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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC78232 FK 973
FK 973 is a dihydrobenzoxazine anticancer agent. FK 973 selectively inhibits DNA synthesis and can form DNA cross-links through cytoplasmic activation. FK 973 exhibits significant antitumor activity in various animal tumor models and human tumor xenografts, with relatively weak myelosuppressive effects. FK 973 is sensitive to neural tumor cells. FK 973 can be used for DNA-targeted antitumor research.
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DC78231 SB-T-1214
SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133+/CD44+ cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers.
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DC78230 BIO-11006
BIO-11006 is a peptide that inhibits the function of the MARCKS protein. BIO-11006 attenuates LPS-induced neutrophil influx into the lungs, NF-κB activation, and expression of the proinflammatory cytokines KC and TNF-α. BIO-11006 also reverses disease progression in an LPS-induced mouse lung injury model. BIO-11006 is indicated for research on acute lung injury/acute respiratory distress syndrome (ALI/ARDS).
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DC78229 GDC-0152-acetamide
GDC-0152-acetamide is a pan-inhibitor of apoptosis protein (IAP) antagonist. GDC-0152-acetamide induces cIAP1/2 autoubiquitination and degradation, activating the non-canonical NF-κB pathway to promote TNF-α secretion and tumor cell apoptosis. GDC-0152-acetamide is promising for research of ERα-positive breast cancer.
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DC78228 CR-3294
CR-3294 is an autophagy inducer in hypoxic cells. CR-3294 is an inducible enzyme nitric oxide synthase (iNOS) inhibitor. CR-3294 inhibits both the DNA binding of HIF-1alpha and VEGF mRNA synthesis. CR-3294 can be used for the study of breast cancer and inflammatory bowel disease (IBD), such as Crohn’s disease, ulcerative colitis.
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DC78227 U-97456
U-97456 is a N-hydroxyacetyl derivate with antibacterial activity. U-97456 shows MIC <50 μg/mL against M. tuberculosis H37Rv. U-97456 can be used for the research of infection.
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DC78226 Ranbezolid
Ranbezolid (RBx7644 free base) is an orally active, oxazolidinone antibiotic against Gram-positive and Gram-negative anaerobes including Staphylococcus aureus, Staphylococcus epidermidis and Bacteroides fragilis. Ranbezolid can inhibit the 50s ribosomal subunit with an IC50 of 17 μM for bacterial ribosomes. Ranbezolid interferes cell wall and lipid synthesis. Ranbezolid can rapidly kill bacteria, significantly reduce bacterial load, and has better cardiovascular safety. Ranbezolid can be used for the study of antibiotics for anaerobic bacteria.
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DC78225 PNU-140457
PNU-140457 is an antibacterial agent targeting 30S ribosomal subunit. PNU-140457 is promising for research of bacterial Infections.
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DC78224 RWJ-416457
RWJ-416457 is an orally active antibacterial agent targeting 23S rRNA ribosome. RWJ-416457 is promising for research of Gram-positive bacterial infections.
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DC78223 S 33138
S33138 is a D3 receptor antagonist. S33138 inhibits addiction in animal models of addiction. S33138 reduces cognitive impairment in rodent and primate models of schizophrenia and Parkinson's disease. S33138 can be used in research on neurological disorders such as schizophrenia and Parkinson's disease.
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DC78222 Sch-40338
Sch-40338 is a dual antagonist of platelet-activating factor (PAF) and histamine with an IC50 of 0.59 μM (PAF-induced platelet aggregation) and a Ki of 5.4 μM (Histamine H₁ receptor binding). Sch-40338 can be used for the study of allergic disease.
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DC78221 ARUK2010489
ARUK2010489 (Compound 23) is a potent, selective and brain-penetrant NUAK1 inhibitor with a pIC50 of 8.7. ARUK2010489 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 7%, 39% and 26% at 1 μM. ARUK2010489 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).
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DC78220 ARUK2010694
ARUK2010694 (Compound 20) is a potent and selective NUAK1 inhibitor with a pIC50 of 8.7. ARUK2010694 also inhibits CDK2, CDK4 and CDK6 activity, with inhibitory rate of 13%, 63% and 32% at 1 μM. ARUK2010694 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).
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DC78219 ETI41
ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.63 μM) and TLR9 (IC50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research.
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DC78218 XIAP ligand 5
XIAP ligand 5 is a XIAP antagonist. XIAP ligand 5 is an E3 ligase ligand. XIAP ligand 5 can be used for synthesis of PROTAC GNE-1567.
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DC78217 CDK12-Cyclin K ligand-1
CDK12-Cyclin K ligand-1 is a ligand of PROTAC degrader that binds to the E3 ligase. CDK12-Cyclin K ligand-1 can be used in the synthesis of PROTAC degrader such as PP-C8.
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DC78216 EMD 386088 free base
EMD386088 free base is a potent serotonin 6 receptor (5-HT6R) agonist. EMD386088 free base induces cell death. EMD386088 free base regulates the activity of ERK1/2. EMD386088 free base has the potential for the research of alzheimer's disease (AD) and schizophrenia.
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DC78215 WIN-63291
WIN-63291 is a selective and orally active phosphodiesterase (PDE) III inhibitor. WIN-63291 can be used for the research of cardiovascular disease.
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DC78214 E3 Ligase Ligand-linker Conjugate 181
E3 Ligase Ligand-linker Conjugate 181 is an E3 ligase ligand-linker conjugate. E3 Ligase Ligand-linker Conjugate 185 can be used to synthesize MS115.
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DC78213 (S,S,S)-VH032
(S,S,S)-VH032 is the ligand for E3 Ligase (VHL) that can be used for synthesis of PROTAC SGK3 degrader-2.
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DC78212 (R,S,R)-AHPC-Me-Ac
(R,S,R)-AHPC-Me-Ac is an E3 ligase ligand used in the synthesis of the PROTAC SHP2 Protein degrader-2.
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DC78211 AKR1B1/STAT3/SLC7A11-regulator-1
AKR1B1/STAT3/SLC7A11-regulator-1 (5a) is an AKR1B1/STAT3/SLC7A11 regulator that reverses DOX resistance in MCF-7/ADR cells by enhancing ferroptosis activity. AKR1B1/STAT3/SLC7A11-regulator-1 can be used in breast cancer research.
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DC78210 BW A4C
BW A4C is a selective 5-lipoxygenase (5-LO) inhibitor. BW A4C is also an inhibitor of linoleic acid 8R-dioxygenase in Gaeumannomyces graminis, with an IC50 value of 0.2 μM. BW A4C can be used in research on diseases such as asthma.
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DC78209 WEHI-326
WEHI-326 is a potent antimalarial agent targeting Plasmodium falciparum ROM8 and CSC1 proteins (IC50=0.006 μM). WEHI-326 is promising for research of malaria.
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DC78208 E3 ligase Ligand 68
E3 ligase Ligand 68 is an E3 ligase ligand that can be used in the synthesis of PROTACs, such as PROTAC ER Degrader-3.
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DC78207 Xanthochymol
Xanthochymol is an antifungal agent found in Clusia rosea. Xanthochymol can induce fungal apoptosis.
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DC78206 Indolimine-214
Indolimine-214 is a metabolite of M. morganii Indolimine-214 increases the level of γH2AX in HeLa cells. Indolimine-214 can be used in the study of inflammatory bowel disease (IBD) and colorectal cancer (CRC).
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DC78205 GSK-1292263 hydrochloride
GSK-1292263 (hydrochloride) is an orally active GPR119 agonist (pEC50 of approximately 6.9 and 6.7 nM for human and rat GPR119, respectively). GSK-1292263 is used in the research of type 2 diabetes and dyslipidemia.
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DC78204 BI-5756
BI-5756 is a CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. BI-5756 can significantly increase HDL-C levels and reduce LDL-C levels. BI-5756 can also enhance the function of regulatory T cells while maintaining T cell-mediated anti-tumor activity. BI-5756 can directly inhibit the growth of tumor cells and upregulate the expression of MHC I, MHC II, and CD80 on tumor cells. BI-5756 has a protective effect in graft-versus-host disease models. BI-5756 can be used in research on tumors, graft-versus-host disease, and metabolic diseases.
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DC78203 NVS2.1
NVS2.1 is a potent, orally active and brain-penetrant readthrough promoter. NVS2.1 triggers the degradation of eRF1 by activating the ribosome-related quality control pathways (involving GCN1, RNF14, and RNF25), thereby facilitating the reading through of premature termination codons. NVS2.1 can be used for the research of genetic diseases caused by nonsense mutations.
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