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Metabolic Enzyme/Protease

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Cat. No. Product Name Field of Application Chemical Structure
DC73770 TPN171 Featured
TPN171 (TPN-171) is a highly potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 0.62 nM, 32-fold selectivity over PDE6.
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DC70373 DX314 Featured
DX314 is a potent, specific CYP26B1 inhibitor with IC50 of 108 nM, >15-fold selectivity over CYP26A1.DX314 potentiates all-trans-RA (atRA) gene expression effects in healthy and diseased reconstructed human epidermis (RHE).DX314 potentiates the effects of atRA on the expression and localization of keratin 10 (KRT10), protects barrier function in RHE.DX314 reduces comedonal number, induces epidermal thickening, and increases comedonal profile, while having no effect on transepidermal water loss (TEWL) in treated rhino mice.
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DC70372 DX308 Featured
DX-308 is a potent, selective dual CYP26A1/B1 inhibitor and retinoic acid metabolism blocking agent.DX308 does not interact with off‐target nuclear receptors or CYP450s, is not genotoxic, and is stable in skin, despite vigorous hepatic metabolism.Topical DX308 induces comedolysis and epidermal thickening without apparent adverse effects in vivo.DX308 shows potent modulation of retinoid‐responsive genes by DX308 in both healthy and keratinization disorder keratinocytes (KCs).DX 308 may present an improved therapeutic alternative for the treatment of keratinization disorders and other retinoid‐responsive skin ailments.
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DC73744 ADAM9i Featured
ADAM9i is a specific small molecule inhibitor of ADAM9 protein with binding KD of 5.9 uM and enzyme IC50 of 5.2 uM, promotes the selective degradation of KRAS and sensitizes pancreatic cancers to chemotherapy.
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DC73706 ER-001135935 Featured
ER-001135935 is a potent selective inhibitor of aldehyde dehydrogenase family 1 member A3 (ALDH1A3) with IC50 of 64 nM, Ki value of 106 nM.
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DC81677 TRPM5 agonist-1 Featured
TRPM5 agonist-1 is an orally active TRPM5 agonist with a pEC50 of 8.1. TRPM5 agonist-1 shows excellent selectivity (> 100-fold) versus related cation channels (TRPM8, TRPV1, TRPV4, TRPA1, TRPM4). TRPM5 agonist-1 exhibits locally acting stimulatory effect on gastrointestinal transit in mice. TRPM5 agonist-1 can be used for research on promoting gastric motility.
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DC73778 WX-340 Featured
WX-340 is a highly specific and selective, peptidic cyclic competitive inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 12 and 170 nM for human and mouse uPA, respectively, inhibit 10 Units of human uPA with IC50 of 90 nM.
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DC41081 4'-Hydroxy diclofenac Featured
4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties.
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DC29002 Siguazodan Featured
Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.
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DC12014 NSC117079 Featured
A selective protein phosphatase PHLPP inhibitor with IC50 of 4 uM for PP2C domain of PHLPP2.
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DC70322 CPL500036 Featured
CPL500036 (CPL-500036) is a highly potent, selective and orally bioavailable PDE10A inhibitor with IC50 of 35 nM.CPL500036 is highly selective for PDE10A over other PDEs and common off-targets.CPL500036 effectively penetrates the brain where increases cAMP/cGMP levels and phosphorylates effector proteins like AMPA subunits.CPL500036 reduced sensorimotor deficits in 6-OHDA-lesioned rats.Acute and chronic CPL500036 did not reduce effects of L-DOPA in sensorimotor tests.Chronic CPL500036 treatment did not decrease L-DOPA-induced contralateral rotation.
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DC73707 KOTX1 Featured
KOTX1 is a potent, selective and reversible ALDH1A3 inhibitor with IC50 of 5.14 nM by Aldefluor assay in A375 cells.
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DC81818 σ1R/H3R ligand-1
σ1R/H3R ligand-1 is a dual σ1R/H3R antagonist with a σ1R Ki of 8.8 nM and an H3R Ki of 31.2 nM. Through the dual action of simultaneously antagonizing σ1R and H3R, σ1R/H3R ligand-1 exhibits potent dose-dependent analgesic activity in mouse models of visceral pain and neuropathic pain. σ1R/H3R ligand-1 can be used for the research of visceral pain and neuropathic pain.
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DC81817 ΔDi6S sodium
ΔDi6S sodium is a chondroitin that can be isolated from chondroitin-4-sulfate in whale cartilage.
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DC81803 αGlcCer
αGlcCer is a glycosphingolipid.
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DC81796 ZX-2401
ZX-2401 (Compound 98a) is a 1,3,5-Triazine-based analogue of Purine. ZX-2401 has a significant antiviral activity against viruses of the Flaviviridae family, such as West Nile Virus (WNV), Hepatitis C (HCV), Yellow Fever Virus (YFV), Dengue Virus (DV), Bovine Viral Diarrhea Virus (BVDV) and Banzi Virus (BV) with EC90s of 0.6-10 μg/mL. ZX-2401 significantly reduces virus production with an EC90 of 3.3 mg/mL. ZX-2401 can be used for influenza infections research.
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DC81723 VHR-IN-3
VHR-IN-3 (Compound 1) is a selective vaccinia H1-related (VHR) phosphatase inhibitor with a Ki of 0.81 μM. VHR-IN-3 mimics the phosphate group through the sulfonic acid group and competitively binds to the catalytic active center of VHR. VHR-IN-3 can be used for the research of cervical cancer.
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DC81699 U 88204
U 88204 is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 of 0.25 μM. U 88204 blocks HIV-1 replication in infected cells. U 88204 can be used for the research on HIV-infection and of acquired immunodeficiency syndrome (AIDs).
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DC81666 Topoisomerase IV-IN-3
Topoisomerase IV-IN-3 is a Staphylococcus aureus Topoisomerase IV inhibitor, DNA gyrase inhibitor and antibacterial agent. Topoisomerase IV-IN-3 has IC50 values of 1.32 μM and 0.48 μM against topoisomerase IV, and 0.88 μM and 0.54 μM against DNA gyrase. Topoisomerase IV-IN-3 inhibits decatenation, ATPase, and supercoiling activities of its target enzymes. Topoisomerase IV-IN-3 exerts antibacterial activity against Gram-positive and Gram-negative bacterial strains. Topoisomerase IV-IN-3 exhibits low cytotoxicity toward human fibroblast cells. Topoisomerase IV-IN-3 can be used for the research of bacterial infections.
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DC81649 TLR2/9 antagonist 1
TLR2/9 antagonist 1 (Compound 24) is a reversible covalent TLR2 (IC₅₀ = 0.5 μM (TLR2/TLR6); IC₅₀ = 0.6 μM (TLR2/TLR1)) and TLR9 (IC₅₀ = 0.32 μM) antagonist. TLR2/9 antagonist 1 has no significant effect on other TLR subtypes. TLR2/9 antagonist 1 can be used for studying central nervous system diseases and malignant tumors caused by inflammation.
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DC81610 Tenivastatin calcium
Tenivastatin calcium is a HMG-CoA reductase inhibitor. Tenivastatin calcium can reduce blood lipid level can be used for the research of hyperlipidemia.
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DC81590 T133
T133 is an orally active ATP-competitive mTOR inhibitor with an IC50 of 0.34 nM and a Ki of 0.17 nM. T133 suppresses phosphorylation of AKT, S6K1, and 4EBP1. T133 inhibits cancer cell proliferation and migration, induces apoptosis, cell cycle arrest, and autophagy. T133 exhibits dose-dependent antitumor efficacy in xenograft mouse models. T133 can be used for the research of cancer, such as gastric cancer and lung cancer.
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DC81555 SNA C(Bz) amidite
SNA C(Bz) amidite is a phosphoramide monomer that can be used to synthesize oligonucleotides.
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DC81548 SM-122
SM-122 is a monovalent Smac mimetic targeting cellular inhibitor of apoptosis protein (cIAP)-1/2. SM-122 can induce cIAP-1/2 degradation and weakly induce apoptosis in tumor cells. SM-122 can be used for the research of cancer, such as breast cancer.
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DC81517 Selnoflast monopotassium
Selnoflast (RO7486967) monopotassium, formerly somalix/RG6418/IZD334 monopotassium, is an orally active, potent, selective and reversible small molecule NLRP3 inflammasome inhibitor. Selnoflast monopotassium is a potent inhibitor of IL-1β release stimulated by NLRP3 activation in human Alzheimer's disease (AD) monocyte-derived macrophages. Selnoflast monopotassium is promising for research of AD and systemic inflammatory diseases, such as ulcerative colitis and chronic obstructive pulmonary disease.
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DC81509 SD3A
SD3A is an antiplatelet agent. SD3A inhibits granule secretion and GP IIb/IIIa activation. SD3A inhibits mitochondrial function. SD3A has an antiaggregant effect on washed platelets stimulated with Collagen. SD3A results in reduced thrombus formation without affecting coagulation.
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DC81506 SCH 47896
SCH 47896 is a phenolic derivative of SCH39370, a potent specific inhibitor of metalloendopeptidase (NEP). SCH 47896 can be used for the research of cardiovascular disease, such as hypertension.
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DC81499 SB5-171
SB5-171 is a covalent PfCLK3 inhibitor with IC50 values of 10-12 nM. SB5-171shows antiparasitic activity. SB5-171 can be used for the research of malaria.
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DC81496 SB1578
SB1578 (CT-1578) is a selective JAK2 and FLT3 inhibitor with an IC50 of 46 nM and 60 nM, respectively. SB1578 exhibits high selectivity for other kinase targets. SB1578 can be used for the study of non-oncology indication rheumatoid arthritis.
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DC81486 S-Adenosyl-L-ethionine
S-Adenosyl-L-ethionine is S-Adenosyl-L-methione analog. S-Adenosyl-L-ethionine is able to replace S-Adenosyl-L-methione during HydG catalysis. HydG can utilize S-Adenosyl-L-ethionine as an effective alternative cosubstrate to S-Adenosyl-L-methione under normal enzymatic turnover conditions, producing the Ω intermediate and allowing efficient catalytic turnover of substrate L-tyrosine.
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