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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
2438 Results for "
decrease
" in MedChemExpress (MCE) Product Catalog:
Products (2438)
2438 Results for "decrease" in MCE Product Catalog:
Referencia número: HY-148032
No. CAS: 20776-45-8
Synonyms: 5-BT
Target:
Áreas de investigación:
5-Benzyloxytryptamine (5-BT) is a selective partial agonist for 5-hydroxytryptamine 1D/1B (5-HT1D/1B) receptors with an IC50 value of 40 nM for bovine caudate 5-HT1D and reduced affinity for other receptors (5-HT2 IC50>470 nM). 5-Benzyloxytryptamine inhibits adenylate cyclase to decrease neurotransmitter release and downregulate cAMP signaling. 5-Benzyloxytryptamine is promising for research of neurotransmitter imbalance-related disorders like migraine .
Referencia número: HY-150085
No. CAS: 2393881-77-9
Target:
Áreas de investigación:
GSK951 is a highly potent, selective, and reversibly covalent KLK5 inhibitor, with an IC50 of approximately 250 pM and a pIC50 of 9.6 against hKLK5. It exhibits over 100-fold selectivity over KLK7, KLK14, matriptase, and elastase. GSK951 binds to the catalytic site of KLK5 via covalent interaction with the catalytic serine, with a slow dissociation rate. GSK951 improves skin barrier function, reduces transepidermal water loss, decreases the expression of proinflammatory cytokines, and inhibits the elevated KLK5 protease activity in the stratum corneum. GSK951 can be used in studies related to skin barrier dysfunction.
Referencia número: HY-150661S
No. CAS: 2482467-12-7
Synonyms: 3-epi-25-Hydroxy Vitamin D3-13C5
Target:
Áreas de investigación:
3-epi-Calcifediol- 13C5 (3-epi-25-Hydroxy Vitamin D3- 13C5) is the 13C-labeled 3-epi-Calcifediol (HY-32351B). 3-epi-25-hydroxy Vitamin D3 is the C-3 epimer of 25-hydroxy vitamin D3.1 Dietary administration of 3-epi-25-hydroxy vitamin D3 (0.5 and 1 IU/g) decreases levels of serum parathyroid hormone (PTH) in male, but not female, weanling rats.
Synonyms: Q702
Target:
Áreas de investigación:
Adrixetinib (Q702) is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib acts as a potent immune modulator that remodels the tumor microenvironment. Adrixetinib increases the abundance of M1 macrophages and CD8⁺ T cells, while decreasing the levels of M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib upregulates the expression of MHC class I and E-cadherin in tumor cells. Adrixetinib shows remarkable antitumor efficacy in syngeneic mouse tumor models. Adrixetinib is suitable for the research of breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma .
Referencia número: HY-16347
No. CAS: 290296-54-7
Synonyms: CID 6451149 hydrochloride
Target:
Áreas de investigación:
Netupitant hydrochloride (CID 6451149 hydrochloride) is a blood-brain barrier penetrable, orally active NK1 receptor inhibitor with a Ki of 0.95 nM (CHO cells) against the human receptor. Netupitant hydrochloride antagonizes the effects induced by Substance P, inhibits the maximal response of Substance P with a long-lasting action, and suppresses NK1 agonist-induced behaviors in mice and gerbils. Netupitant hydrochloride reduces the frequency of bladder contractions, prolongs contraction intervals, decreases basal pressure at high doses, and acts on the afferent branch of the micturition reflex. Netupitant hydrochloride can be used in research related to overactive bladder, chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, anxiety disorders, and depression .
Referencia número: HY-164896
No. CAS: 3080918-74-4
PIN1 degrader-2 is a covalent PIN1 degrader with an IC50 of 4.1 nM. PIN1 degrader-2 induces a decrease in the thermal stability of PIN1 and triggers concentration-dependent PIN1 degradation in various cancer cells. PIN1 degrader-2 covalently modifies PIN1 Cys113. PIN1 degrader-2 also reduces the cell viability of pancreatic cancer, breast cancer, prostate cancer and lung cancer cells. PIN1 degrader-2 can be used in research related to pancreatic cancer, breast cancer, prostate cancer and non-small cell lung cancer .
Referencia número: HY-169061
Áreas de investigación:
WQQ-345 is an orally active BCAT1 inhibitor with an IC50 values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer .
Referencia número: HY-171099
No. CAS: 2245949-62-4
Synonyms: LI-2124
Target:
Áreas de investigación:
SC-919 is an orally active IP6K inhibitor, with an IC50 of < 5.2 nM against IP6K1, < 3.8 nM against IP6K2, and 0.65 nM against IP6K3. By inhibiting the activity of IP6K, SC-919 reduces intracellular IP7 levels, thereby suppressing XPR1-mediated cellular phosphate efflux. SC-919 increases intracellular phosphate and ATP levels while reducing phosphate entry into the bloodstream, thus decreasing plasma phosphate levels. SC-919 can be used in research related to chronic kidney disease and hyperphosphatemia .
Referencia número: HY-175857
HDAC-IN-92 is a pan-HDAC inhibitor with an IC50 of 12.58 µM in A2780 cells. HDAC-IN-92 demonstrates broad-spectrum, notable cytotoxic activity against a range of human cancer cell lines, including ovarian, liver, and breast carcinomas. HDAC-IN-92 causes apoptosis and demonstrates a notable decrease in tumor cell colony formation. HDAC-IN-92 inhibits the formation of blood vessels in the chick chorioallantoic membrane (CAM). HDAC-IN-92 exhibits anti-tumor effect in a 4T1 tumor-bearing mouse model. HDAC-IN-92 can be used for research targeting solid tumor .
Referencia número: HY-17587R
No. CAS: 36861-47-9
Synonyms: 4-MBC (Standard); Enzacamene (Standard)
Target:
Áreas de investigación:
4-Methylbenzylidene camphor (Standard) is the analytical standard of 4-Methylbenzylidene camphor. This product is intended for research and analytical applications. 4-Methylbenzylidene camphor (4-MBC) is an endocrine disrupter that produces estrogen-like effects. 4-Methylbenzylidene camphor decreases the proliferation of human trophoblast cells and induces apoptosis. 4-Methylbenzylidene camphor activates PI3K/AKT and ERK1/2 signaling pathways and elevates intracellular ROS production. 4-Methylbenzylidene camphor is a ultraviolet (UV) filter and may hamper normal placental formation during early pregnancy .
Referencia número: HY-178042
No. CAS: 2756257-56-2
SS-3091 is a pan-KRas inhibitor active across KRas G12D, KRas G12C, KRas G12V, KRas G12S mutants, with minimal effects on non-KRas-driven cancer cells. SS-3091 binds to the KRas·ARaf interaction interface, destabilizes the complex, and attenuates KRas activity. SS-3091 suppresses phosphorylation of S6K, Akt, and ERK. SS-3091 reduces proliferation and decreases colony formation of cancer cells bearing KRas G12 mutations. SS-3091 can be used for the research of KRas-driven cancers .
Referencia número: HY-178383
Target:
Áreas de investigación:
α-Glucosidase-IN-98 is a potent orally active α-Glucosidase inhibitor with an IC50 of 18.1 μM. α-Glucosidase-IN-98 reversibly binds with α-Glucosidase via hydrogen bonds, electrostatic interactions and hydrophobic effects, which induces significant conformational alterations in the secondary structure of α-Glucosidase. α-Glucosidase-IN-98 decreases postprandial hyperglycemia in Starch (HY-B2225B)/Sucrose (HY-B1779)-challenged mice. α-Glucosidase-IN-98 can be used for type 2 diabetes mellitus (T2DM) research .
Referencia número: HY-179003
Target:
mTOR Glutaminase Reactive Oxygen Species (ROS) Autophagy Apoptosis Ferroptosis Glutathione Peroxidase
Áreas de investigación:
mTOR/GLS1-IN-1 (Compoud 9d) is a potent dual targeted mTOR/GLS1 inhibitor. Has anti proliferative activity against various tumor cells. mTOR/GLS1-IN-1 dose dependently induces ROS accumulation, induces autophagosome formation, and induces apoptosis. mTOR/GLS1-IN-1 can increase Fe 2+, decrease GPX4, and induce ferroptosis. mTOR/GLS1-IN-1 can inhibit cell migration, invasion, and angiogenesis. mTOR/GLS1-IN-1 can be used in the research of cancer, such as breast cancer .
Referencia número: HY-181818
Áreas de investigación:
4,5-Dehydro-6-oxoallosecurinine is a Keap1-Nrf2 pathway activator. 4,5-Dehydro-6-oxoallosecurinine promotes the nuclear translocation of Keap1-Nrf2, and induces the expression of antioxidant and cytoprotective genes. 4,5-Dehydro-6-oxoallosecurinine reduces the production of NO, and decreases the levels of iNOS, TNF-α, IL-6 and IL-1β in LPS-stimulated microglia. 4,5-Dehydro-6-oxoallosecurinine can be used for the research of neurodegenerative diseases .
Referencia número: HY-182300
No. CAS: 171092-64-1
Target:
Áreas de investigación:
FE 999011 is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with IC50 values of 7 nM and 3 nM against human and rat sources, respectively. FE 999011 acts as a glucose tolerance-improving agent and a GLP-1 receptor activator, which reduces blood glucose fluctuation, promotes GLP-1 release and decreases the insulin-glucose ratio. FE 999011 regulates lipid metabolism, delays the onset of diabetes, stabilizes food and water intake, reduces hypertriglyceridemia, prevents the elevation of free fatty acids, and delays the progression of impaired glucose tolerance to disease. FE 999011 can be used in relevant studies of type 2 diabetes .
Referencia número: HY-183057
No. CAS: 2234900-83-3
Áreas de investigación:
GRK2 modulator 1 is an orally active, brain-penetrant and selective GRK2 modulator. GRK2 modulator 1 enhances the active, non-phosphorylated GRK2 and prevents mitochondrial GRK2 and TOMM6 aggregation. GRK2 modulator 1 enhances the non-amyloidogenic processing of APP and prevent PHF-tau, neurodegeneration, and neuronal loss. GRK2 modulator 1 decreases the senescence marker, UPAR, reduces the Alzheimer disease (AD)-related mortality, and prolongs survival. GRK2 modulator 1 exerts neuroprotection by inhibiting HDAC6, and counteracts age-related cardiac dysfunction. GRK2 modulator 1 can be used for research on AD .
Referencia número: HY-18314B
No. CAS: 504433-24-3
Target:
Áreas de investigación:
(Z)-GW 441756 is a hepatocyte nuclear factor 4α (HNF4α) activator, with an EC50 of 9.2 μM and a Ka of 4.6 μM in human systems. (Z)-GW 441756 directly interacts with the ligand-binding domain of HNF4α via persistent hydrogen bonds and hydrophobic interactions within the binding pocket. (Z)-GW 441756 reduces the accumulation of triglycerides and total cholesterol. (Z)-GW 441756 inhibits ferroptosis through a non-antioxidant mechanism. (Z)-GW 441756 decreases plasma triglyceride and total cholesterol levels in animal models of hyperlipidemia. (Z)-GW 441756 can be used in studies related to hyperlipidemia .
Referencia número: HY-184312
No. CAS: 1031072-40-8
Áreas de investigación:
PPAR agonist 8 is an orally active pan-PPAR agonist, with KD values of 0.576 μM, 2.06 μM and 1.45 μM for PPARα, PPARγ and PPARδ, respectively. PPAR agonist 8 upregulates the expression of ATP-binding cassette transporter A1 (ABCA1) and promotes cholesterol efflux. PPAR agonist 8 reduces plasma cholesterol levels, decreases cholesterol accumulation in the liver and cholesterol deposition in pancreatic islets, regulates glucose and lipid metabolism, and causes no side effects of weight gain and obesity. PPAR agonist 8 can be used in the research of type 2 diabetes, hepatic steatosis and pancreatic islet dysfunction .
Referencia número: HY-187214
Áreas de investigación:
PROTAC G9a degrader-1 is a selective and orally active G9a PROTAC degrader with a DC50 of 1.29 μM. PROTAC G9a degrader-1 inhibits the NF-κB signaling pathway, suppresses the proliferation and migration of cancer cells, promotes apoptosis and cell cycle arrest, and reduces the expression level of H3K9me2. In in vivo models, PROTAC G9a degrader-1 alleviates skin inflammation, reduces epidermal hyperplasia, and decreases Ki67 expression. PROTAC G9a degrader-1 can be used for the research of triple-negative breast cancer and psoriasis .
Referencia número: HY-187219
Áreas de investigación:
CX-Se13 is an orally active pulmonary fibrosis inhibitor with anti-inflammatory and antioxidant activities. CX-Se13 regulates the Keap1/Nrf2/HO-1/NQO1, YAP/TAZ-TEAD, NF-κB p65 and TGF-β/Smads signaling pathways. CX-Se13 activates the cellular antioxidant defense system, restores redox balance, alleviates inflammatory responses, reduces collagen deposition, decreases pro-inflammatory cytokine levels and inhibits pathological progression. CX-Se13 can be used in studies related to pulmonary fibrosis .
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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
