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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC79194 Phenyl-glutarimide 4'-oxyacetic-amide-C5-amide-Boc
Phenyl-glutarimide 4'-oxyacetic-amide-C5-amide-Boc is an E3 ligase ligand-linker conjugate used in the synthesis of PROTAC SJ995973.
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DC79193 Thalidomide-OCH2-amide-PEG2-C2-Boc
Thalidomide-OCH2-amide-PEG2-C2-Boc is an E3 ligase ligand-linker conjugate containing a cereblon (CRBN) ligand for E3 ubiquitin ligase and a linker. Thalidomide-OCH2-amide-PEG2-C2-Boc can be used to synthesize PROTAC SARS-CoV-2 Degrader-1.
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DC79192 PD 172760
PD 172760 is a selective D4 receptor antagonist. PD 172760 along with the action of other neurotransmitter receptors may be important in treating psychosis.
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DC79191 LacNAc-VC-PAB-MMAE
LacNAc-VC-PAB-MMAE is a component of an Antibody-Drug Conjugate (ADC). LacNAc-VC-PAB-MMAE is assembled onto the N-glycosylation site of Trastuzumab by WT Endo-S2.
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DC79190 DD-04-038
DD-04-038 is a molecular glue degrader. DD-04-038 induces proteins (such as IKZF1/3, ZBED3 and PATZ1) to bind to CRBN, promoting their ubiquitination and degradation.
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DC79189 ALK ligand-Linker Conjugate 1
ALK ligand-Linker Conjugate 1 is a ALK ligand-linker conjugate that can be used for synthesis of PROTAC ALK degrader-4.
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DC79188 NSC 850745
NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC50 values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer.
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DC79187 SMARCA2/4 Ligand-Linker Conjugate 2
SMARCA2/4 Ligand-Linker Conjugate 2 is a target protein ligand-linker conjugate that can be used to synthesize PROTAC AU-15330.
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DC79186 A2073
A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways. A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia.
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DC79185 AD-5467
AD-5467 is a potent and selective aldose reductase inhibitor. AD-5467 exhibits antidiabetic effect. AD-5467 can be used for the research of metabolic disease, such as diabetes.
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DC79184 Osunprotafib hydrochloride
Osunprotafib (ABBV-CLS-484) hydrochloride is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib hydrochloride has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib hydrochloride increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib hydrochloride generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction.
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DC79183 CCC-0975
CCC-0975 is a hepatitis B virus (HBV) inhibitor (EC50=10 μM). CCC-0975 interferes with the conversion of relaxed circular DNA (rcDNA) to cccDNA, synchronously reducing cccDNA and its precursor deproteinized rcDNA (DP-rcDNA) without promoting their intracellular degradation. CCC-0975 is promising for research of chronic hepatitis B.
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DC79182 PNU-142586
PNU-142586 is the major metabolite of Linezolid. PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism.
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DC79181 FAPI-JNU
FAPI-JNU is a molecule targeting fibroblast activation protein (FAP). FAPI-JNU specifically binds to FAP highly expressed in the tumor microenvironment, and uses radionuclides [68Ga]Ga or [177Lu]Lu to achieve tumor imaging diagnosis. [177Lu]Lu−FAPI−JNU can effectively target and inhibit tumor growth in tumor-bearing mice. FAPI-JNU is promising for research of FAP-positive tumors (such as various solid tumors).
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DC79180 Dacemazine
Dacemazine (Ahistan) is a phenothiazine derivative that acts as a histamine H1 receptor antagonist. Dacemazine exhibits local anesthetic activity and can alleviate spasms induced by acetylcholine and histamine.
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DC79179 Pomalidomide-PEG6-C2-COOH
Pomalidomide-PEG6-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 6-unit PEG linker used in PROTAC technology.
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DC79177 PXR ligand-Linker Conjugate 1
PXR ligand-Linker Conjugate 1 is a conjugate of PXR ligand and linker, which can be used to synthesize PROTAC MI1013.
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DC79176 KRAS G12C Ligand-Linker Conjugates 1
KRAS G12C Ligand-Linker Conjugates 1 is a conjugate of KRASG12C ligand and linker, which can be used in the synthesis of PROTAC YF135.
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DC79175 BCPT02
BCPT02 is a ADC linker, used in the synthesis of antibody-drug conjugates (ADCs).
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DC79174 STG-001
STG-001 is a retinol binding protein 4 (RBP4) antagonist. STG-001 inhibits RBP4 to reduce the synthesis of retinal and diretinol, thereby preventing photoreceptor degeneration. STG-001 can be used in the study of sexually precocious nephropathy (STGD).
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DC79173 Kynuramine
Kynuramine is an endogenous amine that serves as a fluorescent substrate and probe for plasma amine oxidase.
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DC79172 SC-57461
SC-57461 is a potent, selective, and orally effective LTA4 hydrolase (Ki = 23 nM and 27 nM) inhibitor. SC-57461 can significantly inhibit edema. SC-57461 is commonly used in the study of inflammatory skin conditions.
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DC79171 SP-141 hydrochloride
SP-141 (hydrochloride) is a specific inhibitor of MDM2. SP-141 (hydrochloride) promotes MDM2 auto-ubiquitination and degradation. SP-141 (hydrochloride) might be used for the research of pancreatic cancer and breast cancer cells.
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DC79170 VUBI1-octanoic acid
VUBI1-octanoic acid is a conjugate of SOS1 ligand and linker, which can be used in the synthesis of (4S)-PROTAC SOS1 degrader-1.
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DC79169 Thalidomide-amine-C11-acid
Thalidomide-amine-C11-acid is an E3 ligase ligand-linker conjugate which consists of Thalidomide 5-fluoride and a linker. Thalidomide-amine-C11-acid can be used to synthesize JQAD1
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DC79168 Thalidomide-C1-O-CO-C11
Thalidomide-C1-O-CO-C2 is a ligand for E3 ubiquitin ligase. Thalidomide-C1-O-CO-C2 can be connected to Aurora-A ligand 1 by a linker to form PROTAC CDK4/6/9 degrader 2
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DC79167 AM11638
AM11638 is an endocannabinoid analog targeting cannabinoid receptors (CB1 and CB2 receptors) with analgesic effects. AM11638 is promising for research of neurological diseases and inflammation-related diseases.
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DC79166 Luvesilocin
Luvesilocin (Example 6) is a tryptamine prodrug. Luvesilocin can convert into an active form, acting as a 5HT2A agonist in vivo upon administration. Luvesilocin can be studied in research for mental diorders.
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DC79165 Pomalidomide-PEG3-Cys
Pomalidomide-PEG3-Cys is an E3 ligase ligand-linker conjugate that incorporates a CRBN ligand Pomalidomide and 3-unit PEG linker. Pomalidomide-PEG3-Cys can be used for synthesis of PROTAC BRD4 Degrader-33.
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DC79164 BMS-229724
BMS-229724 is an orally active and tight-binding cytosolic phospholipase A2 (cPLA2) inhibitor with an IC50 of 2.8 μM. BMS-229724 can inhibit the production of arachidonic acid and eicosanoids in U937 cells, neutrophils, platelets, and other cells. BMS-229724 has anti-inflammatory activity and can be used in the research of diseases such as skin inflammation.
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