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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
117 Results for "
Small-molecule activator
" in MedChemExpress (MCE) Product Catalog:
Products (117)
117 Results for "Small-molecule activator" in MCE Product Catalog:
8
8 Publications Verification
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5-A-RU-PABC-Val-Cit-Fmoc is the proagent of 5-A-RU . 5-A-RU, a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways .
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8 Publications Verification
FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg 2+ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers .
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5
5 Cited Publications
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EN6 is a small-molecule in vivo autophagy activator that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase. EN6-mediated modification of ATP6V1A uncouples v-ATPase from Rag, leading to inhibition of mTORC1 signalling, increased lysosomal acidification, and activation of autophagy. EN6 also scavenges TDP-43 aggregates (causative agents of frontotemporal dementia) in a lysosome-dependent manner .
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5 Cited Publications
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UCL-TRO-1938 is a potent small molecule allosteric activator of PI3Kα with an EC50 value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective effects from ischaemia reperfusion injury and enhances nerve regeneration following nerve crush .
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3 Cited Publications
Synonyms: Abequolixron hydrochloride
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RGX-104 hydrochloride is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
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2 Cited Publications
Cat. No.: HY-19767
CAS No.: 1629249-33-7
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GSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer .
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2 Cited Publications
Cat. No.: HY-19767A
CAS No.: 1629249-40-6
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GSK 3008348 hydrochloride is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer .
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2 Cited Publications
ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer.
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1 Cited Publications
Synonyms: Somalix; RO-7486967; IZD334
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Selnoflast (RO7486967), formerly somalix/RG6418/IZD334, is an orally active, potent, selective and reversible small molecule NLRP3 inflammasome inhibitor. Selnoflast is a potent inhibitor of IL-1β release stimulated by NLRP3 activation in human Alzheimer's disease (AD) monocyte-derived macrophages. Selnoflast is promising for research of AD and systemic inflammatory diseases, such as ulcerative colitis and chronic obstructive pulmonary disease .
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1 Cited Publications
Cat. No.: HY-W011890
CAS No.: 38609-97-1
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Cridanimod is a potent progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression. Cridanimod is a small-molecule immunomodulator and interferon inducer .
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1 Cited Publications
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HPA-12 is a blood-brain barrier-permeable small-molecule inhibitor of ceramide transfer protein (CERT) with four stereoisomers (the (1R,3R)-stereoisomer exhibits the highest activity). HPA-12 blocks the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus by binding to the START domain of CERT, leading to intracellular ceramide accumulation and inhibition of sphingomyelin (SM) synthesis. HPA-12 induces endoplasmic reticulum stress via the GRP78/ATF6/CHOP axis and activates mitochondrial autophagy, thereby inhibiting cell growth and inducing apoptosis. In in vivo experiments, HPA-12 significantly reduces the leukemia burden and splenomegaly in mouse models of acute myeloid leukemia (AML) and prolongs survival. HPA-12 is applicable for the research of lipid metabolism in acute myeloid leukemia and Alzheimer's disease .
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1 Cited Publications
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RBN013209 is an orally active small molecule inhibitor of CD38 with an IC50 of 0.01 to 0.1 μM for human CD38. RBN013209 prevents the conversion of extracellular NAD + to ADPR or cADPR in tumor cells and PBMCs. RBN013209 can be used in the study of tumor. In addition, RBN013209 enables CAR-T cells to maintain the naive state and central memory state, and decreases the expression of cell activation markers and exhaustion-related inhibitory receptors .
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1 Cited Publications
Cat. No.: HY-153713
Purity: 98.05%
MYC-RIBOTAC is a nucleic acid-targeting degrader (ribonuclease-targeting chimera, RIBOTAC) that targets the MYC internal ribosome entry site (IRES). MYC-RIBOTAC contains a MYC mRNA binding component and a small molecule that recruits and locally activates RNAse L1. MYC-RIBOTAC reduces MYC mRNA and protein expression levels, induces cell apoptosis, and can be used for antitumor research . MYC-RIBOTAC consists of pre-miR-155 binder Anticancer agent 167 (HY-156839), RNA binder NCI-B16 (HY-156215), and Linker Amino-PEG4-alcohol (HY-W008005).
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1
1 Cited Publications
Cat. No.: HY-10219G
CAS No.: 53123-88-9
Synonyms: Sirolimus (GMP); AY-22989 (GMP); NSC 226080 (GMP)
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1 Cited Publications
Cat. No.: HY-170327
CAS No.: 664975-73-9
ZCL279 is a small molecule modulator (SMM) that inhibits Cdc42-intersectin (ITSN) interaction. ZCL279 can activate Cdc42 (a cytoplasmic small GTPase in the Ras superfamily) at lower concentrations (<10 μM) and significantly inhibit it at higher concentrations (<10 μM) .
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TRP Channel Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Keap1-Nrf2 Amyloid-β Fungal Apoptosis
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis .
Synonyms: BMS-649
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SR11237 (BMS-649) GMP is SR11237 (HY-107413) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SR11237 is a RXR activator and lipid metabolism regulator that promotes the differentiation of induced neural stem cells into dopaminergic (TH-positive) neurons. SR11237 induces transcriptional regulation of lipogenic genes and cholesterol transporters, increases glycosaminoglycan release, and elevates total cellular triglyceride levels. SR11237 promotes heterodimerization of RXR with Nurr1, thereby enhancing tyrosine hydroxylase expression and facilitating dopamine release. SR11237 produces a synergistic effect when used in combination with bFGF/EGF. SR11237 is mainly used in studies related to osteoarthritis and Parkinson's disease .
Cat. No.: HY-174216
CAS No.: 3068830-89-4
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PZL-A is a activator of mitochondrial DNA (mtDNA) synthesis. PZL-A restores wild-type-like activity to mutant forms of polymerase γ (POLγ) with AC50 s of 160 and 20 nM for A467T and G848S. PZL-A activates mtDNA synthesis in cells, enhancing biogenesis of the oxidative phosphorylation machinery and cellular respiration. PZL-A is promising for relieving POLG disease and other severe conditions linked to depletion of mtDNA .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
