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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
44 Results for "
feedback
" in MedChemExpress (MCE) Product Catalog:
Products (44)
44 Results for "feedback" in MCE Product Catalog:
3
3 Cited Publications
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KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity .
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2 Cited Publications
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SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD +. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD + in mice .
1
Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC50 = 0.4 nM). Seldegamadlin inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) .
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1 Cited Publications
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ODN 2216 is a type A CpG oligodeoxynucleotide vaccine adjuvant and a TLR9 agonist. ODN 2216 interacts with TLR9 in the lysosomes of CD4 + T cells and activates feedback-dependent signaling pathways. ODN 2216 induces the production of type I interferons, IL-6 and TGF-β via the IRAK4/IRF7 axis, while increasing intracellular ATP levels. ODN 2216 not only induces the differentiation of CD4 + T cells into anti-inflammatory Th3-like regulatory phenotypes to inhibit autologous proliferation, but also enhances the specific CD8 + T cell-mediated cytotoxicity against Mammaglobin-A in breast cancer cells. ODN 2216 is widely used in studies related to breast cancer and systemic lupus erythematosus .
1
1 Cited Publications
Synonyms: AMG-510 racemate
Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research .
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1 Cited Publications
Synonyms: (-)-Scopolamine methyl bromide; Hyoscine methyl bromide
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Methscopolamine bromide ((-)-Scopolamine methyl bromide; Hyoscine methyl bromide) is a peripherally acting muscarinic receptor (mAChR) antagonist that cannot cross the blood-brain barrier. Methscopolamine bromide blocks the muscarinic negative feedback regulation of acetylcholine release from striatal cholinergic terminals, thereby increasing acetylcholine release in the striatum of freely moving rats. Methscopolamine bromide does not induce motor excitation in freely moving rats, nor does it alter the duration of ethanol-induced loss of righting reflex in mice. Methscopolamine bromide fails to antagonize the arecoline-mediated reduction in the duration of ethanol-induced loss of righting reflex in mice .
1
1 Cited Publications
Art. -Nr.: HY-150741C
Reinheit: 97.92%
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ODN 2216 sodium is a type A CpG oligodeoxynucleotide vaccine adjuvant and a TLR9 agonist. ODN 2216 sodium interacts with TLR9 in the lysosomes of CD4 + T cells and activates feedback-dependent signaling pathways. ODN 2216 sodium induces the production of type I interferons, IL-6 and TGF-β via the IRAK4/IRF7 axis, while increasing intracellular ATP levels. ODN 2216 sodium not only induces the differentiation of CD4 + T cells into anti-inflammatory Th3-like regulatory phenotypes to inhibit autologous proliferation, but also enhances the specific CD8 + T cell-mediated cytotoxicity against Mammaglobin-A in breast cancer cells. ODN 2216 sodium is widely used in studies related to breast cancer and systemic lupus erythematosus .
1
1 Cited Publications
Art. -Nr.: HY-162080
CAS. Nr.: 374705-10-9
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METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
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1 Cited Publications
Art. -Nr.: HY-162080A
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METTL1-WDR4-IN-1 (Compound 1) TFA is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50=144 μM). METTL1-WDR4-IN-1 TFA inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking the m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 TFA can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 TFA can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
Art. -Nr.: HY-106203
CAS. Nr.: 752253-39-7
Synonyms: SSR-125543
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Crinecerfont (SSR-125543) is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency . Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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AUT1 is a recombinant human Kv3 channel modulator. AUT1 modulates Kv3.1b and Kv3.2a channels in human recombinant with pEC50 values of 5.33 and 5.31 μM, respectively. AUT1 can be used for the research of disorders associated with dysfunction of inhibitory feedback in corticolimbic circuits, such as schizophrenia .
Art. -Nr.: HY-157421
CAS. Nr.: 2847156-05-0
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Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD +, thereby enhancing enzymatic activity and significantly increasing intracellular NAD + levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders .
Synonyms: SSR-125543 hydrochloride
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Crinecerfont (SSR-125543) hydrochloride is an orally effective corticotropin-releasing factor receptor type-1 (CRF1 receptor) antagonist. Crinecerfont hydrochloride blocks CRF1 receptor signaling to reduce adrenocorticotropic hormone secretion. Crinecerfont hydrochloride improves hypothalamic-pituitary-adrenal axis negative feedback sensitivity in chronically stressed mice. Crinecerfont hydrochloride can be used for the research of chronic stress conditions and classic congenital adrenal hyperplasia due to 21-hydroxylase deficiency . Crinecerfont hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Art. -Nr.: HY-156696
CAS. Nr.: 215183-03-2
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S3226 is a highly selective NHE-3 inhibitor (IC50<1 μM) that specifically blocks NHE-3-mediated sodium transport. S3226 significantly inhibits blastocyst formation and expansion in mouse embryos, and reduces fluid and electrolyte reabsorption in rat proximal tubules in a dose-dependent manner. S3226 effectively alleviates ischemia-induced acute renal failure by improving renal function parameters, reducing renal tubular injury and restoring intracellular pH homeostasis, without interfering with the normal tubuloglomerular feedback response. S3226 is widely used in studies of acute renal failure and related pathological mechanisms .
Art. -Nr.: HY-159190
CAS. Nr.: 2409140-12-9
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HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .
Art. -Nr.: HY-W019334
CAS. Nr.: 202842-98-6
Synonyms: 3,4-DMPP
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3,4-Dimethylpyrazole phosphate is a nitrification inhibitor. 3,4-Dimethylpyrazole phosphate decreases gross soil autotrophic nitrification rates and reduces gross mineralization rates through feedback regulation. 3,4-Dimethylpyrazole phosphate can also reduce the risk of nitrate leaching and N losses due to denitrification and do not increase NH3 volatilization .
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FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies .
Synonyms: KHK-IN-3
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Cardiovascular Disease Metabolic Disease Inflammation/Immunology
KHK-IN-3 (Example 1) is a ketohexokinase (KHK) inhibitor. KHK-IN-3 can be used in the study of kidney disease, nonalcoholic steatohepatitis (NASH), diabetes and heart failure. KHK is a rate-limiting enzyme and fructokinase involved in fructose metabolism. KHK catalyzes the phosphorylation of fructose to fructose-1-phosphate (FIP) at the expense of ATP. The lack of feedback inhibition of fructose metabolism triggers the accumulation of downstream intermediates such as lipogenesis, gluconeogenesis, and oxidative phosphorylation .
Art. -Nr.: HY-P11112
CAS. Nr.: 1609454-11-6
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Art. -Nr.: HY-P3019
CAS. Nr.: 357952-09-1
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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
