| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S2881 | Homo-PROTAC cereblon degrader 1 | Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3. |
|
|
| S8300 | CC-885 |
CC-885 is a novel cereblon (CRBN) modulator. This compound selectively promotes CRBN- and p97-dependent PLK1 Ubiquitination and degradation. |
|
|
| S4925 | SMER3 | SMER3, the small-molecule enhancer of rapamycin (SMER), is an inhibitor of the Skp1-Cullin-F-box (SCF)Met30 Ubiquitin ligase with IC50 of 51 nM. | ||
| E1427 | MRT-2359 | MRT-2359 is a potent degrader of GSPT1. It exhibits anti-tumour activity in non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cells. | ||
| E7042 | SMIP004 | SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells. | ||
| E7619 | VH032 | VH032 is a potent and selective VHL ligand used in PROTACs that binds to the VHL E3 ligase with a Kd of 185 nM and disrupts the VHL:HIF-α interaction. By stabilising HIF-α, it activates the hypoxic response and serves as a tool for developing therapies targeting hypoxia signalling. | ||
| E1957 | NX-1607 (Cbl-b-IN-3) | NX-1607 (Cbl-b-IN-3) is an oral inhibitor of Casitas B-lineage lymphoma proto-oncogene B (CBL-B), which is an E3 Ubiquitin ligase and a key regulator of T, NK, and dendritic cell activation and suppresses their anti-tumour functions. NX-1607 enhances antigen recall, reduces T cell exhaustion, and increases cytokine production in response to T cell receptor stimulation, thereby counteracting suppressive signals from the tumour microenvironment. | ||
| E1216 | Heclin | Heclin is an inhibitor of HECT-type E3 ubiquitin ligase with an IC50 of 6.8, 6.3, and 6.9 μM for Smurf2, Nedd4, and WWP1 HECT domains, respectively. | ||
| S9889 | dCBP-1 | dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP by hijacking the E3 ubiquitin ligase CRBN, also is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression. | ||
| S0322 | BC-1215 | BC-1215 is an inhibitor of F-box protein 3 (Fbxo3, a ubiquitin E3 ligase component) with IC50 of 0.9 μg/mL and LC50 of 87 μg/ml for IL-1β release. This compound inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6. | ||
| E5844New | NSC2805 | NSC2805 is a potent inhibitor of WWP2 ubiquitin ligase with an IC50 of 0.38 μM. It is used in cancer research for studying WWP2-associated pathways. | ||
| S9832 | CC-90009 | CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation. | ||
| E1847 | GBD-9 | GBD-9 is a double-mechanism efficient degrader of BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). This compound acts both as a PROTAC molecule to induce the degradation of BTK and as a Molecular Glue to degrade GSPT1. It exhibits anti-proliferative effects, inhibiting cancer cell survival. | ||
| S0097 | (S,R,S)-AHPC (MDK7526) | (S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC is potentially useful for the targeted degradation of the Androgen Receptor. (S,R,S)-AHPC can be connected to the ligand for protein such as BCR-ABL1 by a linker to form PROTACs such as GMB-475. GMB-475 induces the degradation of BCR-ABL1 with IC50 of 1.11 μM in Ba/F3 cells. | ||
| S0345 | Smurf1-IN-A01 | Smurf1-IN-A01 can inhibit Smurf1-mediated Smad1/5 degradation and accelerate BMP-2 signal responsiveness with a Kd of 3.664 nM. | ||
| S3502 | (S,R,S)-AHPC-PEG4-NH2 hydrochloride | (S,R,S)-AHPC-PEG4-NH2 hydrochloride (VH032-PEG4-NH2 hydrochloride, VHL Ligand-Linker Conjugates 4 hydrochloride, E3 ligase Ligand-Linker Conjugates 7) is a PROTAC E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker. | ||
| S1015 | Thalidomide-OH | Thalidomide-OH (Cereblon ligand 2, E3 ligase Ligand 2) is a presumed hydroxylated thalidomide metabolite, with weak antiangiogenic activity (the average inhibition rate of vessel density was 14% in 100 μg), also can be applicable to the recruitment of CRBN protein. | ||
| E1300 | SJ6986 | SJ6986 is a CRBN modulator and specifically degrades GSPT1/2, with a DC50 of 2.1 nM (Dmax 99%) for GSPT1. | ||
| E0071 | MuRF1-IN-1 | MuRF1-IN-1 is a muscle ring finger protein-1 (MuRF1) inhibitor that attenuates skeletal muscle atrophy and dysfunction in cardiac cachexia. | ||
| E1937 | PT-179 | PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. This compound specifically binds CRBN, forms a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediates the degradation of the tagged protein. | ||
| E6651New | HGC652 | HGC652 is a TRIM21-dependent Molecular Glue degrader that binds the E3 Ubiquitin Ligase TRIM21 (Kd ≈ 0.06 µM) to induce a TRIM21–NUP98 ternary complex, driving the ubiquitination and selective degradation of nuclear pore complex proteins like NUP155, leading to nuclear pore collapse and cancer cell death. | ||
| E5839New | OICR-8268 | OICR-8268 is a potent, reversible and in-cell active DCAF1 ligand. It significantly binds to DCAF1 WDR domain with an Kd value of 38 nM. It serves as a promising starting point for developing chemical handles for DCAF1-based PROTACs targeting selective protein degradation as well as cancer therapeutics. | ||
| E5877New | LYG-409 | LYG-409 is a potent, selective, and orally bioavailable degrader of GSPT1, with a DC50 of 7.87 nM. It exhibits strong antiproliferative activity in KG-1 cells with an IC50 of 9.50 nM and demonstrates significant antitumor efficacy in vivo in models of acute myeloid leukaemia and prostate cancer. | ||
| E0351 | NSC232003 | NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor that binds to the 5mC binding pocket of the SRA domain of UHRF1. This compound modulates DNA methylation in a cellular context. | ||
| E1678 | SPOP-i-6lc | SPOP-i-6lc is a selective speckle-type POZ protein (SPOP) E3 ubiquitin ligase inhibitor with IC50 of 2.1 μM and 3.5 μM, in A498 and OS-RC-2 cell lines, respectively. In vitro, It suppresses viability and proliferation of A498 and OS-RC-2 kidney cancer cell lines. | ||
| E1087 | 5-amino-2,4-dimethylpyridine (5A-DMP) |
5-amino-2,4-dimethylpyridine (5A-DMP) is a novel tandem Tudor domain (TTD)-binding compound that inhibits the full-length UHRF1:LIG1 interaction in Xenopus egg extracts. |
||
| S2754 | Xevinapant (AT406) | Xevinapant (AT406, ARRY-334543, Debio1143, SM-406) is a potent Smac mimetic and an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to XIAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1. |
|
|
| S1172 | Serdemetan (JNJ-26854165) | Serdemetan (JNJ-26854165) acts as an HDM2 ubiquitin E3 Ligase antagonist and also induces early Apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed Apoptosis in the absence of functional p53. Phase 1. |
|
|
| S2781 | RITA | RITA induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and this compound also inhibits MDM2-p53 interaction by targeting p53. |
|
|
| S2225 | TAME | Tosyl-L-Arginine Methyl Ester (TAME) is an APC inhibitor. |
|
|
| S2678 | NSC 207895 | NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase. |
|
|
| S8979 | THAL-SNS-032 | THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to that binds the E3 ubiquitin ligase Cereblon (CRBN). |
|
|
| S8888 | GMB-475 | GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. | ||
| S6794 | Thalidomide-O-COOH (Cereblon ligand 3) | Thalidomide-O-COOH (Cereblon ligand 3, E3 ligase Ligand 3), a Thalidomide-based Cereblon (CRBN) ligand used in the recruitment of CRBN protein, can be connected to the ligand for protein by a linker to form PROTACs (Proteolysis Targeting Chimera). |