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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC48945 RORγt/DHODH-IN-1
RORγt/DHODH-IN-1 (compound (R)-14d) is a potent and orally active dual RORγt/DHODH inhibitor, with IC50s of 0.083 μM and 0.172 μM, respectively. RORγt/DHODH-IN-1 exhibits remarkable in vivo anti-inflammatory activity.
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DC48944 RORγt/DHODH-IN-3
RORγt/DHODH-IN-3 (compound (S)-14d) is a dual RORγt/DHODH inhibitor, with IC50s of 0.098 μM and 0.432 μM, respectively. RORγt/DHODH-IN-3 exhibits remarkable in vivo anti-inflammatory activity.
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DC48943 YF-452
YF-452 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2). YF-452 remarkably inhibits the migration, invasion and tube-like structure formation of human umbilical vein endothelial cells (HUVECs) with little toxicity. YF-452 inhibits VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal regulated kinase (ERK), focal adhesion kinase (FAK) and Src. YF-452 is a potential antiangiogenic drug candidate for cancer research.
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DC48942 Butyrolactone V
Butyrolactone V is a butanolide compound. Butyrolactone V shows antiplasmodial activity against Plasmodium falciparum K1 with an IC50 of 7.9 µg/ml.
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DC48940 HPK1-IN-18
HPK1-IN-18 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-18 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019238067A1, compound 1).
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DC48939 ROS-ERS inducer 1
ROS-ERS inducer 1 is a type II ICD (immunogenic cell death) inducer. ROS-ERS inducer 1 is a Pt(II)-N-heterocyclic carbene (Pt(II)-NHC) complex derived from 4,5-diarylimidazole. ROS-ERS inducer 1 successfully induces endoplasmic reticulum stress (ERS) accompanied by reactive oxygen species (ROS) generation and finally lead to the release of damage-associated molecular patterns (DAMPs) in HCC cells. ROS-ERS inducer 1 displays much higher anticancer activities than Cisplatin.
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DC48938 DCN1-UBC12-IN-1
DCN1-UBC12-IN-1 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.86 nM. Anticardiac fibrotic effect.
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DC48937 Methyl 3,4,5-trimethoxy-2-(2-(nicotinamido)benzamido)benzoate
Methyl 3,4,5-trimethoxy-2-(2-(nicotinamido)benzamido)benzoate is a fungal metabolite.
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DC48936 HPK1-IN-14
HPK1-IN-14 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-14 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 79) .
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DC48935 Kotanin
Kotanin is a metabolite of Aspergillus glaucus.
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DC48934 EP2 receptor antagonist-1
EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects.
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DC48933 TP-16
TP-16 is a novel and selective EP4 antagonist with an IC50 of 2.1 nM.
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DC48932 Bis-PEG4-TFP ester
Bis-PEG4-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC48931 PfPKG-IN-1
PfPKG-IN-1 is a imidazole-based inhibitor of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG).
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DC48930 Fumiquinazoline D
Fumiquinazoline D, a secondary metabolite, is a mycotoxin.
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DC48929 B-Raf IN 6
B-Raf IN 6 (compound 2c) is a potent inhibitor of protein kinase B-Raf with an IC50 of 1.7 nM. B-Raf IN 6 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease.
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DC48928 HPK1-IN-15
HPK1-IN-15 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-15 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2018049200A1, compound 50).
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DC48927 Hcyb1
Hcyb1 is a highly selective PDE2 inhibitor. Hcyb1 has a highly selective inhibition of PDE2A (IC50=0.57 μM) and over 250-fold selectivity against other recombinant PDE family members. Hcyb1 produces neuroprotective and antidepressant‐like effects most likely mediated by cAMP/cGMP-CREB-BDNF signaling.
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DC48926 CPT-Se3
CPT-Se3, a selenoprodrug of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT–Se3 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se3 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.19-4.7 μM).
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DC48925 MsbA-IN-6
MsbA-IN-6 is a potent inhibitor of MsbA. MsbA-IN-6 is an antibiotic. Gram-negative ATP-binding cassette (ABC) transporter MsbA, an essential inner membrane protein, transports lipopolysaccharide from the inner leaflet to the periplasmic face of the inner membrane. MsbA-IN-6 kills Escherichia coli through inhibition of its ATPase and transport activity, with no loss of activity against clinical multidrug-resistant strains.
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DC48924 Fenticonazole
Fenticonazole is an imidazole derivative with antibacterial and antifungal activity. Fenticonazole has the potential for the research of mixed vaginitis.
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DC48922 GSK2647544
GSK2647544 is an orally available, selective inhibitor of Lp-PLA2. Lipoprotein-associated phospholipase (Lp-PLA2) is a calcium-independent phospholipase A2 with proinflammatory activities that is primarily secreted by monocyte-derived macrophages.
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DC48921 Benzomalvin B
Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P.
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DC48920 Antibacterial agent 67
Antibacterial agent 67 (IC50 = 0.03 μM) has a great enzyme-inhibiting activity increase toward succinate dehydrogenase in comparison with fluxapyroxad (IC50 = 4.40 μM).
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DC48919 Noladin ether
Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception.
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DC48918 (S)-Butaprost free acid
(S)-Butaprost (free acid) is a potent and highly selective agonist of EP2 receptor.
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DC48917 EB-0176
EB-0176 is a potent inhibitor of ER α-glucosidases (α-Glu) Iand II with IC50s of 0.6439 and 0.0011 μM, respectively. EB-0176 is a N-substituted derivative of valiolamine with broad-spectrum antiviral. EB-0176 has the potential for the reseach of broad-spectrum agent against the existing and emerging viruses.
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DC48916 SIK1 activator 1
SIK1 activator 1 exhibited remarkable inhibitory activity on hepatic gluconeogenesis by enhancing the SIK1 phosphorylation and ameliorated the hyperglyceamia of type 2 diabetic mice.
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DC48915 Maximiscin
Maximiscin, a fungal metabolite, induces DNA damage and shows selective cytotoxic activity against a subtype of triple-negative breast cancer.
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DC48914 FmocNH-PEG3-CH2CH2NH2 hydrochloride
FmocNH-PEG3-CH2CH2NH2 (hydrochloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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