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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC49134 BRD4 D1-IN-1
BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC.
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DC49133 SSTR5 antagonist 2 hydrochloride
SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM).
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DC49132 KRAS G12C inhibitor 23
KRAS G12C inhibitor 23 is a KRAS G12C inhibitor. KRAS G12C inhibitor 23 inhibits H358 cells with an IC50 of 491 nM (WO2021218939A1, compound 1).
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DC49131 GLP-1 receptor agonist 9
GLP-1 receptor agonist 9 is a GLP-1 receptor agonist, example 7, extracted from WO2020234726 A1.
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DC49129 AChE-IN-4
AChE-IN-4 shows the acetylcholine esterase inhibition (AChEI) with an IC50 value of 24.1 μM.
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DC49128 11-Keto fusidic acid
11-Keto fusidic acid shows strong antibacterial activity toward Staphylococcus aureus with an MIC value of 0.078 μg/mL.
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DC49127 Oritinib
Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.
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DC49126 HPK1-IN-10
HPK1-IN-10 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-10 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 103) .
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DC49125 Toddacoumalone
Toddacoumalone is a natural inhibitor of phosphodiesterase 4 (PDE4) with moderate potency and imperfect drug-like properties. Toddacoumalone has the potential for the research of inflammatory diseases such as psoriasis.
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DC49124 GLP-1 receptor agonist 7
GLP-1 receptor agonist 7 is a potent agonist of glucagon-like peptide-1 (GLP-1). GLP-1 receptor agonist 7 has the potential for the research of GLP-1-associated diseases, disorders, and conditions including diabetes mellitus (extracted from patent WO2021219019A1, compound 130b).
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DC49123 Xanthoquinodin A1
Xanthoquinodin A1 is an anticoccidial antibiotic having a new xanthone-anthraquinone conjugate system.
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DC49122 TPE-MI
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells. TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin treatment of the malaria parasitesPlasmodium falciparum .
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DC49121 L-Tyrosine-13C6
L-Tyrosine-13C6 is the 13C-labeled L-Tyrosine. L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex.
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DC49120 L-Phenylalanine-13C6
L-Phenylalanine-13C6 ((S)-2-Amino-3-phenylpropionic acid-13C6) is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
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DC49119 H-Tyr(3-I)-OH-13C6
H-Tyr(3-I)-OH-13C6 is the 13C-labeled H-Tyr(3-I)-OH. H-Tyr(3-I)-OH is a potent and effective tyrosine hydroxylase inhibitor. H-Tyr(3-I)-OH is an intermediate in the production of thyroid hormones and has a role as a human or mouse metabolite.
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DC49118 D-Glucose-13C3
D-Glucose-13C3 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response.
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DC49117 D-Glucose-13C3-1
D-Glucose-13C3-1 (Glucose-13C3-1) is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response.
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DC49116 L-Ornithine-1,2-13C2 hydrochloride
L-Ornithine-1,2-13C2 hydrochloride is the 13C-labeled L-Ornithine hydrochloride. L-Ornithine hydrochloride is a free amino acid that plays a central role in the urea cycle and is also important for the disposal of excess nitrogen.
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DC49115 Biotin-PEG9-amine
Biotin-PEG9-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC49114 Sartorypyrone B
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases.
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DC49113 Inubritannolide A
Inubritannolide A displays slight strong neuroprotective potency against different types of neuronal cells mediated by various inducers including H2O2, 6-hydroxydopamine (6-OHDA), and lipopolysaccharide (LPS).
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DC49112 19,20-Epoxycytochalasin D
19,20-Epoxycytochalasin D, a cytochalasin, is a fungal metabolite from Nemania sp. 19,20-Epoxycytochalasin D shows potent in vitro antiplasmodial activity and phytotoxicity.
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DC49111 19,20-Epoxycytochalasin C
19,20-Epoxycytochalasin C, a cytochalasin, is a fungal metabolite from Nemania sp. 19,20-Epoxycytochalasin C shows potent in vitro antiplasmodial activity and phytotoxicity.
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DC49110 Avellanin B
Avellanin B is a fungal metabolite with pressor effect.
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DC49109 EGFR-IN-24
EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively.
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DC49108 HPK1-IN-9
HPK1-IN-9 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-9 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 112) .
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DC49107 BRD4-BD1/2-IN-2
BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC50s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2).
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DC49106 Mal-Ala-Ala-PAB-PNP
Mal-Ala-Ala-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC49105 DCN1-UBC12-IN-3
DCN1-UBC12-IN-3 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.25 nM. Anticardiac fibrotic effect.
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DC49104 RET-IN-6
RET-IN-6 is a potent RET (rearranged during transfection) inhibitor with an IC50 of 4.57 nM (CN113461670A, compound 321).
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