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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC81822 Bireociclib (XZP-3287,CDK4/6-IN-2)
CDK4/6-IN-2 is a CDK4 and CDK6 inhibitor obtained from patent US20180000819A1 (Compound 1). It exhibits IC50 values of 2.7 nM for CDK4 and 16 nM for CDK6.
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DC81821 BBI-2779
BBI-2779 is a potent, selective, and orally active inhibitor of CHK1 with an IC50 of 0.3 nM. It preferentially kills cancer cells containing extrachromosomal DNA (ecDNA) by inducing replication stress and cell death. In gastric cancer models with FGFR2 gene amplification on ecDNA, BBI-2779 suppresses tumor growth and prevents drug resistance.
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DC81820 AD1058
AD1058 is an orally bioavailable ATR inhibitor with blood-brain barrier permeability (IC50 = 1.6 nM). It demonstrates antitumor effects through inhibition of tumor cell proliferation, induction of cell cycle arrest, and promotion of apoptosis. This compound is applicable for studies involving advanced malignancies and brain metastases.
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DC81819 360A
360A stabilizes G-quadruplex structures and inhibits telomerase activity, showing an IC50 of 300 nM in TRAP-G4 assays.
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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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DC81816 δ-Carboline
δ-Carboline is a nitrogen-containing heterocyclic compound, and its derivatives all exhibit anti-cancer and antibacterial activities.
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DC81815 γ-Linolenic acid NHS ester
γ-Linolenic acid NHS ester is a lipid metabolite of γ-Linolenic acid (GLA), which can serve as a synthetic intermediate or probe labeling reagent for the preparation of GLA conjugates. In practical applications, γ-Linolenic acid NHS ester can be conjugated with taxanes and polysaccharides to form dual-type conjugates for drug delivery purposes.
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DC81814 βGlcCer
βGlcCer is a glycosphingolipid.
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DC81813 β-Funaltrexamine
β-funaltrexamine (β-FNA) is a irreversible and selective μ opioid receptor antagonist that exhibits anti-inflammatory and neuroprotective effects. β-Funaltrexamine reduces TLR4 signaling, inhibits cytokine-induced iNOS activation and neuroinflammation, and ameliorates neuronal degeneration. β-funaltrexamine inhibits NF-κB signaling and chemokine expression in both human astrocytes and mice. β-funaltrexamine can be used for research on neurodegenerative diseases, such as stroke.
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DC81812 β-catenin-IN-9
β-catenin-IN-9 is a β-catenin inhibitor. β-catenin-IN-9 induces apoptosis, cell cycle arrest, and inhibits migration, invasion, and epithelial-mesenchymal transition (EMT) in colorectal cancer cells. β-catenin-IN-9 suppresses the transcription of β-catenin and vimentin, and significantly inhibits β-catenin at the protein level. β-catenin-IN-9 can be used for the research of colorectal cancer.
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DC81811 β-Catenin modulator-9
β-Catenin modulator-9 (Compound IIa-2075) is a β-Catenin modulator. β-Catenin modulator-9 specifically targets the activity of the stable β-catenin pool and inhibits the Wnt signaling pathway. β-Catenin modulator-9 can be used in cancer-related research.
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DC81810 β-Aspartyl phosphate
β-Aspartyl phosphate is a nucleoside metabolite.
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DC81809 α-Synuclein-IN-17
α-Synuclein-IN-17 (Compound 10) is an α-Synuclein inhibitor, with an IC50 value of 9 μM. α-Synuclein-IN-17 exhibits potent inhibitory activity against both in-vitro assembled asyn fibrils and LBD brain tissue-amplified asyn fibrils. α-Synuclein-IN-17 can be used for the study of Parkinson's disease (PD) and Lewy Body Disease (LBD).
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DC81808 α-Synuclein aggregate binder 2
α-Synuclein aggregate binder 2 (Compound 1) is a specific alpha-synuclein binder with a Ki of 1.6 nM. α-Synuclein aggregate binder 2 has a weak binding affinity for β-amyloid aggregates with a Ki of 295 nM. α-Synuclein aggregate binder 2 can be used as a tracer in Parkinson's disease.
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DC81807 α-Obscurine derivative-1
α-Obscurine derivative-1 (Compound 7) is a α-Obscurine derivative. α-Obscurine derivative-1 inhibits CaV3.1 ion channel current with an IC50 of 0.19 μM. α-Obscurine derivative-1 can be used in the research of neurological disorders.
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DC81806 α-Hydroxysalmeterol
α-Hydroxysalmeterol is a metabolite that can be formed via cytochrome P450 isoform 3A4-induced hydroxylation of Salmeterol. α-Hydroxysalmeterol is a potentially relevant urine biomarker to include when screening for Salmeterol misuse.
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DC81805 α-Glucosidase-IN-113
α-Glucosidase-IN-113 is an α-glucosidase inhibitor with an IC50 of 17.52 μM. α-Glucosidase-IN-113 shows antiglycating activity and inhibits advanced glycation end-product formation. α-Glucosidase-IN-113 can be used for the research of type 2 diabetes.
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DC81804 α-Glucosidase-IN-100
α-Glucosidase-IN-100 (compound 6) is a potent alpha glucosidase inhibitor. α-Glucosidase-IN-100 can be used to study metabolic diseases such as diabetes.
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DC81803 αGlcCer
αGlcCer is a glycosphingolipid.
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DC81802 α-Amylase-IN-13
α-Amylase-IN-13 is an orally active, selective, brain-penetrant α-amylase inhibitor (IC50 = 0.71 μM). α-Amylase-IN-13 inhibits α-amylase through a mixed type of inhibition mechanism. α-Amylase-IN-13 leads to a significant reduction in blood glucose level in diabetic rats. α-Amylase-IN-13 causes significant histopathological improvements in the kidney, liver, and pancreas. α-Amylase-IN-13 can be used for the study of diabetic complications.
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DC81801 α5β1 integrin-IN-1
α5β1 integrin-IN-1 (compound 65) is a potent and selective α5β1 integrin inhibitor with a pIC50 of 9.4. α5β1 integrin-IN-1 displays >10000-fold selectivity for α5β1 over αVβ3 (pIC50 = 5.5). α5β1 integrin-IN-1 reduces airway smooth muscle (ASM) tension through the disruption of cellular tethering. α5β1 integrin-IN-1 exhibits excellent inhalation pharmacokinetics in rodent. α5β1 integrin-IN-1 can be used for asthma research.
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DC81800 α4β7 Integrin-IN-1
α4β7 Integrin-IN-1 (Example 356) is a potent inhibitor of α4β7 integrin (integrin). Its ability to block the interaction between α4β7 integrin and MadCAM-1 (EC50) is 0.05 nM. α4β7 Integrin-IN-1 can be used for the study of inflammatory bowel disease.
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DC81799 α1A/1D-Adrenoceptor antagonist-1
α1A/1D-Adrenoceptor antagonist-1 (Compound 15) is a selective α1A/1D-adrenoceptor dual antagonist with IC50 values of 20.26 and 164.9 nM. α1A/1D-Adrenoceptor antagonist-1 shows an IC50 of 1912 nM for α1B-adrenoceptor.α1A/1D-Adrenoceptor antagonist-1 can be used for research of benign prostatic hyperplasia.
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DC81798 α,δ-NAG
α,δ-NAG is an orally active glutaminase-resistant less-hydrolyzable L-Glutamine derivative. α,δ-NAG is a G protein-coupled receptor (GPCR) allosteric modulator. α,δ-NAG suppresses neutrophilic airway inflammation by activating the GPCR/ERK/MKP-1 pathway. α,δ-NAG can be used for the researches of inflammation and immunology, such as asthma.
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DC81797 ZY39
ZY39 is a SaClpP agonist. ZY39 promotes the enzymatic hydrolysis of SaClpP and HsClpP in vitro. ZY39 inhibits the growth of Staphylococcus aureus strains. ZY39 reduces the load of Staphylococcus aureus in organs and ascites in mouse peritonitis models and zebrafish infection models, and improves the survival rate of model animals. ZY39 can be used in studies related to Staphylococcus aureus infection, such as peritonitis.
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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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DC81795 ZX079
ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC50 value of 0.035 nM and a CBP DC50 value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia. (Pink: BRD4 (BD1) and BRD4 (BD2) and CBP and p300 ligand ; Blue: Cereblon ligand ; Black: linker ).
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DC81794 ZSTK3744 hydrochloride
ZSTK3744 hydrochloride is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 hydrochloride directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 hydrochloride induces apoptosis in triple-negative breast cancer cells. ZSTK3744 hydrochloride exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.
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DC81793 ZSTK3744
ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 induces apoptosis in triple-negative breast cancer cells. ZSTK3744 exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.
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