Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
29 Results for "
Cullin E3 ligase
" in MedChemExpress (MCE) Product Catalog:
Products (29)
29 Results for "Cullin E3 ligase" in MCE Product Catalog:
27
Research Areas:
Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
1
1 Cited Publications
Homo-PROTAC pVHL30 degrader 1 is a Homo-PROTAC autodegraders targeting the von Hippel-Lindau E3 ubiquitin ligase (VHL), with Kd values of 11 nM and 25 nM for pVHL19-EloBC and pVHL30-EloBC, respectively. Homo-PROTAC pVHL30 degrader 1 induces Cullin2 depletion, promotes VHL dimerization to form a ternary complex, and drives proteasome-dependent and CRL2-VHL-like ubiquitination-dependent autodegradation. Homo-PROTAC pVHL30 degrader 1 does not trigger hypoxic responses, and only causes extremely mild stabilization of hypoxia-inducible factor α subunits. Homo-PROTAC pVHL30 degrader 1 can be used in studies related to cervical cancer and osteosarcoma .
1
1 Cited Publications
Cat. No.: HY-163638
CAS No.: 3094209-54-5
Research Areas:
BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent BRD4 Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of BRD4 by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer research .
Cat. No.: HY-49444
CAS No.: 793719-01-4
Target:
Research Areas:
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .
Cat. No.: HY-172615
CAS No.: 3033019-04-1
Research Areas:
AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies .
Research Areas:
MD13 is a MIF PROTAC degrader with a DC50 of approximately 100 nM. MD13 induces ubiquitination and degradation of MIF by recruiting the Cereblon Cullin RING E3 ubiquitin ligase complex. MD13 inactivates the MAPK pathway and induces G2/M phase cell cycle arrest. MD13 exhibits antiproliferative effects in 3D tumor spheroid models. MD13 can be used in lung cancer-related research .
Research Areas:
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Research Areas:
Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
Cat. No.: HY-173002
CAS No.: 3107482-42-5
Target:
Research Areas:
MS9024 is a selective DNMT1 Molecular glue degrader with a DC50 of 35 nM. MS9024 degrades DNMT1 in a concentration-, time- and proteasome-dependent manner without altering DNMT1 transcription. MS9024 mediates degradation via HECT E3 ligase and/or UHRF1, but not via lysosomes or Cullin RING E3 ligase. MS9024 can be used in the research of colorectal cancer, breast cancer and non-small cell lung cancer .
Cat. No.: HY-14658S
CAS No.: 1219177-18-0
Cat. No.: HY-178472
CAS No.: 3106831-75-5
Research Areas:
AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 can form a stable ternary complex with Aurora A kinase and HSP90, recruiting cullin family E3 ubiquitin ligases and MDM2 to mediate the ubiquitination and proteasome degradation of Aurora A kinase. AurAP14 increases p53 levels and decreases C-MYC levels; AurAP14 induces Apoptosis. AurAP14 can be used in the study of non-small cell lung cancer .
Cat. No.: HY-175321
Target:
Research Areas:
PROTAC c-Met degrader-6 is an orally active c-Met PROTAC degrader with DC50 values of 0.52 nM (EBC-1) and 0.45 nM (Hs746T), respectively. PROTAC c-Met degrader-6 induces potent targeted degradation of c-Met via the ubiquitin-proteasome system by bridging the target protein c-Met and the Cullin-CRBN E3 ubiquitin ligase to form a ternary complex, thereby inducing tumor cell cycle arrest and apoptosis. PROTAC c-Met degrader-6 can be used in the research of various MET-driven cancers (such as gastric cancer, liver cancer, non-small cell lung cancer, etc.) .
Cat. No.: HY-178122
Research Areas:
THNAN69 is a PROTAC degrader targeting LIMK2, which efficiently degrades ectopically expressed EGFP-LIMK2 in live HuCCT1 cells with a DC50 of 1 nM. THNAN69 induces isoform-specific ubiquitin-mediated degradation of LIMK2 by recruiting the CRBN E3 ligase, forming a stable ternary complex with LIMK2 and CRBN; this degradation process depends on the activity of cullin-RING ligase. THNAN69 does not reduce phosphorylated cofilin levels, as LIMK1 can compensate for the loss of LIMK2; it also stimulates compensatory activation of the Rho signaling pathway including PAK1/2 and ROCK1/2. THNAN69 serves as a selective chemical probe for dissecting the LIMK2 isoform-dependent biological mechanisms. THNAN69 can be used in the research of cholangiocellular carcinoma and acute lymphoblastic leukemia .
Cat. No.: HY-179582
Target:
Research Areas:
PROTAC DNPH1 Degrader 1 is a potent PROTAC DNPH1 degrader with a DC50 of 28 nM. PROTAC DNPH1 Degrader 1 mediates proteasome- and VHL-dependent DNPH1 knockdown, drives DNPH1 ubiquitination and proteasomal degradation. PROTAC DNPH1 Degrader 1 can be used for the research of brca1 mutant cancer .
Cat. No.: HY-176070
Target:
Research Areas:
HRG038 is a covalent CUL4 DCAF16-base PROTAC-liked BRD4 degrader. HRG038 induces proteasome- and Cullin E3 ligase-dependent degradation, covalently targets cysteine residue C173 on DCAF16 to mediate BRD4 degradation, and induces reduction in BRD3 levels. HRG038 shows selective loss of the short BRD4 isoform over the long isoform in non-cancer cells, degrades both BRD4 isoforms in breast cancer cells, and does not impair cell viability in non-cancer cells. HRG038 can be used for the research of breast cancer .
Cat. No.: HY-173274
CAS No.: 3056259-55-0
Target:
Research Areas:
CB039 is a RBM39 molecular glue degrader with an IC50 of 36.7 nM against HCT-116 cells. CB039 induces RBM39 degradation in a dose- and time-dependent manner. This process depends on the Cullin-RING E3 ubiquitin ligase complex (CRL) and proteasome, and promotes the recruitment of RBM39 to the DCAF15-DDB1 complex with an IC50 of 594 nM. CB039 causes abnormal RNA splicing, reduces CEP192 protein levels, induces G2/M phase cell cycle arrest and mitotic spindle disorder. CB039 can be used in studies on RBM39-targeted protein degradation and colorectal cancer-related mechanisms .
Cat. No.: HY-162240
Target:
Research Areas:
SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research .
Cat. No.: HY-169148
Target:
Research Areas:
YT117R is a PROTAC degrader targeting BRD4. YT117R binds stereoselectively and site-specifically to the cysteine residue C1113 of DCAF1 to form a covalent interaction. YT117R promotes BRD4 degradation via a DCAF1-dependent, proteasome- and cullin-RING E3 ligase-mediated process. YT117R exhibits stereoselective activity dependent on wild-type DCAF1, which is blocked by the DCAF1 C1113A mutation .
Cat. No.: HY-P703242
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: CUL1; Cullin-1; Cullin 1; CUL-1; RBX1; E3 Ubiquitin-Protein ligase RBX1; Ring-Box 1; RING Finger Protein 75; RNF75; RING-Box Protein 1; ROC1; Ring-Box 1, E3 Ubiquitin Protein ligase; Regulator Of Cullins 1; ZYP Protein; BA554C12.1; Protein ZYP; E3 Ubiquit
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P703243
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: CUL1; Cullin-1; Cullin 1; CUL-1; RBX1; E3 Ubiquitin-Protein ligase RBX1; Ring-Box 1; RING Finger Protein 75; RNF75; RING-Box Protein 1; ROC1; Ring-Box 1, E3 Ubiquitin Protein ligase; Regulator Of Cullins 1; ZYP Protein; BA554C12.1; Protein ZYP; E3 Ubiquit
Species:
Human
Source:
Sf9 insect cells
- 1
- 2
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
