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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
68 Results for "
Cullin
" in MedChemExpress (MCE) Product Catalog:
Products (68)
68 Results for "Cullin" in MCE Product Catalog:
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-175321
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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
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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-176070
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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
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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-175320
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PROTAC c-Met degrader-5 is an orally active c-Met PROTAC degrader. PROTAC c-Met degrader-5 induces c-Met degradation via Cullin-CRBN, with a DC50 value of 0.32 nM, and inhibits the phosphorylation of c-Met and its downstream signaling molecule STAT3. PROTAC c-Met degrader-5 inhibits cancer cell proliferation, migration and invasion, induces apoptosis, alters cell cycle distribution, and suppresses the growth of EBC-1 xenograft tumors. PROTAC c-Met degrader-5 can be used to study MET-driven cancers as well as Tepotinib (HY-14721)-resistant cancers harboring c-Met D1228N and c-Met Y1230H mutations .
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-P5022
CAS No.: 2243207-02-3
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Cat. No.: HY-122874
CAS No.: 2187412-79-7
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DI-404 is a potent inhibitor of DCN1 with a KKd value of 6.7 nM. DI-404 selectively inhibits neddylation of cullin 3 in a dose-dependent manner .
Cat. No.: HY-169026
CAS No.: 2543578-57-8
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DCN1-IN-2 is a DCN1 inhibitor with an IC50 value of 2.96 nM. DCN1-IN-2 can alleviate Ang II/TGFβ-induced activation of cardiac fibroblasts. DCN1-IN-2 can reduce ISO-induced cardiac fibrosis and remodeling in mice by selectively inhibiting cullin 3 .
Cat. No.: HY-172252
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CSN5-IN-2 (Compound 31) is a CSN5 inhibitor with an IC50 of 0.36 μM. CSN5-IN-2 can increase the level of Cullin 1 neddylation, and downregulate the expression of RAD51 and PD-L1 in cancer cells. CSN5-IN-2 has anti-tumor activity, and its effect is better when combined with Talazoparib (HY-16106) .
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 .
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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
