
Molecular glue; pre-mRNA splicing modulator |
6305 |
Lenalidomide |
Cereblon binder; induces ubiquitination and degradation of CK1α
by E3 ubiquitin ligase |
5131 |
NAB 2 |
Protects against α-synuclein toxicity; promotes
Rsp5/Nedd4-dependent endosomal transport |
6302 |
Pomalidomide |
Cereblon binder; also TNF-α inhibitor and antiangiogenic |
7288 |
Thalidomide-Cyanine 5 |
High affinity cereblon fluorescent probe |