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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC81552 SMTIN-P01
SMTIN-P01 is a TRAP1 inhibitor that is selective for cytosolic Hsp90 and accumulates in mitochondria. SMTIN-P01 binds to the ATP-binding site of TRAP1 as an ATP mimic, thereby inhibiting ATPase and foldase activities. SMTIN-P01 induces mitochondrial membrane depolarization and proteolytic degradation in cancer cells. SMTIN-P01 exhibits significant cytotoxicity, but shows extremely low toxicity to primary mouse hepatocytes, and does not interfere with SIRT3-related functions or the levels of cytosolic Hsp90 substrates. SMTIN-P01 has important application value in cancer-related research.
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DC81551 SMARCA2/4-ligand-7
SMARCA2/4-ligand-7 is a SMARCA2/4 ligand, which can be used for the synthesis of PROTACs, such as PROTAC SMARCA2/4 degrader-41.
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DC81549 SM-15178
SM-15178 is a potent, orally active and selective leukotriene B4 (LTB4) receptor antagonist with an IC50 of 0.30 μM. SM-15178 attenuates LTB4-induced neutrophil accumulation in mouse skin and bronchoconstriction in guinea pigs. SM-15178 emonstrates significant anti-inflammatory efficacy across multiple animal models of inflammation. SM-15178 can be used for the research of chronic inflammatory diseases such as inflammatory bowel disease, psoriasis, and asthma.
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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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DC81547 SM-11044
SM-11044 is a β-adrenoceptor agonist with Ki values of 18.1 μM (β1), 4.1 μM (β2) and 1.3 μM (β3), showing higher binding selectivity for the β3-adrenoceptor. SM-11044 stimulates cAMP accumulation in cells expressing this receptor. SM-11044 mediates ileal relaxation, tracheal relaxation, pulmonary parenchymal relaxation, increased right atrial heart rate and adipocyte lipolysis.
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DC81546 SM00465
SM00465 (Compound 207) is a Cbl-b inhibitor-linker conjugate composed of INT4 and Linker. SM00465 can be used for ADC synthesis. SM00465 is applicable to the research of immune-related diseases.
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DC81545 SLD1121
SLD1121 is an agonist of the Wnt/β-catenin signaling pathway that enhances Wnt signaling by targeting LRP6 (Kd: 4.52-7.49 nM). SLD1121 interacts with the intracellular domain of LRP6, stabilizes LRP6, promotes its nuclear translocation, and facilitates its binding to β-catenin, TCF4 or LEF1 in the nucleus, thereby inducing the expression of Wnt-regulated genes and stem cell-related genes. SLD1121 induces the transition of hair follicles from telogen to anagen in the mouse hair growth cycle and promotes hair growth in mice. SLD1121 is applicable to hair loss-related research.
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DC81544 SLC6A19-IN-4
SLC6A19-IN-4 is an allosteric-competitive and orally active B0AT1 inhibitor. SLC6A19-IN-4 inhibits both human and mouse B0AT1 with IC50 values of 513 nM and 295 nM, respectively. SLC6A19-IN-4 exhibits excellent metabolic stability. SLC6A19-IN-4 significantly increases urinary phenylalanine (Phe) excretion and reduces plasma Phe levels through dual inhibition of B0AT1 in both the intestine (reducing absorption) and kidney (promoting excretion) in vivo. SLC6A19-IN-4 can be used for phenylketonuria (PKU) and other disorders involving SLC6-family transporters research.
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DC81543 SK-129
SK-129 is a blood-brain barrier-permeable inhibitor of α-synuclein (αS) oligomers with a Kd of 221 nM. SK-129 preferentially binds to neurotoxic αS oligomers over physiological αS monomers, inhibits αS aggregation, blocks the interaction and co-aggregation of αS with tau protein, and prevents the maturation of αS-tau condensates into amyloid aggregates. SK-129 reduces ROS production, rescues dopaminergic neuron degeneration, improves motor function, restores endogenous dopamine synthesis, increases the number of Tyrosine Hydroxylase-positive neurons, prevents brain histopathological changes, alleviates neuroinflammation, and improves survival rates in relevant models. SK-129 can be used in research related to Parkinson's disease (PD) and Lewy body dementia (LBD).
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DC81542 SIRT6-IN-6
SIRT6-IN-6 (compound 6d) is a potent and selective SIRT6 inhibitor with an IC50 of 4.93 μM and a Ki of ~10 μM. SIRT6-IN-6 shows selectivity against other members of the HDAC family (SIRT1-3 and HDAC1-11). SIRT6-IN-6 significantly increases the level of glucose transporter GLUT-1, thereby reducing blood glucose in a mouse model of type 2 diabetes. SIRT6-IN-6 can be used for type 2 diabetes research.
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DC81541 SIRT2-IN-18
SIRT2-IN-18 (Compound 8) is a SIRT2 inhibitor with IC50s of 5.3  and 12.3 μM for SmSIRT2 and hSIRT2, respectively. SIRT2-IN-18 shows potent antischistosomal activities against both Liberian and Puerto Rican strains of Schistosoma mansoni and reduces schistosomula and adult worm pair viability, pairing, and egg production, with low cytotoxicity in mammalian cells. SIRT2-IN-18 increases histone H3 hyperacetylation and induces cytochrome c-mediated apoptosis.
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DC81540 SIMR-2418
SIMR-2418 is an effective inhibitor of the main protease (Mpro) of SARS-CoV-2, with an IC50 value of 20.7 μM. SIMR-2418 can be used for research on SARS-CoV-2 virus infection.
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DC81539 Simotaxel
Simotaxel (MST 997) is an orally active derivative of the taxane class. Simotaxel binds to β-tubulin and promotes tubulin polymerization (EC₅₀ = 0.9 μM), inhibits tubulin depolymerization, and causes cell cycle arrest at the G₂-M phase. Simotaxel disrupts the formation of the mitotic spindle and triggers the caspase-dependent apoptotic pathway (apoptosis). Simotaxel has inhibitory effects on Paclitaxel sensitive cell lines and overcomes drug resistance. Simotaxel can be used to study Paclitaxel / Docetaxel resistant solid tumors.
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DC81538 Simeton
Simeton is a methoxy-5-triazine herbicide used for weed control in agricultural crops including corn, wheat, maize, and barley. Simeton is a methoxy-5-triazine herbicide widely used for weed control in agricultural crops including corn, wheat, maize, and barley.
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DC81537 Simeconazole
Simeconazole is a demethylation inhibitor-class fungicide. Simeconazole prevents the infection of barley leaves by Blumeria graminis f sp hordei, inhibits the development of powdery mildew on barley and cucumber leaves, and exhibits cuticular membrane permeability in tomato fruits. Simeconazole can be used in research related to barley powdery mildew and cucumber powdery mildew.
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DC81536 Sim-9
Sim-9 is a covalent allosteric inhibitor of interferon regulatory factor 3 (IRF3). Sim-9 binds covalently to the Cys222 residue of IRF3, induces its conformational change, blocks its interactions with TRIF, MAVS and STING, and inhibits IRF3 homodimerization and type I interferon response. Sim-9 exhibits significant anti-inflammatory, organ-protective and survival benefits in mouse models of sepsis and acute pancreatitis. Sim-9 can be used for research related to inflammatory diseases.
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DC81535 SIK2/3-IN-3
SIK2/3-IN-3 (Example 15) is a potent, selective SIK2/3 inhibitor that exhibits preferential inhibitory activity against SIK2 (IC50 = 10.3 nM) and SIK3 (IC50 = 0.8 nM) over SIK1 (IC50 = 801 nM). SIK2/3-IN-3 can be used for the study of inflammatory diseases.
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DC81534 SIK2/3-IN-2
SIK2/3-IN-2 (compound 12, compound I-200) is a potent SIK2/3 inhibitor (SIK2 IC50 = 65 nM, SIK3 IC50 = 14 nM). SIK2/3-IN-2 is also a p21-activated protein kinase (PAK) 1 inhibitor with a Ki of 20.7 nM. SIK2/3-IN-2 can be used for hyperproliferative diseases and cancer research, such as Paclitaxel-resistant ovarian cancer.
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DC81533 SIAIS001
SIAIS001 is a potent and orally active PROTAC ALK degrader with a DC50 of 3.9 nM. SIAIS001 induces G1/S phase cell cycle arrest and inhibits proliferation of SR cells (IC50 = 0.9 nM). SIAIS001 can be used for non-small cell lung cancer (NSCLC) and anaplastic large-cell lymphomas (ALCLs) research. (Pink: Anaplastic lymphoma kinase (ALK) ligand ; Blue: TNF Receptor ligand ; Black: linker).
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DC81532 SHP2-IN-46
SHP2-IN-46 is an orally active SHP2 inhibitor (IC50 = 11.76 μM). SHP2-IN-46 inhibits SHP2 enzymatic activity and mediates anti-tumor activity. SHP2-IN-46 suppresses cell proliferation in various cancer cells. SHP2-IN-46 can be used in research related to lung adenocarcinoma, pancreatic cancer and hepatoblastoma.
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DC81531 SHK1112218
SHK1112218 is an orally active mitochondrial proton carrier with an EC50 of 0.48 μM. SHK1112218 restores proton transport and increases oxygen consumption rate. SHK1112218 can be used for the research of diabetes, obesity, and metabolic dysfunction-associated steatotic liver disease.
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DC81530 SH-273
SH-273 is a dual targeting compound. SH-273 has dual function to stimulate STING function (EC50: 100 nM) and inhibits PI3Kγ (IC50: 7 nM). SH-273 can be used in the research of pancreatic cancer.
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DC81529 SGS-518
SGS-518 is a selective 5-HT6R antagonist. SGS518 can be used for the research of cognitive impairments such as amnesia, anxiety and depression, and it is effective in protecting mouse retina at high doses.
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DC81528 SGK1-IN-9
SGK1-IN-9 (Compound 1) is a SGK1 inhibitor. SGK1-IN-9 can be used in cancer research.
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DC81527 SGK1-IN-8
SGK1-IN-8 (compound 55) is a SGK1 and GSK3β inhibitor, with an IC50 of 0.11 μM against human SGK1 and an IC50 of 3.39 μM against human GSK3β. SGK1-IN-8 inhibits the catalytic activities of SGK1 and GSK3β, and reduces the phosphorylation level of TAU protein at the Ser214 site. SGK1-IN-8 is available for the research of Alzheimer's disease.
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DC81526 SGK1-IN-7
SGK1-IN-7 is a blood-brain barrier-permeable SGK1 inhibitor with an IC50 of 0.72 μM. SGK1-IN-7 reduces the phosphorylation level of TAU protein at the Ser396 and Ser214 epitopes. SGK1-IN-7 antagonizes the toxicity induced by Okadaic acid. SGK1-IN-7 can be used in the research of Alzheimer's disease.
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DC81525 SGI-1776-VHL-02-epimer
SGI-1776-VHL-02-epimer (SGI-1776-cis-VHL-02) is an epimer control compound of with SGI-1776-VHL-02. SGI-1776-VHL-02-epimer has an inverted stereocenter in the critical hydroxyl-proline group in the VHL ligand. SGI-1776-VHL-02-epimer cannot trigger the VHL E3 ligase complex and does not degrade PIM1.
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DC81524 SGI-1776-VHL-02
SGI-1776-VHL-02 is a stereoselective PIM PROTAC degrader. SGI-1776-VHL-02 promotes the ubiquitination and degradation of PIM1, PIM2 and PIM3. SGI-1776-VHL-02 downregulates c-myc protein levels, induces Apoptosis, and reduces the colony-forming ability of prostate cancer cells. SGI-1776-VHL-02 can be used in studies related to prostate cancer. (Pink: Pim and Autophagy and Apoptosis ligand ; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker ).
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DC81523 SG-210
SG-210 (SPR 210) is an orally active and selective aldose reductase (AR) inhibitor. SG-210 has IC50 values of 9.5 nM and 10 nM for AR from porcine lens and human placenta, respectively. SG-210 can inhibit sorbitol accumulation and ameliorate diabetic neuropathy and retinopathy in Streptozotocin-induced diabetic rats. SG-210 can be used in the research of diseases such as diabetes-related complications.
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DC81522 SET7-IN-DC21
SET7-IN-DC21 is a selective, potent SET7 inhibitor (IC50 = 15.93 μM; KD = 18.00 μM). SET7-IN-DC21 has good selectivity for several other epigenetic targets, such as SUV39H1, G9a, NSD1, DOT1L and MOF. SET7-IN-DC21 can be used for the researches of cancer, infection, inflammation, metabolic and cardiovascular disease, such as breast cancer.
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