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Home > Inhibitors & Agonists > Proteasome/Ubiquitin

Proteasome/Ubiquitin

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Cat. No. Product Name Field of Application Chemical Structure
DC79698 Bortezomib
Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).
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DC79694 BIIB021 mesylate
BIIB021 (CNF2024) mesylate is the mesylate of BIIB021. BIIB021 is an orally active Hsp90 inhibitor. BIIB021 inhibits the proliferation of chronic myeloid leukemia (CML) cells, with IC50 values of K562, K562/G, 32Dp210, and 32Dp210-T315I cells are 513.99, 603.53, 110.08, and 148.07 nM, respectively. BIIB021 degrades BCR-ABL protein and inhibits the β-catenin/c-Myc pathway. BIIB021 can also induce autophagy in CML cells. BIIB021 can be used for the research of CML.
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DC79525 ML229
ML229 is an HSP90 inhibitor. ML229 can be used in the research of infectious diseases such as candidiasis.
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DC79224 KW-2478 hydrochloride
KW-2478 (hydrochloride) is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 downregulates STAT3 expression. KW-2478 may be used in research on cancers such as CML and liver cancer.
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DC79168 Thalidomide-C1-O-CO-C11
Thalidomide-C1-O-CO-C2 is a ligand for E3 ubiquitin ligase. Thalidomide-C1-O-CO-C2 can be connected to Aurora-A ligand 1 by a linker to form PROTAC CDK4/6/9 degrader 2
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DC79088 Hakin-1
Hakin-1 is a E3 Ubiquitin-Ligase Hakai inhibitor. Hakin-1 blocks Hakai-mediated global ubiquitination and specific ubiquitination of E-cadherin and inhibits epithelial-mesenchymal transition (EMT) progression. Hakan-1 inhibits tumor progression and cancer metastasis. Hakin-1 can be used for the study of carcinoma such as colorectal cancer.
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DC79083 ML189
ML189 is an HSP90 inhibitor. ML189 can be used in the research of infectious diseases such as candidiasis.
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DC79015 LXE408 fumarate
LXE408 fumarate is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 fumarate has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 fumarate has a low propensity to cross the blood brain barrier. LXE408 fumarate has the potential for visceral leishmaniasis (VL) research.
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DC78938 Carmaphycin-17
Carmaphycin-17 (CP-17) is a selective 20S proteasome inhibitor with an EC50 of 217  nM. Carmaphycin-17 has potent antimicrobial activity against Trichomonas vaginalis. Carmaphycin-17 overcomes Metronidazole resistance and significantly reduces parasite burden upon topical treatment without any apparent adverse effects in vaginal trichomonad infection mice model. Carmaphycin-17 can be used for sexually transmitted disease like trichomoniasis research.
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DC78555 PSEC13
PSEC13 is an activator of HSF-1/DAF-16 axis. PSEC13 can upregulate heat shock proteins. PSEC13 can form hydrogen bonds with key residues in the HSP-16.2 active site. PSEC13 can be used to enhance proteostasis and extend lifespan through the modulation of HSP-16.2. PSEC13 could promote the nuclear translocation of daf-16, upgrading the proportion of intermediate. PSEC13 can be studied in research for aging and age-related diseases.
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DC78355 KUNB106
KUNB106 is a selective Hsp90β inhibitor with KDs of 91 nM and 38 μM against Hsp90β and Hsp90α. KUNB106 exhibits antiproliferative activity against MDA-MB-231 cells, A549 and SKOV-3 cells. KUNB106 can be used for the study of triple negative breast cancer.
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DC78296 TRIM25 ligand-1
TRIM25 ligand-1 (Compound 10) is a covalent ligand. TRIM25 ligand-1 can covalently bind to Cys498 in the PRYSPRY domain of TRIM25 and enhance its auto-ubiquitination activity. TRIM25 ligand-1 is selective for TRIM25 in vitro and in live cells.
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DC78276 ML-93
ML-93 is an orally active SAE inhibitor, with an IC50 value of 0.4 μM. ML-93 inhibits the SUMOylation pathway in HCT116 cells. ML-93 shows robust antitumor activity in the HCT116 colorectal carcinoma xenograft model. ML-93 can be used for the study of colorectal cancer.
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DC78197 HSP90i
HSP90i is the ligand for HSP90 and can be used for synthesis of LYTACs, such as dPDL1-4.
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DC78196 HSP90i-COCH2CH2-PEG4-NHBoc
HSP90i-COCH2CH2-PEG4-NHBoc is a conjugate of the HSP90 Ligand and the linker. HSP90i-COCH2CH2-PEG4-NHBoc can be used for synthesis of LYTACs, such as dPDL1-4
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DC78172 TIR-199
TIR-199 is a novel and highly specific dual proteasome inhibitor that can effectively inhibit the PSMB5 subunit of constitutive proteasome and the PSMB8 subunit of immunoproteasome. TIR-199 can induce the death of various tumor cells. TIR-199 can be used for research on myeloma.
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DC78137 TP-110
TP-110 is a proteasome inhibitor. TP-110 specifically inhibits the protease-like activity of the 20S proteasome, but does not affect the trypsin-like or peptidyl-glutamyl peptide hydrolysis activity. TP-110 inhibits the NF-κB pathway, activates caspase-8, -9, and -3, and causes PARP cleavage, significantly reducing the levels of cIAP-1 and XIAP. TP-110 causes cell cycle arrest at the G2/M phase and promotes apoptosis of cancer cells. TP-110 can be used in cancer research of prostate cancer and multiple myeloma, etc.
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DC78023 DDO-4033
DDO-4033 is a SPOP inhibitor (IC50 = 16.9 μM, Kd = 15.1 μM). DDO-4033 impairs the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts SPOP recruitment to its substrate LATS1, inhibits its polyubiquitination and subsequent degradation, and upregulates LATS1 expression. DDO-4033 has promising antitumor activity and is promising for renal cell carcinoma research.
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DC77956 Obudanersen
Obudanersen is an antisense oligonucleotide targeted to ubiquitin protein ligase E3A-antisense transcript (UBE3A-ATS). It is used for the study of Angelman syndrome.
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DC77955 Obudanersen sodium
Obudanersen sodium is an antisense oligonucleotide targeted to ubiquitin protein ligase E3A-antisense transcript (UBE3A-ATS). It is used for the study of Angelman syndrome.
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DC77855 Apazunersen
Apazunersen is an antisense oligonucleotide (ASO) that targets and inhibits expression of the UBE3A antisense transcript (UBE3A-AS) to prevent silencing of the paternally inherited allele of the UBE3A gene and reactivate expression of the deficient protei
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DC77854 Apazunersen sodium
Apazunersen sodium is an antisense oligonucleotide (ASO) that targets and inhibits expression of the UBE3A antisense transcript (UBE3A-AS) to prevent silencing of the paternally inherited allele of the UBE3A gene and reactivate expression of the deficient
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DC74282 HY041004 Featured
HY041004 is the first small molecule inhibitor of deubiquitinase Josephin Domain-containing protein 2 (JOSD2) with IC50 of 0.26 uM for JOSD2 catalytic activity inhibition.
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DC10831 HS-27 Featured
Hs-27 is a Novel Hsp90 Inhibitor, Exhibits Diagnostic and Therapeutic Potential in Triple Negative Breast Cancer.
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DC7816 MG-132 Featured
MG-132 is an inhibitor of proteasome with IC50 of 100 nM, and also inhibits calpain with IC50 of 1.2 μM.
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DC7702 MG-101 Featured
MG-101 is a calpain inhibitor (IC50 = 0.09 μM) that activates p53-dependent apoptosis in tumor cell lines.
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DC11555 GNE-6776 Featured
GNE-6776 is a novel potent, specific, non-covalent, orally bioavailable USP7 inhibitor with IC50 of 1.34 uM .
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DC77117 Boc3Arg
Boc3Arg is the tert-butyl carbamate-protected arginine. Boc3Arg is an efficient tag to induce degradation through directly localizing the protein to the 20S proteasome.
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DC74299 BC18630 free base Featured
BC18630 free base (BC 18630) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 39 nM in cell-based assays.
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DC74298 BC18630 Featured
BC18630 (BC 18630) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 39 nM in cell-based assays.
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