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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
10071 Results for "
activators
" in MedChemExpress (MCE) Product Catalog:
Products (10071)
10071 Results for "activators" in MCE Product Catalog:
Cat. No.: HY-16342
CAS No.: 827034-92-4
Target:
Domaines de recherche:
NA808 is an Serine Palmitoyltransferase (SPT) inhibitor. NA808 reduces sphingomyelin synthesis, inhibits its activation in hepatic stellate cells, and decreases the expression of α-SMA protein and mRNA, as well as collagen 1A1 mRNA (IC50 0.16, 0.12, and 0.11 μM, respectively). NA808 inhibits HCV replication and reduces NS3 and RdRp protein expression in HCV replicon cells without significant cytotoxicity and exhibits almost no immunosuppressive effect at effective concentrations. NA808 demonstrates broad-spectrum antiviral activity in humanized chimeric liver mice infected with various HCV genotypes, and dose-dependently reduces serum and hepatic HCV RNA levels. NA808 can be used for research on non-alcoholic steatohepatitis and hepatitis C virus infection .
Cat. No.: HY-164530
CAS No.: 1970149-05-3
SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines .
Cat. No.: HY-165459
CAS No.: 401907-57-1
Synonyms: MK-056
Target:
Domaines de recherche:
KJM429 (MK-056) is a high-affinity ligand for the rat vanilloid receptor rTRPV1 (Ki=30-63 nM) with a unique dual regulatory function. KJM429 acts as a competitive antagonist to inhibit TRPV1 receptor activation induced by Capsaicin (HY-10448), resiniferatoxin, thermal stimulation and weak acid (pH 6.0), and switches to a TRPV1 agonist under strong acid conditions (pH<5.5). KJM429 effectively blocks calcium influx induced by Capsaicin and partial thermal stimulation, and triggers calcium uptake under low pH conditions, with minimal effects on non-TRPV1-mediated calcium signaling. KJM429 can be used for research on the mechanisms of pain-related diseases such as postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis and pruritus .
Cat. No.: HY-167874
CAS No.: 2488255-42-9
Domaines de recherche:
ASP-8731 is an orally active BACH1 inhibitor. ASP-8731 activates antioxidant, anti-inflammatory and globin gene pathways by relieving the inhibitory effect of BACH1 on NRF2-mediated gene transcription. ASP-8731 significantly upregulates the expression of HMOX1, FTH1 and various globins (such as HGB, HBG, HBA), increases fetal hemoglobin (HbF) levels, and effectively induces F-cell production in hydroxyurea-unresponsive cells. Meanwhile, ASP-8731 reduces inflammatory responses and white blood cell counts by downregulating VCAM1, ICAM-1 and the phosphorylation level of NF-κB(p65), and blocks heme-induced glutathione depletion and microcirculatory stasis. ASP-8731 holds potential for inhibiting sickle cell disease and related hematological disorders .
Cat. No.: HY-168954
CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC50 of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22% .
Cat. No.: HY-169279
Target:
Domaines de recherche:
PROTAC PXR degrader-1 is a PROTAC degrader targeting PXR, with a DC50 value of 49.8 nM in SNU-C4 3xFLAG-PXR KI cells. PROTAC PXR degrader-1 exhibits selectivity towards CAR, VDR, FXR, LXRα and LXRβ. PROTAC PXR degrader-1 induces the formation of a ternary complex with PXR and VHL, triggering proteasomal degradation of PXR. PROTAC PXR degrader-1 reduces both agonist-induced and basal PXR-mediated CYP3A4 promoter activation, and decreases the expression of endogenous CYP3A4 gene in cancer cells. PROTAC PXR degrader-1 enhances the cytotoxic effect of paclitaxel on cancer cells. PROTAC PXR degrader-1 can be used for the research of colorectal cancer .
Cat. No.: HY-169481
CAS No.: 3027918-96-0
Domaines de recherche:
AP-1 is a targeted ALK PROTAC degrader. AP-1 effectively degrades various ALK fusion/mutation forms, including degradation of NPM-ALK (DC50 = 4.6 nM) and EML4-ALK (DC50 = 357.6 nM), and exhibits a typical hook effect at high concentrations. AP-1 inhibits phosphorylation of downstream STAT3, downregulates gene expression in the JAK-STAT pathway, and kills ALK-positive tumor cells via activating the caspase-3-dependent apoptosis pathway. AP-1 shows cytotoxicity against a variety of cancer cells and possesses anti-tumor activity. AP-1 can be used in research related to non-small cell lung cancer, neuroblastoma, and anaplastic large cell lymphoma .
Cat. No.: HY-171837A
CAS No.: 678138-44-8
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t9,t11,c15-CLNA is a conjugated linolenic acid (CLNA) isomer produced by Lactobacillus plantarum ZS2058. t9,t11,c15-CLNA has the main activities of anti-inflammatory, antioxidant and improving intestinal barrier function. The regulatory mechanism of t9,t11,c15-CLNA includes upregulation of tight junction proteins, inhibition of pro-inflammatory cytokines (such as TNF-α, IL-6) and activation of antioxidant enzymes (such as SOD, CAT). t9,t11,c15-CLNA can be used in the study of inflammatory bowel diseases (such as colitis) .
Cat. No.: HY-171949
CAS No.: 18866-87-0
Synonyms: 3α,7α,12α,25-Tetrahydroxycoprostane
Domaines de recherche:
5β-Cholestane-3α,7α,12α,25-tetrol (3α,7α,12α,25-Tetrahydroxycoprostane) is a bile acid alcohol. 5β-Cholestane-3α,7α,12α,25-tetrol is a GPBAR1 (also known as TGR5) activator (EC50: 1.36 μM). 5β-Cholestane-3α,7α,12α,25-tetrol is the predominant bile-alcohol disease marker present in patients with Cerebrotendinous xanthomatosis (CTX) .
Cat. No.: HY-175275
CAS No.: 488815-65-2
Synonyms: BEM
Domaines de recherche:
10-Butyl Ether Minocycline (BEM), a Minocycline (HY-17412A) derivative, is an MMP-8 and MMP-9 inhibitor with IC50s of 69.4 µM and 47.0 µM, respectively. 10-Butyl Ether Minocycline suppresses LPS (HY-D1056)-induced microglial activation. 10-Butyl Ether Minocycline inhibits VEGF-induced endothelial cell migration and L-Glutamine (HY-N0390)-induced ROS levels. 10-Butyl Ether Minocycline significantly reduces alcohol consumption in the Chronic Intermittent Ethanol (CIE) mouse model of alcohol dependence. 10-Butyl Ether Minocycline can be used for the study of neuroimmune-inflammatory diseases and Alcohol use disorder (AUD) .
Cat. No.: HY-176724
Domaines de recherche:
ZnPc-O3-JQ1 is a photoactivatable BRD4-targeting degrader and photosensitizer, composed of monosubstituted amino zinc phthalocyanine (ZnPc), the BRD4 ligand JQ1, and a PEG linker. Upon activation by light, ZnPc-O3-JQ1 generates reactive oxygen species (ROS) and induces BRD4 degradation in an E3 ubiquitin ligase-independent manner. BRD4 degradation further reduces HIF-1α and GCL levels and restricts the SLC7A11/GSH-related antioxidant response, thereby enhancing photodynamic therapy-associated oxidative stress. ZnPc-O3-JQ1 can be used in research related to bladder cancer .
Cat. No.: HY-177277
CAS No.: 1549766-06-4
Target:
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HM5023507 is an orally active and selective PI3Kδ/γ inhibitor with IC50s of 4 and 5 μM for PI3Kδ and PI3Kγ over PI3Kβ and PI3Kα. HM5023507 attenuates the PI3Kδ/γ signaling in human basophils. HM5023507 also attenuates the activation and function of human B and T cells and cytokine and IgG production during cocultures, and Th17 differentiation of CD4 T cells. HM5023507 inhibited semiestablished collagen-induced arthritic inflammation in the rat models. HM5023507 can be used for inflammatory diseases like rheumatoid arthritis research .
Cat. No.: HY-178281
CAS No.: 931928-13-1
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E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research .
Cat. No.: HY-178721
CAS No.: 2768690-22-6
Domaines de recherche:
Lithocholic amide-C2-N(didecane) (Compound LC10) is a Lithocholic acid (HY-B0172) analogue. Lithocholic amide-C2-N(didecane) can form lipid nanoparticles spontaneously in the aqueous milieu, permeate through the skin, penetrate the deeper dermal layers, and exert anti-inflammatory effects against psoriasis-like chronic skin inflammations. Lithocholic amide-C2-N(didecane) can inhibit abnormal proliferation of keratinocytes, downregulate the mRNA expression of the psoriasis-associated receptor EphA2 and reduce serum levels of multiple pro-inflammatory factors such as IL-1α, IL-1β, and IFN-γ by inhibiting activation of the Th17/Th2 inflammatory pathway .
Cat. No.: HY-179047
CAS No.: 3040320-18-8
Domaines de recherche:
SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8 +T cells. SMU-L11-R shows potential in colorectal cancer studies .
Cat. No.: HY-179386
Target:
PARP Histone Methyltransferase Apoptosis Pyroptosis Necroptosis Reactive Oxygen Species (ROS) PANoptosis
Domaines de recherche:
PARP1/EZH2-IN-1 is a selective PARP1 and EZH2 dual inhibitor. PARP1/EZH2-IN-1 has IC50s of 28 nM, 414 nM and 74 nM for PARP1, PARP2 and EZH2, respectively. PARP1/EZH2-IN-1 inhibits the proliferation and migration of TNBC cells (triple-negative breast Cancer cells). PARP1/EZH2-IN-1 induces PANoptosis (Apoptosis, Pyroptosis and Necroptosis), increases the level of reactive oxygen species (ROS), and activates related inflammatory pathways. PARP1/EZH2-IN-1 can be used in triple-negative breast cancer research .
Cat. No.: HY-180245
Target:
STAT Ferroptosis Apoptosis Glutathione Peroxidase Bcl-2 Family Reactive Oxygen Species (ROS)
Domaines de recherche:
STAT3-IN-51 is a STAT3 inhibitor that directly binds to the STAT3 SH2 domain. STAT3-IN-51 induces apoptosis, ferroptosis, and immunogenic cell death (ICD) to potentiate anti-tumor immunity. STAT3-IN-51 inhibits STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling. STAT3-IN-51 induces ROS generation, decreases Bcl-2 expression, disruptes mitochondrial function, suppresses GPX4 activity, and promotes lipid peroxidation. STAT3-IN-51 can be used for the study of colorectal carcinoma, breast adenocarcinoma, non-small cell lung cancer (NSCLC) and Cisplatin (HY-17394)-resistant pulmonary adenocarcinoma .
Cat. No.: HY-180555
Domaines de recherche:
SN38-(PEG)2-Pom-α is a selective PROTAC RPL15 degrader. SN38-(PEG)2-Pom-α induces ubiquitin-mediated degradation of RPL15 without affecting TOP1. SN38-(PEG)2-Pom-α induces damage-associated molecular pattern (DAMP) secretion from cancer cells, which activated cGAS-STING signaling in dendritic cells. SN38-(PEG)2-Pom-α enhances anti-PD-1 immunotherapy in a murine melanoma tumor model expressing human CRBN. SN38-(PEG)2-Pom-α can be used for melanoma research .
Cat. No.: HY-180581
Target:
Domaines de recherche:
LOXL2/sGC modulator-1 (Compound 11k) is a LOXL2 inhibitor (IC₅₀ = 0.13 μM) and an sGC activator. LOXL2/sGC modulator-1 shows good selectivity for LOX (IC₅₀ > 45.9 μM) and LOXL3 (IC₅₀ = 1.30 μM). LOXL2/sGC modulator-1 significantly increases intracellular cGMP levels in the presence of the gGC inhibitor ODQ (HY-101255). LOXL2/sGC modulator-1 significantly inhibits hypoxia-induced collagen deposition and cross-linking, while promoting vasodilation. LOXL2/sGC modulator-1 can be used for the study of pulmonary arterial hypertension .
Cat. No.: HY-180585
Domaines de recherche:
LOXL2/sGC modulator-2 (Compound 9k) is a selective and orally active lysyl oxidase-like 2 (LOXL2) and soluble guanylate cyclase (sGC) dual-target regulator. LOXL2/sGC modulator-2 shows inhibitory activity for LOXL2 with an IC50 of 0.1 μM and can activate sGC. LOXL2/sGC modulator-2 can ameliorate vascular remodeling and reduce pulmonary artery pressure. LOXL2/sGC modulator-2 can downregulate PKG1, PCNA, α-SMA, collagen I and fibronectin levels. LOXL2/sGC modulator-2 can be used for the research of pulmonary arterial hypertension .
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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
