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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC78243 (S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide
(S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide (N-Docosahexacnoylethanolamide(22:6)) is a DHEA homolog. (S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide blocks the Shaker-related voltage-gated potassium channels. (S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide can inhibit the Kv1.2 K+ currents with an IC50 of 1.5 μM.
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DC78242 ER ligand-12
ER ligand-12 is an estrogen receptor (ER) ligand that can be used in the synthesis of PROTACs, such as PROTAC ER Degrader-2.
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DC78241 GNE-1567
GNE-1567 is a potent ERα PROTAC degrader and a selective XIAP antagonist with a Kd value of 0.03 μM. GNE-1567 is indicated for breast cancer research.
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DC78240 ST09
ST09 is an efficient and low toxicity curcumin derivative. ST09 significantly inhibits cell migration and downregulates the expression of MMP1, MMP2, and Vimentin. ST09 has strong cytotoxicity to breast cancer cells, such as MDA-MB-231, MCF7 and T47D cells. ST09 induces cell apoptosis by upregulating Bax and cleaved caspase-3/9. ST09 can be used in the research of cancer such as breast cancer.
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DC78239 (1R,2R)-Elpipodect
(1R,2R)-Elpipodect ((1R,2R)-MK-8189) is the (1R,2R) enantiomer of Elpipodect). Elpipodect (MK-8189) is an orally active and selective PDE10A inhibitor with a Ki of 29 pM. Elpipodect can be used in research of schizophrenia.
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DC78238 4-AcO-DALT hydrochloride
4-AcO-DALT hydrochloride is a tryptamine compound with psychoactive effects. 4-AcO-DALT hydrochloride inhibits 5-HT receptors, alpha receptors, dopamine receptors, histamine receptor 1 (H1), muscarinic M2 receptor and Sigma 2 receptor. 4-AcO-DALT hydrochloride shows Ki values of 582 nM, 2689 nM, 2099 nM, 2116 nM, 958 nM, 137 nM, 824 nM, 479 nM, 406 nM, 874 nM, 4190 nM, 482 nM, 214 nM, 803 nM, 4522 nM, 1907 nM for 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7A, H1, Sigma 2, α2A, α2B, α2C, D2, D3 receptors.
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DC78237 AGW-11
AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer.
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DC78236 SMU-C68
SMU-C68 is a highly selective small-molecule TLR1/2 heterodimer agonist (EC50=0.009 μM). SMU-C68 activates NF-κB and MAPK pathways to promote pro-inflammatory cytokine release (e.g., TNF-α, IL-1β). SMU-C68 is promising for research of cancers.
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DC78235 BMY-28271
BMY-28271 is an orally active cephalosporin. BMY-28271 has a widely expanded spectrum with high activity against gram-positive and gram-negative bacteria. BMY-28271 is a poor substrate for various beta-lactamases. BMY-28271 can be used for the research of infection.
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DC78234 BMS-269223
BMS-269223 is a potent, selective and orally active factor Xa inhibitor (Ki = 6.5 nM, EC2xPT = 32 μM). BMS-269223 can prolong prothrombin time and inhibit thrombosis formation. BMS-269223 can be used for the research of cardiovascular disease.
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DC78233 DHGA5
DHGA5 is a GA3β-hydroxylase (OsGA3ox2) inhibitor. DHGA5 inhibits Arabidopsis root growth with an IC50 of 97 μM. DHGA5 also suppresses the elongation of rice second leaf sheath. DHGA5 can alleviate oxidative damage to Arabidopsis seedlings under NaCl salt stress and reduce the accumulation of superoxide anion.
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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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