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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
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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DC79163 LXT34
LXT34 (Example 2) is a GPR120 agonist. LXT34 has an anti-inflammatory activity. LXT34 promotes GLP-1 formation in the gastrointestinal tract and improves insulin resistance in macrophages and pancreas cells. LXT34 can be used for inflammatory diseases, such as type 2 diabetes, obesity and non-alcoholic fatty liver research.
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DC79162 Dopamine D4 receptor ligand 3
Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pKi: 8.86). Dopamine D4 receptor ligand 3 has pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells.
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DC79161 SAR216471
SAR216471 is a P2Y12 receptor antagonist. SAR216471 reversibly blocks the binding of 2MeSADP to P2Y12 receptors in vitro with an IC50 of 17 nM. SAR216471 can result in the inhibition of platelet aggregation. SAR216471 exhibits anti-thrombotic activity in rat model. SAR216471 can be studied in research on thrombosis.
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DC79160 Thalidomide-PEG3-amide-C2-COOH
Thalidomide-PEG3-amide-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs, such as BCL6 PROTAC 1.
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DC79159 TriOncoFAP-GlyPro-MMAE
TriOncoFAP-GlyPro-MMAE is a small molecule drug conjugate (SMDC) targeting fibroblast activation protein (FAP) with an IC50 of 13 pmol/L. TriOncoFAP-GlyPro-MMAE combines a FAP-targeting ligand (TriOnco), a cleavable glycine-proline linker, and a cytotoxic payload (MMAE).
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DC79158 YZ-35
YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer.
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DC79157 CCI17464
CCI17464 is a selective, orally active EP4 agonist. CCI17464 can be used in a Freund's complete adjuvant (FCA) acute rat inflammatory pain model and shows complete reversal of allergic reactions.
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DC79156 LY2457546
LY2457546 is a potent and orally active multi-targeted anti-angiogenic tyrosine kinases inhibitor. LY2457546 demonstrates potent activity against targets that include VEGFR2, PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. LY2457546 can be used for the research of cancer, such as leukemia.
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DC79155 MOL-6131
MOL-6131 is a highly selective, reversible tryptase inhibitor, with a Ki of 45 nM. MOL-6131 significantly reduces the following features of allergic airway inflammation: eosinophil infiltration in lung tissue, goblet cell hyperplasia and mucus occlusion of airways.
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DC79154 IHMT-15130
IHMT-15130 is a highly potent irreversible BMX kinase inhibitor (IC50=1.47 nM). IHMT-15130 inhibits the secretion of inflammatory cytokines, blocks inflammatory signaling pathways, and alleviates Angiotensin II-induced myocardial hypertrophy in mice. IHMT-15130 is promising for research of myocardial hypertrophy.
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DC79153 CRBN Ligand-Linker Conjugate 2
CRBN Ligand-Linker Conjugate 2 is a synthesized E3 ligand-linker conjugate that can be used for synthesis of PROTACs, such as FIP22. FIP22 is a potent and selective IRAK4 PROTAC degrader with anti- atopic dermatitis activity.
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DC79152 TcO-ABX474
TcO-ABX474 (TcO-5) is a potent prostate-specific membrane antigen (PSMA) inhibitor with a Kd value of 6.1 nM. TcO-ABX474 inhibits prostate cancer cell growth and metastasis. TcO-ABX474 is promising for research of prostate cancer.
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DC79151 RS 93427-007
RS 93427-007 is an orally active prostacyclin stable mimetic agent. RS 93427-007 can be used for the research of cardiovascular disease, such as atherosclerosis.
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DC79150 SM1-71-R
SM1-71-R is a reversible analog o SM1-71). SM1-71-R lacks the acrylamide warhead and therefore cannot form a covalent bond with the kinase. SM1-71-R can be used as a control compound for SM1-71.
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DC79149 CC-3052
CC-3052 is a phosphodiesterase 4 (PDE4) inhibitor with immunomodulatory activities. CC-3052 reduces neutrophil apoptosis in HIV⁺. CC-3052 is promising for research of HIV-related diseases.
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DC79148 Dimephosphon
Dimephosphon is an anti-inflammatory agent with antihistamine and antiserotonin activities. Dimephosphon helps maintain the conduction function of the spinal cord and reduces the excitability of spinal motor neurons in the area surrounding the lesion. Dimephosphon directly activates lymphatic vessel movement and improves lymphatic circulation. Dimephosphon can be used for the study of inflammatory edema, acute spinal cord injury and lymphatic circulation disorders.
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DC79147 IDN-1965
IDN-1965 is an irreversible, broad-spectrum caspase inhibitor. IDN-1965 prevents downstream apoptotic events (such as DNase activation) and significantly delays cytochrome c release by inhibiting caspase activity. IDN-1965 significantly delayed death in mice with cardiomyocyte apoptosis. IDN-1965 completely prevents left ventricular dilation, systolic dysfunction, and fibrosis in mice with dilated cardiomyopathy. IDN-1965 can be used to study apoptosis-related diseases such as heart failure and the mechanisms of apoptosis initiation.
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DC79146 GLK7-001
GLK7-001 is a Trypanosoma cruzi glucokinase (TcGlcK) inhibitor. GLK7-001 has in vitro trypanocidal activity.
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DC79145 HOE-288
HOE-288 is an orally active angiotensin-converting enzyme (ACE) inhibitor. HOE-288 can be used for the research of neurological disease.
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DC79144 α-Synuclein inhibitor 15
α-Synuclein inhibitor 15 (Compound 1) is an inhibitor targeting the fibrillation growth of α-synuclein (IC50=18 μM). α-Synuclein inhibitor 15 is promising for research of neurodegenerative diseases, such as Parkinson's disease (PD) and Lewy body dementia (LBD).
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DC79143 TBK1 ligand 2
TBK1 ligand 2 (Compound 1b) is a TBK1 inhibitor. TBK1 ligand 2 can be used for synthesis of PROTAC TBK1 degrader-2.
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