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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
14 Results for "
cullin neddylation
" in MedChemExpress (MCE) Product Catalog:
Products (14)
14 Results for "cullin neddylation" in MCE Product Catalog:
10
10 Publications Verification
Research Areas:
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
4
4 Cited Publications
Research Areas:
NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction .
2
2 Cited Publications
Research Areas:
DI-1859 is a DCN1 and cullin 3 inhibitor with a Ki of <1 nM against human DCN1. DI-1859 forms a covalent bond with Cys115 of DCN1, cleaves its dimethylamino group, disrupts the DCN1-UBC12 interaction, and selectively inhibits the neddylation modification of cullin 3 relative to other cullins. DI-1859 inactivates CRL3, promotes the accumulation of NRF2 and SLC7A11, upregulates the expression of HO-1 and NQO1, reduces reactive oxygen species (ROS) levels, enhances insulin signaling, promotes insulin secretion, activates RhoA, regulates the phosphorylation of AKT, without completely blocking the neddylation modification of cullin 3 or restoring the expression of IRS-1. DI-1859 can be used in the research of Acetaminophen (HY-66005)-induced hepatotoxicity, hyperglycemia, metabolic dysfunction-associated steatotic liver disease, insulin resistance, breast cancer and lung cancer .
1
1 Cited Publications
Cat. No.: HY-160799
CAS No.: 2412367-83-8
Target:
Research Areas:
HA-9104 is a potent and selective inhibitor of cullin-5 neddylation via virtually targeting the V30 pocket of UBE2F. HA-9104 binds to UBE2F, reduces its protein levels, and consequently inhibits cullin-5 neddylation. HA-9104 has potent growth suppression and radiosensitizing activities via targeting the UBE2F-CRL5 axis and causing DNA damage, leading to induction of apoptosis and G2/M arrest in lung and pancreatic cancer cells .
1
1 Cited Publications
Target:
Research Areas:
DI-591 is a potent, high-affinity and cell-permeable inhibitor of the DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 nM and 10.4 nM, respectively and has no appreciable binding to DCN3, DCN4, and DCN5 proteins. DI-591 selectively inhibits neddylation of cullin 3 but has no or minimal effect on neddylation of other cullin family members .
Cat. No.: HY-156240
CAS No.: 2247060-97-3
Target:
Research Areas:
DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research .
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-122874
CAS No.: 2187412-79-7
Target:
Research Areas:
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-172252
Target:
Research Areas:
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-P70093
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: DCUN1D1; DCN1-Like Protein 1; Defective In cullin neddylation 1 Domain Containing 1; DCNL1; DCUN1L1; DCN1, Defective In cullin neddylation 1, Domain Containing 1 (S. Cerevisiae); SCCRO; DCN1, Defective In cullin neddylation 1, Domain Containing 1; RP42; D
Species:
Human
Source:
E. coli
Cat. No.: HY-P76866
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: DCUN1D2; DCNL2; Prev. C13orf17; DCN1, Defective In cullin neddylation 1, Domain Containing 2; Defective In cullin neddylation Protein 1-Like Protein 2; Defective In cullin neddylation Protein 1-Like Protein; DCUN1 Domain-Containing Protein 2; Chromosome 1
Species:
Human
Source:
E. coli
Cat. No.: HY-111505R
CAS No.: 2089293-61-6
Research Areas:
NAcM-OPT (Standard) is the analytical standard of NAcM-OPT (HY-111505). This product is intended for research and analytical applications. NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction .
Cat. No.: HY-189074
Research Areas:
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 .
Cat. No.: HY-187337
CAS No.: 3140110-11-5
HaloPROTAC 4 is a HaloPROTAC degrader with a pIC50 of 8.1 against human CRBN. HaloPROTAC 4 binds to CRBN to recruit the CUL4CRBN E3 ubiquitin ligase complex, and covalently binds to HaloTag fusion proteins, thereby inducing proteasome-dependent degradation of HaloTag fusion proteins. HaloPROTAC 4 serves as a protein knockdown tool for chemogenetic-related studies .
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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
