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specific inhibition

" in MedChemExpress (MCE) Product Catalog:

119

Inhibitors & Agonists

1

Screening Libraries

2

Biochemical Assay Reagents

12

Peptides

5

Inhibitory Antibodies

11

Natural
Products

1

Isotope-Labeled Compounds

3

Click Chemistry

5

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0822
    Shikonin
    Maximum Cited Publications
    66 Publications Verification

    C.I. 75535; Isoarnebin 4

    		 Exosomes Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV AIM2 Cancer
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .
    Shikonin
  • HY-P9915
    Daratumumab
    10+ Cited Publications

    Anti-Human CD38, Human Antibody; HuMax-CD38; JNJ-54767414

    		 CD38 ADC Antibody Inflammation/Immunology Cancer
    Daratumumab (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab has anti-multiple myeloma (MM) effect. Daratumumab impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
    Daratumumab
  • HY-N1584
    Halofuginone
    15+ Cited Publications

    RU-19110

    		 DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Infection Cardiovascular Disease Inflammation/Immunology Cancer
    Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
    Halofuginone
  • HY-114258
    LY3295668
    3 Publications Verification

    AK-01

    		 Aurora Kinase Apoptosis Cancer
    LY3295668 (AK-01) is a highly specific and orally active inhibitor of Aurora-A kinase with a Ki values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 avoids the formation of polyploids related to AurB inhibition. LY3295668 can be used for the study of small cell lung cancer .
    LY3295668
  • HY-100421
    CPI-455
    10+ Cited Publications

    		 Histone Demethylase Cancer
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
    CPI-455
  • HY-153321
    Bexobrutideg
    1 Publications Verification

    NX-5948; BTK-IN-24

    		 PROTACs Btk Inflammation/Immunology Cancer
    Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
    Bexobrutideg
  • HY-15802
    WZ4003
    5+ Cited Publications

    		 AMPK Cancer
    WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1 (ARK5)/NUAK2, without significant inhibition on other 139 kinases.
    WZ4003
  • HY-50937
    ST 2825
    Maximum Cited Publications
    70 Publications Verification

    		 MyD88 Inflammation/Immunology
    ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity .
    ST 2825
  • HY-129388B
    Pulrodemstat benzenesulfonate
    4 Publications Verification

    CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate

    		 Histone Demethylase Inflammation/Immunology Cancer
    Pulrodemstat (CC-90011) benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat benzenesulfonate is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
    Pulrodemstat benzenesulfonate
  • HY-159607
    PRT3789

    		PROTACs SWI/SNF Complex Cancer
    PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer .
    PRT3789
  • HY-155338
    SWTX-143

    		YAP Cancer
    SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity .
    SWTX-143
  • HY-P9915A
    Daratumumab (Anti-CD38)
    10+ Cited Publications

    Anti-Human CD38, Human Antibody (PBS)

    		 ADC Antibody CD38 Cancer
    Daratumumab (PBS) (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab (PBS) has anti-multiple myeloma (MM) effect. Daratumumab (PBS) impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
    Daratumumab (Anti-CD38)
  • HY-116788
    Lipofermata
    5+ Cited Publications

    		 Bacterial Infection
    Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM .
    Lipofermata
  • HY-126675A
    AS2863619
    5+ Cited Publications

    		 CDK STAT Inflammation/Immunology
    AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene .
    AS2863619
  • HY-16712
    LDN-214117
    2 Publications Verification

    		 TGF-β Receptor Cancer
    LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
    LDN-214117
  • HY-N1584A
    Halofuginone hydrobromide
    15+ Cited Publications

    RU-19110 hydrobromide

    		 DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Infection Cardiovascular Disease Inflammation/Immunology Cancer
    Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
    Halofuginone hydrobromide
  • HY-113763
    L524-0366

    		TNF Receptor Others
    L524-0366 is a specific, dose-dependent TWEAK-Fn14 inhibitor. L524-0366 specifically binds to the Fn14 surface with a KD of 7.12 μM, competitively inhibiting the binding of Fn14 to TWEAK (inhibition rate reaching 16%). L524-0366 inhibits TWEAK-induced glioma cell migration without potential cytotoxic effects .
    L524-0366
  • HY-137817
    BCH001

    		DNA/RNA Synthesis Metabolic Disease
    BCH001, a quinoline derivative, is a specific PAPD5 inhibitor. BCH001 restores telomerase activity and telomere length in dyskeratosis congenita (DC) induced pluripotent stem cells. BCH001 shows no inhibition of poly(A)-specific ribonuclease (PARN) or several other canonical and non-canonical polynucleotide polymerases. BCH001 is used to regulate aging .
    BCH001
  • HY-15320
    NBI-74330
    5+ Cited Publications

    		 CXCR Inflammation/Immunology Endocrinology
    NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of ( 125I)CXCL10 and ( 125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
    NBI-74330
  • HY-100421A
    CPI-455 hydrochloride
    10+ Cited Publications

    		 Histone Demethylase Cancer
    CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
    CPI-455 hydrochloride
  • HY-120072
    PF-3450074
    5 Publications Verification

    PF-74

    		 HIV Infection
    PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle . CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
    PF-3450074
  • HY-108350
    MI-2-2
    1 Publications Verification

    		 Epigenetic Reader Domain Cancer
    MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation .
    MI-2-2
  • HY-15838
    ID-8
    5 Publications Verification

    		 DYRK Cancer
    ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs .
    ID-8
  • HY-133118
    6RK73
    4 Publications Verification

    		 Deubiquitinase Cancer
    6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer .
    6RK73
  • HY-128348
    PK68

    		RIP kinase Inflammation/Immunology Cancer
    PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis .
    PK68
  • HY-15798
    UNC2881

    		VSV TAM Receptor Cardiovascular Disease
    UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC50s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research .
    UNC2881
  • HY-N4104
    Agaric acid
    1 Publications Verification

    Agaricinic Acid

    		 Mitochondrial Metabolism Bacterial Calcium Channel Infection Metabolic Disease
    Agaric acid (Agaricinic Acid) is an orally active inhibitor of adenine nucleotide translocase found in specific fungi. Agaric acid can inhibit the biofilm formation of various bacteria such as Salmonella. Agaric acid can also induce mitochondrial permeability transition, prompting mitochondria to release Ca 2+, disrupting the transmembrane potential, and causing mitochondrial swelling. In addition, Agaric acid can also inhibit citrate transport in liver mitochondria and participate in the inhibition of fatty acid synthesis, affecting multiple metabolic processes .
    Agaric acid
  • HY-P5979
    LRRKtide

    		LRRK2 Neurological Disease
    LRRKtide is a polypeptide substrate. LRRKtide is a specific phosphorylation substrate of LRRK2, a kinase associated with Parkinson's disease, and its phosphorylation site is a threonine residue. LRRKtide can be used for characterization of the catalytic properties of LRRK2, as well as studies on kinase activity and inhibition. LRRKtide is applicable to research related to Parkinson's disease .
    LRRKtide
  • HY-105056
    Bretazenil

    Ro 16-6028

    		 GABA Receptor Neurological Disease
    Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
    Bretazenil
  • HY-P99914
    Emfizatamab

    GNC-038

    		 PD-1/PD-L1 CD19 TNF Receptor CD3 Interleukin Related IFNAR Inflammation/Immunology Cancer
    Emfizatamab (GNC-038) is a monoclonal antibody against CD19/CD3E/TNFRSF9/PD-L1. Emfizatamab exhibits antitumor activity, being capable of activating CD3 and 4-1BB signals on T cells, as well as targeting the high expression of CD19 or PD-L1 on tumor cells. Emfizatamab functions as a CD19-specific T cell engager by mediating direct antitumor activity. Emfizatamab can also overcome the inhibition of T cells by PD-L1. Emfizatamab can be used in the research of tumors such as R/R non-Hodgkin lymphoma or acute lymphoblastic leukemia .
    Emfizatamab
  • HY-126675
    AS2863619 free base
    5+ Cited Publications

    		 CDK STAT Inflammation/Immunology
    AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene .
    AS2863619 free base
  • HY-139659
    ARD-61

    		PROTACs Androgen Receptor Progesterone Receptor Apoptosis Cancer
    ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ARD-61
  • HY-P99925
    Enoticumab

    REGN421

    		 Notch Metabolic Disease Cancer
    Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
    Enoticumab
  • HY-114672
    MBCQ

    		Phosphodiesterase (PDE) Cardiovascular Disease
    MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE .
    MBCQ
  • HY-115570
    GW406108X
    1 Publications Verification

    GW108X

    		 Kinesin ULK Autophagy Cancer
    GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK .
    GW406108X
  • HY-145721A
    Mongersen sodium

    GED-0301 sodium

    		 TGF-beta/Smad Inflammation/Immunology
    Mongersen sodium is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen sodium restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen sodium can attenuate Crohn's disease-like experimental colitis in mice .
    Mongersen sodium
  • HY-145721
    Mongersen

    GED-0301

    		 TGF-beta/Smad Inflammation/Immunology
    Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice .
    Mongersen
  • HY-P2862
    Enolase, S.cerevisiae

    		Biochemical Assay Reagents Others
    Enolase is a glycolytic enzyme present in the cell wall of S. cerevisiae. Enolase exhibits specific affinity to imported tRNA and can facilitate formation of preMsk1p-tRNA complex. Enolase can be overproduced in tumor cells where rate of glycolysis is increased. Enolase depletion can lead to tRNA inhibition in vivo .
    Enolase, S.cerevisiae
  • HY-P1597
    Malantide
    1 Publications Verification

    		 PKA PKC Cancer
    Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a Km of 16 μM .
    Malantide
  • HY-129388A
    Pulrodemstat
    4 Publications Verification

    CC-90011; LSD1-IN-7

    		 Histone Demethylase Inflammation/Immunology Cancer
    Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
    Pulrodemstat
  • HY-W653977
    Chlortetracycline-13C,d3 hydrochloride

    7-Chlorotetracycline-13C,d3 hydrochloride

    		 Isotope-Labeled Compounds Antibiotic Bacterial Parasite Infection
    Chlortetracycline-13C,d3 hydrochloride (7-Chlorotetracycline-13C,d3 hydrochloride) is the 13C- and deuterium labeled Chlortetracycline hydrochloride (HY-B1327). Chlortetracycline hydrochloride is an orally active, selective antibiotic, that inhibits methanogenic bacteria through inhibition of bacterial protein synthesis. Chlortetracycline hydrochloride is a specific and potent calcium ionophore antibiotic, that inhibits binding of aminoacyl-tRNA to ribosomes .
    Chlortetracycline-13C,d3 hydrochloride
  • HY-N1584C
    Halofuginone lactate
    15+ Cited Publications

    RU-19110 lactate

    		 DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Infection Cardiovascular Disease Inflammation/Immunology Cancer
    Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
    Halofuginone lactate
  • HY-13714
    Nolatrexed

    AG 337 free base

    		 Antifolate Others
    Nolatrexed (AG 337 free base) is a compound with antifolate activity, high oral bioavailability, and major toxicity at inhibitory doses is gastrointestinal reactions. It can be safely taken orally at specific doses for inhibition, with effects on platelets and neutrophils.
    Nolatrexed
  • HY-108645
    AL 8697

    		p38 MAPK Autophagy Inflammation/Immunology
    AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity .
    AL 8697
  • HY-N0822R
    Shikonin (Standard)

    C.I. 75535 (Standard); Isoarnebin 4 (Standard)

    		 Reference Standards Exosomes Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV AIM2 Cancer
    Shikonin (Standard) is the analytical standard of Shikonin. This product is intended for research and analytical applications. Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .
    Shikonin (Standard)
  • HY-112289
    IDH889

    		Isocitrate Dehydrogenase (IDH) Cancer
    IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
    IDH889
  • HY-N1584R
    Halofuginone (Standard)

    RU-19110 (Standard)

    		 Reference Standards DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel Infection Cardiovascular Disease Inflammation/Immunology Cancer
    Halofuginone (Standard) is the analytical standard of Halofuginone. This product is intended for research and analytical applications. Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
    Halofuginone (Standard)
  • HY-P5881
    PKCα (C2-4) inhibitor peptide

    		PKC Cardiovascular Disease
    PKCα (C2-4) inhibitor peptide is a PKCα specific inhibitor peptide that blocks the inhibition of IKr by the α1A adrenoreceptor agonist A-61603 (HY-101366) .
    PKCα (C2-4) inhibitor peptide
  • HY-P11331
    Az-NC-002

    		Proteasome Others
    Az-NC-002 is a Proteasome trypsin-like site (β2) and immunoproteasome β2i-specific active probe. Az-NC-002 has weak off-target effects with no significant inhibition for Cathepsin D (HY-P2750), but this inhibition reacts outside of the active site or influence on a small fraction of the enzyme .
    Az-NC-002
  • HY-123129
    RS 2232

    		5-HT Receptor Monoamine Oxidase Neurological Disease
    RS 2232 is an orally active, competitive 5-HT deamination inhibitor with a Ki of 0.054 μM. RS-2232 exhibits reversible and specific inhibition of type A monoamine oxidase. RS 2232 can be used in brain research .
    RS 2232

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