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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
21 Results for "
Cullin Ring Ligase
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "Cullin Ring Ligase" in MCE Product Catalog:
226
Target:
Research Areas:
Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM. Pevonedistat induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat suppresses the growth of human tumour xenografts in mice .
226
226 Publications Verification
Synonyms: MLN4924 hydrochloride
Target:
Research Areas:
Pevonedistat (MLN4924) hydrochloride is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM. Pevonedistat hydrochloride induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat hydrochloride suppresses the growth of human tumour xenografts in mice .
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1 Cited Publications
Cat. No.: HY-174138
Target:
Research Areas:
NF-κB degrader 1 (Compound MD-1) is a NF-κB1 p105 subunit degrader. NF-κB degrader 1 shows anti-inflammatory activity (IC50 for inhibiting TNF-α is 2.02 μM, and for inhibiting NO is 5.40 μM). NF-κB degrader 1 induces p105 degradation dependent on the Cullin-RING ligase (CRL) SCFBTCP, suppressing NF-κB transcriptional activity. NF-κB degrader 1 is promising for research of inflammation-related diseases .
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 .
Cat. No.: HY-175756
CAS No.: 2901804-87-1
Target:
Research Areas:
SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4 DCAF16 and CRL1 FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer .
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-146397
CAS No.: 2760703-21-5
Target:
Research Areas:
TD-802 is a CRBN-recruiting PROTAC androgen receptor (AR) degrader with liver microsomal stability and in vivo pharmacokinetic properties. TD-802 exhibits weak degrading activity against the AR-V7 splice variant, and its degradation process depends on the ubiquitin-proteasome system and Cullin-Ring ubiquitin ligase. TD-802 inhibits the proliferation of AR-dependent prostate cancer cells and the growth of AR-positive prostate cancer tumors in in vivo xenograft models .
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-70062R
CAS No.: 905579-51-3
Synonyms: MLN4924 (Standard)
Research Areas:
Pevonedistat (Standard) is the analytical standard of Pevonedistat. This product is intended for research and analytical applications. Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM. Pevonedistat induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat suppresses the growth of human tumour xenografts in mice .
Cat. No.: HY-170983
MC-25B is a DCAF16-recruiting FKBP12 PROTAC degrader with a DC50 of 0.35 μM. MC-25B promotes the formation of a ternary complex with DCAF16 and nuclear-localized FKBP12_NLS, thereby mediating DCAF16-dependent degradation of FKBP12_NLS via the proteasome and Cullin-RING ligase pathway .
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-P703245
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: CUL3; Uncharacterized Protein CUL3; Cullin 3; KIAA0617; Cullin-3; NEDAUS; CUL-3; PHA2E; 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 Cull
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P705629
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: CUL2; CUL-2; Cullin 2; Testis Secretory Sperm-Binding Protein Li 238E; Cullin-2; 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;
Species:
Human
Source:
Sf9 insect cells
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-P703246
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: CUL4A; CUL-4A; Cullin 4A; Cullin-4B; Cullin-4A; 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
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
Cat. No.: HY-184151
Target:
Research Areas:
KBD-1 is a muscle-specific BRD4 PROTAC degrader with human KDs of 27.04 nM and 37.36 µM against BRD4 and KLHL4L, respectively. KBD-1 recruits the muscle-specific E3 ligase KLHL41, mediating Cullin-RING ligase (CRL)-dependent ubiquitination and proteasome degradation of BRD4. KBD-1 can be used for the research of myosarcoma .
Cat. No.: HY-183755
Target:
Research Areas:
YSA64 is an orally active RBM39-targeting molecular glue. YSA64 promotes degradation via formation of a DCAF15/DDB1 ternary complex, dependent on Cullin-RING E3 ligase and proteasome activity. YSA64 can be used for the research of acute myeloid leukemia and Ewing sarcoma .
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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
