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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
17 Results for "
Cullin-RING ligase
" in MedChemExpress (MCE) Product Catalog:
Products (17)
17 Results for "Cullin-RING ligase" in MCE Product Catalog:
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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 .
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232 Publications Verification
Synonyms: MLN4924 hydrochloride
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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
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NF-κB p105 degrader-1 is a non-covalent, selective Molecular glue-like degrader targeting the NF-κB p105 subunit. NF-κB p105 degrader-1 induces proteasome-mediated degradation via the Cullin-RING ligase SCFβTrCP. NF-κB p105 degrader-1 inhibits LPS-induced production of NO and TNF-α. NF-κB p105 degrader-1 can be used in inflammation-related research .
Cat. No.: HY-172615
CAS No.: 3033019-04-1
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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 .
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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-173002
CAS No.: 3107482-42-5
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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
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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-178122
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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-70062R
CAS No.: 905579-51-3
Synonyms: MLN4924 (Standard)
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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-173274
CAS No.: 3056259-55-0
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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
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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
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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-183755
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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 .
Cat. No.: HY-184151
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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-10484R
CAS No.: 1160295-21-5
Synonyms: MLN4924 hydrochloride (Standard)
Research Areas:
Pevonedistat hydrochloride (Standard) is the analytical standard of Pevonedistat hydrochloride (HY-10484). This product is intended for research and analytical applications. 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 .
Cat. No.: HY-189074
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JN210 is a dual inhibitor of DCN1 and HDAC, with an IC50 of 94.26 nM against human DCN1. JN210 disrupts the UBE2M-DCN1 protein-protein interaction, blocks the neddylation modification of cullin-RING ligases, inhibits HDAC activity and induces histone hyperacetylation. JN210 impairs DNA damage repair function, induces cell apoptosis, exerts cytotoxicity and inhibits tumor growth. JN210 can be used for the research of non-small cell lung cancer .
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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
