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Results for "

interactor

" in MCE Product Catalog:

124

Inhibitors & Agonists

2

Screening Libraries

1

Dye Reagents

20

Peptides

1

Inhibitory Antibodies

11

Natural
Products

2

Recombinant Proteins

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-133014
    RIP2 kinase inhibitor 1

    RIP kinase Inflammation/Immunology
    RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC50 of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders.
  • HY-124512
    Quercetin pentaacetate

    Pentaacetylquercetin

    RSV Infection Inflammation/Immunology
    Quercetin pentaacetate could interact with F-protein with lower binding energy and better stability to block viral adhesion. Quercetin pentaacetate interacts with RSV and inhibit the viral adhesion on cell surface.
  • HY-100798
    Phaclofen

    GABA Receptor Neurological Disease
    Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact.
  • HY-121546
    ALLO-1

    Autophagy Cancer
    ALLO-1, an autophagy receptor, is essential for autophagosome formation around paternal organelles and directly binds to the worm LC3 homologue LGG-1 through its LC3-interacting region (LIR) motif.
  • HY-18619
    YL-109

    Aryl Hydrocarbon Receptor Cancer
    YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness.
  • HY-100464
    tBID

    DYRK Cancer
    tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of  0.33 µM.
  • HY-B0628A
    Vinflunine Tartrate

    Microtubule/Tubulin Cancer
    Vinflunine Tartrat is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity.
  • HY-10996A
    KHS101 hydrochloride

    FGFR Neurological Disease Cancer
    KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).
  • HY-13856
    (R)-PS210

    PDK-1 Cancer
    (R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.
  • HY-N0460
    1-Caffeoylquinic acid

    NF-κB Cancer
    1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with Ki of 0.002 μM and binding energy of 1.50 Kcal/mol. 1-Caffeoylquinic acid has anti-oxidative stress ability. 1-Caffeoylquinic acid inhibits PD-1/PD-L1 interact.
  • HY-12841
    KHK-IN-1

    Others Metabolic Disease
    KHK-IN-1 is a potent ketohexokinase (KHK) inhibitor with IC50 of 12 nM; interacts with Asp-27B in the ATP-binding region of KHK.
  • HY-101809
    CNS-5161 hydrochloride

    CNS 5161A

    iGluR Cardiovascular Disease
    CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
  • HY-P2322
    Iturin A

    Fungal
    IturinA exhibits strong antifungal activity against pathogenic yeast and fungi. Iturin A interacts with the cytoplasmic membrane of the target cell forming ion conducting pores.
  • HY-12841A
    KHK-IN-1 hydrochloride

    Others Others
    KHK-IN-1 hydrochloride is a potent ketohexokinase (KHK) inhibitor with IC50 of 12 nM, interacts with Asp-27B in the ATP-binding region of KHK.
  • HY-112907
    RIP2 Kinase Inhibitor 3

    RIP kinase Inflammation/Immunology
    RIP2 Kinase Inhibitor 3 is a highly potent and selective inhibitor of receptor interacting protein-2 (RIP2) Kinase with an IC50 of 1 nM .
  • HY-18900
    Nec-4

    RIP kinase Inflammation/Immunology
    Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM.
  • HY-114349
    HS-1371

    RIP kinase Cancer Cardiovascular Disease
    HS-1371 is a potent and ATP-competitive receptor-interacting protein kinase 3 (RIP3) inhibitor with an IC50 of 20.8 nM.
  • HY-10984
    Pomalidomide

    CC-4047

    Ligands for E3 Ligase Molecular Glues Apoptosis Cancer
    Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
  • HY-124632
    WJ460

    Others Cancer
    WJ460 is a potent myoferlin (MYOF) inhibitor, which interacts directly with MYOF and exerts anti-metastatic activity in the nanomolar range in breast cancer cells.
  • HY-121793
    Roemerine

    (-)-Roemerine

    P-glycoprotein Cancer
    Roemerine, an aporphine alkaloid, isolated from the leaves of Annona senegalensis, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells.
  • HY-108511A
    PB28

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
  • HY-108511
    PB28 dihydrochloride

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity.
  • HY-B1041
    Aminoguanidine hydrochloride

    Pimagedine hydrochloride; GER-11; Aminoguanidinium chloride

    NO Synthase Endocrinology
    Aminoguanidine hydrochloride is a diamine oxidase and NO synthase inhibitor, reduces levels of advanced glycation end products (AGEs) through interacting with 3-deoxyglucosone, is an investigational drug for the treatment of diabetic nephropathy.
  • HY-114371
    Eclitasertib

    DNL-758; SAR-443122

    RIP kinase Inflammation/Immunology
    Eclitasertib (DNL-758) is a potent receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 of <1 µΜ (From patent WO2017136727A2, example 42).
  • HY-128592
    TAB29

    Others Cancer
    TAB29 is a potent inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) with an IC50 of 874 nM, possesses therapeutic potential for human cancers.
  • HY-122234
    VPC-18005

    Others Cancer
    VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity.
  • HY-128585
    GNE684

    RIP kinase Cancer Inflammation/Immunology
    GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Ki app values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively.
  • HY-32219
    T863

    Acyltransferase Metabolic Disease
    T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.
  • HY-W041994
    GMBS

    Others Cancer
    GMBS is a heterobifunctional cross-linker. GMBS can be used in chemical cross-linking of proteins coupled with mass spectrometry (CXMS) to study protein folding and to map the interfaces between interacting proteins.
  • HY-19761
    RIP2 kinase inhibitor 2

    RIP kinase Cancer
    RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.
  • HY-120142
    EC359

    Apoptosis Cancer
    EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions.
  • HY-114492
    GSK547

    GSK'547

    RIP kinase Cancer
    GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
  • HY-P1868
    α2β1 Integrin Ligand Peptide

    Integrin Infection
    α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
  • HY-P1868A
    α2β1 Integrin Ligand Peptide TFA

    Integrin Others
    α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
  • HY-12837
    EN460

    Others Others
    EN460 is a selective endoplasmic reticulum oxidation 1 (ERO1) inhibitor. EN460 (IC50 of 1.9 μM) interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation.
  • HY-101622
    5-HT6/7 antagonist 1

    5-HT Receptor Dopamine Receptor
    5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.
  • HY-101032
    RIPA-56

    RIP kinase Inflammation/Immunology
    RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM. RIPA-56 can be used for the treatment of systemic inflammatory response syndrome.
  • HY-125466
    cRIPGBM

    RIP kinase Apoptosis Cancer
    cRIPGBM, a proapoptotic derivative of RIPGBM, a cell type-selective inducer of apoptosis in GBM cancer stem cells (CSCs) by binding to receptor-interacting protein kinase 2 (RIPK2), with an EC50 of 68 nM in GBM-1 cells.
  • HY-N9347
    Stepharine

    Toll-like Receptor (TLR) Inflammation/Immunology Cardiovascular Disease
    Stepharine, an natural alkaloid, directly interactes with TLR4 and binds to the TLR4/MD2 complex (TLR4 inhibitor). Stepharine possesses anti-aging, anti-viral and anti-hypertensive effects.
  • HY-N6718
    Filipin III

    Fungal Inflammation/Immunology
    Filipin III is the major component of Filipin, a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure.
  • HY-W011417
    Cinnabarinic acid

    mGluR Apoptosis Others
    Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.
  • HY-130841
    Apcin-A

    APC Ligands for Target Protein for PROTAC Cancer
    Apcin-A, an Apcin derivative, is an anaphase-promoting complex (APC) inhibitor. Apcin-A interacts strongly with Cdc20, and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V (HY-130257).
  • HY-10542A
    (Z)-GW 5074

    Raf Neurological Disease
    (Z)-GW 5074 is a compound which interacts with both mHTT (mutant huntingtin protein) and LC3, but not but not with the wild-type HTT protein. (Z)-GW 5074 inhibits c-Raf, shows no effect on autophagy, and is effective for neurodegenerative disorder.
  • HY-P0122
    iRGD peptide

    c(CRGDKGPDC)

    Integrin Cancer
    iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
  • HY-114492A
    (Rac)-GSK547

    RIP kinase Cancer
    (Rac)-GSK547 is the racemate of GSK547. GSK547 is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
  • HY-101508
    GNA002

    Histone Methyltransferase Cancer
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
  • HY-P1191
    JIP-1(153-163)

    T1-JIP

    JNK Others
    JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).
  • HY-P3061
    [Hyp3]-Bradykinin

    Bradykinin Receptor Endocrinology Cardiovascular Disease
    [Hyp3]-Bradykinin, naturally occurring peptide hormone, is a bradykinin receptor agonist. [Hyp3]-Bradykinin interacts with B2-bradykinin receptors and stimulates inositol phosphate production in cultured human fibroblasts.
  • HY-19764
    GSK2983559 active metabolite

    RIP kinase Cancer
    GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
  • HY-15369
    FPA-124

    Akt Apoptosis Cancer
    FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis.
  • HY-104021
    GSK840

    GSK'840

    RIP kinase Inflammation/Immunology
    GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.
  • HY-112038A
    GSK2983559

    RIP kinase Inflammation/Immunology
    GSK2983559 (compound 3) is a potent, specific and oral active receptor interacting protein 2 (RIP2) kinase inhibitor, which has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
  • HY-125402
    GSK-843

    GSK'843

    RIP kinase Inflammation/Immunology
    GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM.
  • HY-P1191A
    JIP-1(153-163) TFA

    T1-JIP TFA

    JNK Others
    JIP-1(153-163) TFA (TI-JIP TFA) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).
  • HY-D0226
    Quinizarin

    1,4-Dihydroxyanthraquinone

    DNA/RNA Synthesis Fungal Cancer Infection
    Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth.
  • HY-108022
    Azemiglitazone

    MSDC-0602

    Mitochondrial Metabolism Metabolic Disease
    Azemiglitazone (MSDC-0602), a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and has the potential for type 2 diabetes study with reducing risk of PPARγ-mediated side effects.
  • HY-118773
    MreB Perturbing Compound A22 hydrochloride

    A22 hydrochloride

    Bacterial Inflammation/Immunology
    MreB Perturbing Compound A22 hydrochloride is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly. MreB Perturbing Compound A22 hydrochloride blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC=3.1 µg/ml).
  • HY-108474
    Nolatrexed dihydrochloride

    AG 337; Thymitaq

    Thymidylate Synthase Cancer
    Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity.
  • HY-101332
    EGLU

    (2S)-α-Ethylglutamic acid; (2S)-α-EGLU

    mGluR Neurological Disease
    EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) is a potent and competitive mGluR-2 receptor antagonist. EGLU interacts with (lS,3S)-ACPD-sensitive site with a Kd value of 66 μM. EGLU is an antidepressant agent.
  • HY-112038
    GSK2983559 free acid

    RIP kinase Inflammation/Immunology
    GSK2983559 free acid (compound 3) is a potent, specific and oral active receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
  • HY-115688
    TXNIP-IN-1

    Others Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    TXNIP-IN-1 is TXNIP-TRX (thioredoxin-interacting protein- thioredoxin) complex inhibitor extracted from patent US20200085800A1, Compound 1. TXNIP-IN-1 can be used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease.
  • HY-101359
    TPMPA

    GABA Receptor Neurological Disease
    TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells.
  • HY-117113
    JI051

    Notch Cancer
    JI051 is a stabilizer for the Hes1-PHB2 interaction. JI051 interacts with a cancer-associated protein chaperone prohibitin 2 (PHB2), induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1. Anti-cancer activity.
  • HY-18901
    RIPK1-IN-4

    RIP kinase Inflammation/Immunology
    RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase.
  • HY-107597
    SU3327

    JNK Metabolic Disease Inflammation/Immunology
    SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.
  • HY-103661
    BI-6C9

    Mitochondrial Metabolism Apoptosis Neurological Disease
    BI-6C9 is a highly specific BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from mitochondrial apoptosis inducing factor (AIF) release and caspase-independent cell death in neurons.
  • HY-101084
    NSC 228155

    EGFR Histone Acetyltransferase Epigenetic Reader Domain Cancer
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
  • HY-N6715
    Tenuazonic acid

    Influenza Virus Bacterial Infection
    Tenuazonic acid, belonging to tetramic acids that are the largest family of natural products, is a putative nonhost-selective mycotoxin isolated from Alternaria alternate. Tenuazonic acid blocks electron transport beyond primary quinone acceptor (QA) by interacting with D1 protein and it is a broad-spectrum and effective photosystem II (PSII) inhibitor.
  • HY-112273A
    CD532 hydrochloride

    Aurora Kinase Cancer
    CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer.
  • HY-100573
    Necrosulfonamide

    Mixed Lineage Kinase Cancer
    Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis.
  • HY-P1565
    Transdermal Peptide Disulfide

    TD 1 Disulfide(peptide)

    Na+/K+ ATPase Inflammation/Immunology
    Transdermal Peptide Disulfide (TD 1 Disulfide(peptide)) is a 11-amino acid peptide, binds toNa +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide can enhance the transdermal delivery of many macromolecules.
  • HY-116999
    IR415

    HBV Infection
    IR415 is a potent anti-HBV agent and inhibits HBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease. HBx: hepatitis B virus X protein.
  • HY-135909
    TH1217

    ZINC1775962367

    SARS-CoV Cancer Infection
    TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19.
  • HY-112273
    CD532

    Aurora Kinase Cancer
    CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer.
  • HY-N2355
    Solasurine

    Others Others
    Solasurine is a steroidal alkaloid that can be isolated from Solanum surrattence. Solasurine can interact with the C3-like protease (SARS-CoV-2 main protease) amino acids Phe8, Pro9, Ile152, Tyr154, Pro293, Phe294, Val297, and Arg298.
  • HY-120118
    Metarrestin

    ML246

    DNA/RNA Synthesis Cancer
    Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models.
  • HY-128348
    PK68

    RIP kinase Cancer Inflammation/Immunology
    PK68 is a potent and selective 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 with great potential for use in the treatment of inflammatory disorders and cancer metastasis.
  • HY-124418
    SBI-477

    Others Metabolic Disease
    SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
  • HY-111226
    GSK5182

    Estrogen Receptor/ERR Reactive Oxygen Species Cancer Cardiovascular Disease
    GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC).
  • HY-N8160
    Dehydrocurdione

    Keap1-Nrf2 Reactive Oxygen Species Inflammation/Immunology
    Dehydrocurdione, a zedoary-derived sesquiterpene, induces heme oxygenase (HO)-1, an antioxidative enzyme, in RAW 264.7 macrophages. Dehydrocurdione interacts with Keap1, resulting in Nrf2 translocation followed by activation of the HO-1 E2 enhancer. Dehydrocurdione suppresses lipopolysaccharide-induced NO release, a marker of inflammation. Anti-inflammatory activity.
  • HY-P1565A
    Transdermal Peptide Disulfide TFA

    TD 1 Disulfide(peptide) TFA

    Na+/K+ ATPase Others
    Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA) is a 11-amino acid peptide, binds to Na +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide TFA can enhance the transdermal delivery of many macromolecules.
  • HY-N6716
    Filipin complex

    Fungal Antibiotic Others
    Filipin, produced as a mixture of related compounds known as the filipin complex (filipins I-IV) in nature, is a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure. Filipin III is the major component of Filipin.
  • HY-111422
    PLX51107

    Epigenetic Reader Domain Cancer
    PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
  • HY-116501
    VPC-14449

    Androgen Receptor Cancer
    VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer.
  • HY-128780B
    SPR206 acetate

    Bacterial Antibiotic Infection
    SPR206 acetate is a polymyxin analog with antibiotic activity against Gram-negative pathogens, including multidrug-resistant (MDR) variants. SPR206 acetate has an anti-bacterial infection effect by interacting with the bacterium’s outer membrane. The MIC values of SPR206 acetate against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L.
  • HY-15847
    HS38

    DAPK Cardiovascular Disease
    HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders.
  • HY-100131
    GSK481

    RIP kinase Inflammation/Immunology
    GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser 166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM.
  • HY-P9806
    Anti-MERS-D12 mAb

    MERS-D12; MERS Antibody-D12

    SARS-CoV Infection
    Anti-MERS-D12 mAb (MERS-D12; MERS Antibody-D12) is a human monoclonal IgG1. Anti-MERS-D12 mAb binds directly to the DPP4 interacting region of the MERS-CoV Spike receptor binding domain (RBD) and effect neutralization by directly blocking receptor binding.
  • HY-129056
    Melagatran

    Thrombin Cardiovascular Disease
    Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion.
  • HY-108468
    KL001

    Others Metabolic Disease
    KL001 is a first-in-class cryptochrome (CRY, a flavoproteins that are sensitive to blue light, and is involved in the circadian rhythms of plants and animals) stabilizer which specifically interacts with CRY1 and CRY2. KL001 prevents ubiquitin-dependent degradation of CRY, resulting in lengthening of the circadian period. KL001 has the potential to control fasting hormone-induced gluconeogenesis.
  • HY-P1629
    Temporin A

    Bacterial Fungal Antibiotic Infection
    Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans).
  • HY-114641A
    BIIL-260 hydrochloride

    Leukotriene Receptor Inflammation/Immunology
    BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM.
  • HY-132174
    CHIKV-IN-2

    Dihydroorotate Dehydrogenase Infection
    CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools.
  • HY-101451
    PBIT

    Histone Demethylase Cancer
    PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively.
  • HY-106840
    L-365260

    Cholecystokinin Receptor Metabolic Disease Neurological Disease
    L-365260 is a potent and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance.
  • HY-34758
    N-Nitroso-N-methylurea

    NMU; MNU; NMH

    DNA Alkylator/Crosslinker Cancer
    N-Nitroso-N-methylurea (NMU;MNU;NMH) is a potent carcinogen, mutagen and teratogenand. N-Nitroso-N-methylurea is a direct-acting alkylating agent that interacts with DNA. N-Nitroso-N-methylurea targets multiple animal organs to cause various cancer and/or degenerative disease. N-Nitroso-N-methylurea is also a precursor in the synthesis of diazomethane.
  • HY-108474S
    Nolatrexed-d4 dihydrochloride

    Thymidylate Synthase Cancer
    Nolatrexed-d4 dihydrochloride (AG 337-d4) is the deuterium labeled Nolatrexed dihydrochloride. Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity.
  • HY-128342
    Complement C5-IN-1

    Complement System Inflammation/Immunology
    Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM.
  • HY-12646A
    Rhosin

    Ras Apoptosis Cancer
    Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
  • HY-12646
    Rhosin hydrochloride

    Ras Apoptosis Cancer
    Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
  • HY-N2513
    β-Boswellic acid

    Lipoxygenase DNA/RNA Synthesis Cancer
    β-Boswellic acid is isolated from the gum resin of Boswellia serrate. β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation. β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells.
  • HY-130259
    LC3-mHTT-IN-AN2

    ATTECs Autophagy Neurological Disease
    LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
  • HY-135218
    AV-153

    DNA/RNA Synthesis Cancer
    AV-153, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 has anti-cancer activity.
  • HY-W011500
    TCEP hydrochloride

    Tris(2-​carboxyethyl)​phosphine hydrochloride

    Others Others
    TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry.
  • HY-105066
    Davunetide

    Microtubule/Tubulin Amyloid-β Neurological Disease
    Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity.
  • HY-P2260
    Tat-beclin 1

    Autophagy HIV Infection
    Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
  • HY-130258
    LC3-mHTT-IN-AN1

    ATTECs Autophagy Neurological Disease
    LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
  • HY-P2260A
    Tat-beclin 1 TFA

    Autophagy HIV Infection
    Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
  • HY-123611
    Supinoxin

    RX-5902

    DNA/RNA Synthesis Apoptosis Cancer
    Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM.
  • HY-126214
    JH-RE-06

    DNA/RNA Synthesis Cancer
    JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy.
  • HY-124745
    KY-05009

    MAP4K Wnt Apoptosis Cancer
    KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
  • HY-128341
    ERK5-IN-2

    ERK Cancer Cardiovascular Disease
    ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
  • HY-101903A
    BMS-309403 sodium

    FABP Metabolic Disease Cardiovascular Disease
    BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
  • HY-101903
    BMS-309403

    FABP Metabolic Disease Cardiovascular Disease
    BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
  • HY-135218A
    AV-153 free base

    DNA/RNA Synthesis Cancer
    AV-153 free base, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 free base intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 free base interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 free base has anti-cancer activity.
  • HY-103444
    ARP-100

    MMP Cancer
    ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1' pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM).
  • HY-122862
    RAS inhibitor Abd-7

    Ras Cancer
    RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V.
  • HY-110208
    BRD9876

    Kinesin Microtubule/Tubulin Cancer
    BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research.
  • HY-135906
    CK2/ERK8-IN-1

    Casein Kinase ERK Pim DYRK Apoptosis Cancer
    CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.
  • HY-116716
    PIN1 inhibitor API-1

    MicroRNA Cancer
    PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.
  • HY-117937
    BC-1215

    Ligands for E3 Ligase Inflammation/Immunology
    BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCF Fbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC.
  • HY-136265
    BC-LI-0186

    Aminoacyl-tRNA Synthetase Cancer
    BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research.
  • HY-134813A
    MRTX1133 formic

    Ras Cancer
    MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic has picomolar binding affinity, single digit nanomolar activity in cellular assays, and marked in vivo efficacy in tumor models harboring KRAS G12D mutations.
  • HY-134813
    MRTX1133

    Ras Cancer
    MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations.