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Pathways Recommended: PI3K/Akt/mTOR
Results for "

K site

" in MedChemExpress (MCE) Product Catalog:

57

Inhibitors & Agonists

2

Screening Libraries

1

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5

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6

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101562
    Inavolisib
    5+ Cited Publications

    GDC-0077; RG6114

    		 PI3K Apoptosis Cancer
    Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
    Inavolisib
  • HY-100355
    C18-Ceramide (d18:1/18:0)

    C18-Ceramide

    		 Endogenous Metabolite Neurological Disease Cancer
    C18-Ceramide (d18:1/18:0) is a bioactive molecule with multiple functions in cells, not a traditional agonist or inhibitor targeting a single site. It can act on multiple cellular targets, such as proteins related to endoplasmic reticulum stress (e.g., ATF-4, XBP-1, CHOP), proteins in the PI3K/AKT signaling pathway, and SNARE complex proteins. It exerts activities like inducing cell death, promoting autophagy, and regulating exocytosis through mechanisms such as activating endoplasmic reticulum stress, inhibiting the PI3K/AKT signaling pathway, and affecting lipid raft - related functions. It can be used in research on the mechanism of neuronal injury in the field of neuroscience and in the treatment research of cancers such as glioma in the field of oncology .
    C18-Ceramide (d18:1/18:0)
  • HY-N2593
    Isorhapontigenin
    4 Publications Verification

    		 Carnitine Palmitoyltransferase (CPT) Reactive Oxygen Species (ROS) Autophagy Apoptosis NF-κB PI3K Akt MMP Keap1-Nrf2 Metabolic Disease Inflammation/Immunology Cancer
    Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes .
    Isorhapontigenin
  • HY-111126
    K67
    1 Publications Verification

    		 p62 Keap1-Nrf2 Cancer
    K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2 .
    K67
  • HY-106005
    MMV390048
    3 Publications Verification

    		 Parasite PI4K Infection
    MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent .
    MMV390048
  • HY-B0633D
    Hyaluronic acid sodium (MW 200-1560)

    		CD44 Endogenous Metabolite Bacterial Akt PI3K Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Hyaluronic acid sodium (MW 200-1560) is a biopolymer composed of repeating disaccharide units, with a molecular weight of 200-1560. Hyaluronic acid sodium is a major component of the extracellular matrix (ECM). It is synthesized on the plasma membrane. Hyaluronic acid sodium exerts its effects by binding to receptors CD44 and RHAMM. Hyaluronic acid sodium activates PI3K-Akt signaling. Hyaluronic acid sodium also enhances cell invasion and angiogenesis by promoting or stimulating the binding of proteolytic MMP-9 to the cell surface. Elevated hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion, and angiogenesis in digestive system cancers. Hyaluronic acid sodium is involved in tissue remodeling and rapid cell proliferation in several physiological processes, including embryonic morphogenesis and wound healing. Hyaluronic acid sodium can be used as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid sodium can be used as a drug delivery carrier for sodium butyrate, enhancing its anti-proliferative activity against breast cancer cell lines. Hyaluronic acid sodium can lubricate the corneal endothelium. Hyaluronic acid sodium can improve tissue hydration and enhance the resistance of cells to mechanical damage. Hyaluronic acid sodium has been conjugated with antibodies to ensure that the active compound continues to exert its effects at the site of inflammation. Hyaluronic acid sodium can be used in research in the fields of osteoarthritis, ophthalmology, cosmetic dermatology, oncology, and liver diseases .
    Hyaluronic acid sodium (MW 200-1560)
  • HY-B0633E
    Hyaluronic acid, low endotoxin

    Hyaluronan, low endotoxin; Hyaluronate, low endotoxin

    		 Endogenous Metabolite CD44 Bacterial Akt PI3K Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Hyaluronic acid, low endotoxin (Hyaluronan, low endotoxin) is a biopolymer composed of repeating disaccharide units containing low levels of endotoxin. Hyaluronic acid is a major component of the extracellular matrix (ECM). It is synthesized on the plasma membrane. Hyaluronic acid exerts its effects by binding to receptors CD44 and RHAMM. Hyaluronic acid activates PI3K-Akt signaling. Hyaluronic acid also enhances cell invasion and angiogenesis by promoting or stimulating the binding of proteolytic MMP-9 to the cell surface. Elevated hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion, and angiogenesis in digestive system cancers. Hyaluronic acid is involved in tissue remodeling and rapid cell proliferation in several physiological processes, including embryonic morphogenesis and wound healing. Hyaluronic acid can be used as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid can be used as a drug delivery carrier for sodium butyrate, enhancing its anti-proliferative activity against breast cancer cell lines. Hyaluronic acid can lubricate the corneal endothelium. Hyaluronic acid can improve tissue hydration and enhance the resistance of cells to mechanical damage. Hyaluronic acid has been conjugated with antibodies to ensure that the active compound continues to exert its effects at the site of inflammation. Hyaluronic acid can be used in research in the fields of osteoarthritis, ophthalmology, cosmetic dermatology, oncology, and liver diseases .
    Hyaluronic acid, low endotoxin
  • HY-102047B
    KDOAM-25 citrate
    Maximum Cited Publications
    9 Publications Verification

    		 Histone Demethylase Cancer
    KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
    KDOAM-25 citrate
  • HY-148907
    CS640

    		CaMK MEK Mixed Lineage Kinase RIP kinase Tau Protein Neurological Disease
    CS640 (Compound 19) is a chemical probe and a calmodulin-dependent kinase inhibitor. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, MEK5, RIPK4, mLK3 and PIP5K1, with IC50 values of 8, 3, 1, 1, 25 nM, 5.69, 2.75 and 11.2 μM, respectively. CS640 blocks Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, but fails to protect primary mouse cortical neurons from Aβ-induced toxic damage. CS640 is applicable to research related to Alzheimer's disease .
    CS640
  • HY-110079
    TNP

    		IPK Superfamily Cancer
    TNP is a competitive, reversible inhibitor of IP6K1 and IP3K, with IC50s of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP competitively binds to the ATP binding site of IP6K, inhibits the generation of 5-IP7, and thus relieves the inhibition of 5-IP7 on the AKT signaling pathway. TNP can enhance insulin sensitivity and promote thermogenesis in adipose tissue. TNP cannot effectively pass through the blood-brain barrier and is mainly used in the study of obesity, type 2 diabetes, and metabolic syndrome. However, TNP also inhibits CYP3A4 and may need further optimization[1][2][3].
    TNP
  • HY-163944
    LL-K12-18

    		DNA/RNA Synthesis Molecular Glues CDK Apoptosis RAD51 ATM/ATR PARP Cancer
    LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .
    LL-K12-18
  • HY-P4322
    H-Ile-Lys-Val-Ala-Val-OH
    1 Publications Verification

    		 ERK Akt Neurological Disease Cancer
    H-Ile-Lys-Val-Ala-Val-OH is one of the most potent active sites of laminin-1. H-Ile-Lys-Val-Ala-Val-OH promotes cell adhesion, neurite outgrowth, and tumor growth. H-Ile-Lys-Val-Ala-Val-OH stimulates BMMSC population growth and proliferation by activating MAPK/ERK1/2 and PI3K/Akt signalling pathways .
    H-Ile-Lys-Val-Ala-Val-OH
  • HY-159098
    dWIZ-1

    		Molecular Glues PROTACs Histone Acetyltransferase Cardiovascular Disease
    dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease .
    dWIZ-1
  • HY-18674
    K-Ras-IN-1

    		Ras Cancer
    K-Ras-IN-1 is the inhibitor for K-Ras by occupying the binding site of son of sevenless (Sos), preventing the interaction between Sos and K-Ras, inhibiting the Sos-catalyzed GDP to GTP exchange process. K-Ras-IN-1 is promising for research of pancreatic, colon and lung cancer .
    K-Ras-IN-1
  • HY-162809
    XMU-MP-9

    		Ras Cancer
    XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1 and K-Ras, induces conformational changes in the Nedd4-1/K-Ras complex, promotes the ubiquitination and degradation of multiple K-Ras mutants, and inhibits the proliferation of cells carrying K-Ras mutants. XMU-MP-9 can be used for the study of colon, lung and pancreatic cancer .
    XMU-MP-9
  • HY-P11212
    Ac-RHKK(Ac)-AMC

    		Fluorescent Dye Metabolic Disease Cancer
    Ac-RHKK(Ac)-AMC (Compound S1) is a fluorescent substrate for SITR6, that is based on p53 sequence. Ac-RHKK(Ac)-AMC mimics H3K56 deacetylation site and significantly increases the deacetylation signal with low signal-to-background ratio. Ac-RHKK(Ac)-AMC can be used for ageing and cancers research .
    Ac-RHKK(Ac)-AMC
  • HY-174461
    PROTAC PI3Kα degrader-1

    		PROTACs PI3K Cancer
    PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885)) .
    PROTAC PI3Kα degrader-1
  • HY-150249
    GSK3735967
    1 Publications Verification

    		 DNA Methyltransferase Cancer
    GSK3735967 is an selective, reversible, non-nucleoside inhibitor of DNMT1 with an IC50 value of 40 nM. GSK3735967 contains a planar dicyanopyridine core that can specifically embed DNMT1 bound hemimethylated CpG dinucleotides. GSK3735967 has three binding sites, one of which can bind to histone H4K20me3 .
    GSK3735967
  • HY-147007
    β-catenin-IN-3
    1 Publications Verification

    		 β-catenin Wnt CDK Cancer
    β-catenin-IN-3 (Compound C2) is a selective β-catenin inhibitor. β-catenin-IN-3 binds to allosteric site on the surface of β-catenin with K D calculated at 54.96 nM. β-catenin-IN-3 selectively inhibits β-catenin via targeting a cryptic allosteric modulation site, lowers its cellular load. β-catenin-IN-3 significantly reduces viability of β-catenin driven cancer cells, and triggers β-catenin degradation via proteasome system in β-catenin-overexpressing cancer cells .
    β-catenin-IN-3
  • HY-N9362
    Emodinanthrone

    EmodAN

    		 Ferroptosis Antibiotic Cardiovascular Disease Infection
    Emodinanthrone (EmodAn) is a MARCH7 stabilizer that inhibits ferroptosis (EC50=70 nM). Emodinanthrone is also a precursor to Emodin (HY-14393) and possesses antibiotic activity. Emodinanthrone directly binds to MARCH7 and blocks its ubiquitination-mediated degradation at the K608 site; this action enhances MARCH7-mediated K48 ubiquitination and degradation of NCOA4, as well as its regulation of the intracellular localization of TFR1 via K63 ubiquitination, thereby reducing the intracellular labile iron pool and blocking ferroptosis. Emodinanthrone demonstrates in vivo cardioprotective effects and exhibits a favorable safety profile. Emodinanthrone is applicable to research on ferroptosis-related cardiovascular diseases, including Doxorubicin (HY-15142A)-induced cardiomyopathy and myocardial ischemia-reperfusion injury .
    Emodinanthrone
  • HY-156685
    EDI048

    		PI4K Parasite Infection Metabolic Disease Cancer
    EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children .
    EDI048
  • HY-N0857
    Deoxyandrographolide
    1 Publications Verification

    		 GLUT HDAC Virus Protease PI3K AMPK Akt Histone Demethylase MDM-2/p53 IFNAR Reactive Oxygen Species (ROS) Infection Metabolic Disease Inflammation/Immunology
    Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescence and virus infection .
    Deoxyandrographolide
  • HY-102047
    KDOAM-25

    		Histone Demethylase Cancer
    KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
    KDOAM-25
  • HY-150510
    MS8511

    		Histone Methyltransferase Neurological Disease Cancer
    MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
    MS8511
  • HY-155941
    5-Hydroxydecanoic acid

    		Potassium Channel Neurological Disease
    5-Hydroxydecanoic acid (5-HD） is a KATP channel antagonist，which has the effect of blocking the K KATP channel only during ischaemia by competing with the ATP binding site and does not affect pancreatic KATP channels .
    5-Hydroxydecanoic acid
  • HY-150510A
    MS8511 hydrochloride

    		Histone Methyltransferase Neurological Disease Cancer
    MS8511 (hydrochloride) is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 (hydrochloride) reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 (hydrochloride) can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
    MS8511 hydrochloride
  • HY-125969
    Rtt109 inhibitor 1

    		Histone Acetyltransferase Fungal Infection
    Rtt109 inhibitor 1 (Compound 1) is an inhibitor for histone acetyltransferase Rtt109 through a tight binding, uncompetitive system. Rtt109 inhibitor 1 exhibits antifungal activity through acetylation at H3K56 site .
    Rtt109 inhibitor 1
  • HY-P11213
    Ac-RYQK(Ac)-AMC

    		Fluorescent Dye Metabolic Disease Cancer
    Ac-RYQK(Ac)-AMC (Compound S5) is a fluorescent substrate for SITR6, that is based on the H3 sequence. Ac-RYQK(Ac)-AMC mimics H3K56 deacetylation site and significantly increases the deacetylation signal with superior signal-to-background ratio. Ac-RYQK(Ac)-AMC can be used for ageing and cancers research .
    Ac-RYQK(Ac)-AMC
  • HY-161800
    Aminoacyl tRNA synthetase-IN-3

    		Aminoacyl-tRNA Synthetase Infection
    Aminoacyl tRNA synthetase-IN-3 (compound 36K3) is an inhibitor of lysine tRNA synthetase (PfLysRS) from Plasmodium falciparum (IC50=59.2 nM), which inhibits the activity of PfLysRS by occupying the ATP binding site and L-lysine binding site of PfLysRS. Aminoacyl tRNA synthetase-IN-3 can be used in the development of antimalarial drugs .
    Aminoacyl tRNA synthetase-IN-3
  • HY-124742
    AR-HO47108

    		Na+/K+ ATPase Others
    AR-HO47108 is an orally active reversible Na+/K+ ATPase inhibitor. AR-HO47108 reversibly blocks the final step of gastric acid secretion by competitively binding to the potassium ion binding site of the Na+/K+ ATPase in the gastric wall cells. AR-HO47108 can be used for research on diseases related to excessive gastric acid secretion, such as peptic ulcers .
    AR-HO47108
  • HY-165569
    AU-1421

    		Potassium Channel Neurological Disease
    AU-1421 is a potassium ion (K⁺) site-directed regulator that specifically acts on various cation transport ATPases. AU-1421 can distinguish between two different K⁺-sensitive phosphorylation intermediate (E2P) states: for non-K⁺ transport type ATPases (such as the sarcoplasmic reticulum Ca²⁺-ATPase), after binding to AU-1421, it mimics the agonistic effect of K⁺, significantly accelerating the hydrolysis (dephosphorylation) of E2P. For K⁺ transport type ATPases (such as the gastric mucosa H⁺/K⁺-ATPase and the renal Na⁺/K⁺-ATPase), after binding to AU-1421, it inhibits the hydrolysis of E2P, stabilizing the phosphorylated intermediate, thereby blocking the ion transport cycle. AU-1421 can be used to study the mechanism of the potassium ion pump .
    AU-1421
  • HY-144381
    Glutamate-5-kinase-IN-1

    		Bacterial Infection
    Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 μM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents .
    Glutamate-5-kinase-IN-1
  • HY-176283
    Tubulin/LSD1-IN-1

    		Microtubule/Tubulin Histone Demethylase Apoptosis Wee1 Bcl-2 Family Caspase Cancer
    Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells .
    Tubulin/LSD1-IN-1
  • HY-102047A
    KDOAM-25 trihydrochloride

    		Histone Demethylase Cancer
    KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells .
    KDOAM-25 trihydrochloride
  • HY-163360
    PI3Kα-IN-19

    		PI3K Cancer
    PI3Kα-IN-19 (Compound 1) is a PI3Kα inhibitor with a targeted binding site at the p110α catalytic subunit. PI3Kα is one of the most common dysregulated kinases used in cancer research .
    PI3Kα-IN-19
  • HY-155975
    PI3Kδ-IN-14

    		PI3K Inflammation/Immunology
    PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC50: 0.8 nM, Kd: 84.8 nM). PI3Kδ-IN-14 binds to the ATP-binding site of the kinase domain of PI3Kδ. PI3Kδ-IN-14 has anti-inflammatory activity by inhibiting the PI3K/AKT pathway. PI3Kδ-IN-14 ameliorates acute lung injury (ALI) .
    PI3Kδ-IN-14
  • HY-160789
    C3001a

    		Potassium Channel Neurological Disease Inflammation/Immunology
    C3001a is a selective TREK-1 and TREK-2 channel activator with EC50 values of 12.81 μM and 11.31 μM, respectively. C3001a does not affect other two-pore domain K + (K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1. C3001a can be used for the study of pain and pancreatitis .
    C3001a
  • HY-174386
    STAT3-IN-43

    		STAT Cancer
    STAT3-IN-43 (Compound K2) is a covalent inhibitor targeting the allosteric site at the junction of the STAT3 coiled-coil domain and DNA-binding domain, with an IC50 of 40.7 μM. STAT3-IN-43 can be used in cancer research .
    STAT3-IN-43
  • HY-144382
    Glutamate-5-kinase-IN-2

    		Bacterial Infection
    Glutamate-5-kinase-IN-2 (compound 54) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.2 μM. Glutamate-5-kinase-IN-2 shows G5K inhibition by promotes conformational changes at the L-glutamate binding site. Glutamate-5-kinase-IN-2 has the potential for the research of anti-TB agents .
    Glutamate-5-kinase-IN-2
  • HY-178031
    HIV-1-IN-87

    		HIV Reverse Transcriptase Infection
    HIV-1-IN-87 (Compound 11x) is a dual-site HIV-1 inhibitor targeting the non-nucleoside reverse transcriptase inhibitor binding pocket (NNIBP) and its adjacent site (NNIAS). HIV-1-IN-87 has potent antiviral activities against wild-type and mutant strains (such as L100I, K103N and Y181C) (EC50: 4.1-150 nM). HIV-1-IN-87 can be used for HIV-1 infections like acquired immune deficiency syndrome (AIDS) research .
    HIV-1-IN-87
  • HY-114923
    SU-11752

    		DNA-PK PI3K Cancer
    SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC50 of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC50 of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy .
    SU-11752
  • HY-118061
    VCC234718

    		Bacterial Infection
    VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
    VCC234718
  • HY-N9362R
    Emodinanthrone (Standard)

    EmodAN (Standard)

    		 Reference Standards Antibiotic Ferroptosis Infection
    Pro-xylane (Standard) is the analytical standard of Pro-xylane. This product is intended for research and analytical applications. Emodinanthrone (EmodAn) is a MARCH7 stabilizer that inhibits ferroptosis (EC50=70 nM). Emodinanthrone is also a precursor to Emodin (HY-14393) and possesses antibiotic activity. Emodinanthrone directly binds to MARCH7 and blocks its ubiquitination-mediated degradation at the K608 site; this action enhances MARCH7-mediated K48 ubiquitination and degradation of NCOA4, as well as its regulation of the intracellular localization of TFR1 via K63 ubiquitination, thereby reducing the intracellular labile iron pool and blocking ferroptosis. Emodinanthrone demonstrates in vivo cardioprotective effects and exhibits a favorable safety profile. Emodinanthrone is applicable to research on ferroptosis-related cardiovascular diseases, including Doxorubicin (HY-15142A)-induced cardiomyopathy and myocardial ischemia-reperfusion injury .
    Emodinanthrone (Standard)
  • HY-161324
    Tubulin degrader 1

    		Microtubule/Tubulin Cancer
    Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
    Tubulin degrader 1
  • HY-170604
    MMP-2 Inhibitor-4

    		MMP Cardiovascular Disease Cancer
    MMP-2 Inhibitor-4 (Compound 5g) is an MMP-2 inhibitor with an IC50 of 152.62 nM. MMP-2 Inhibitor-4 can reduce the levels of MMP-2 in the K562 cell line through stable binding at the MMP-2 active site, and it demonstrates strong antiangiogenic effects in the ACHN cell line. MMP-2 Inhibitor-4 holds promise for research in chronic myeloid leukemia (CML) .
    MMP-2 Inhibitor-4
  • HY-161694
    DNMT1-IN-3

    		DNA Methyltransferase Cancer
    DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .
    DNMT1-IN-3
  • HY-P10393
    ERα17p

    ERα (295-311)

    		 Apoptosis Cancer
    ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
    ERα17p
  • HY-N2593R
    Isorhapontigenin (Standard)

    		Reference Standards Carnitine Palmitoyltransferase (CPT) Reactive Oxygen Species (ROS) Autophagy Apoptosis NF-κB PI3K Akt MMP Keap1-Nrf2 Inflammation/Immunology Cancer
    Isorhapontigenin (Standard) is the analytical standard of Isorhapontigenin (HY-N2593). This product is intended for research and analytical applications. Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes.
    Isorhapontigenin (Standard)
  • HY-183627
    066ATZ

    		PI5P4K Cancer
    066ATZ is a PIP4K2A/2B inhibitor with human PIP4K2A Ki 100 nM and PIP4K2B Ki 800 nM. 066ATZ binds to ATP-binding sites of PIP4K2A and PIP4K2B to block lipid kinase activity. 066ATZ can be used for the research of non-small cell lung cancer .
    066ATZ
  • HY-P11733
    (KFF)3K-acpP

    		Bacterial Infection
    (KFF)3K-acpP is an antibacterial agent conjugating of cell penetrating peptide (KFF)3K (HY-P10556) and acpP
    peptide nucleic acid. (KFF)3K-acpP binds to the translation start site region of acpP mRNA, sterically blocking ribosome binding and inhibiting translation of the acyl carrier protein. (KFF)3K-acpP induces bacterial envelope stress response pathways, and triggers depletion of outer membrane protein F (ompF) transcript. (KFF)3K-acpP can be used for the research of infections .
    (KFF)3K-acpP

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