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94

Inhibitors & Agonists

2

Fluorescent Dye

6

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3

Inhibitory Antibodies

1

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1

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1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13459
    PF-5274857

    		Smo Cancer
    PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
    PF-5274857
  • HY-130243
    RORγt Inverse agonist 6

    		ROR Inflammation/Immunology
    RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo .
    RORγt Inverse agonist 6
  • HY-13459A
    PF-5274857 hydrochloride

    		Smo Cancer
    PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway .
    PF-5274857 hydrochloride
  • HY-149880
    c-Met-IN-18

    		c-Met/HGFR Cancer
    c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    c-Met-IN-18
  • HY-145843
    c-Myc inhibitor 5

    		c-Myc Cancer
    c-Myc inhibitor 5 (DA3) is a fluorescent, long chain-bridged bispurine that selectively targets the c-MYC G-quadruplex (KD of 16 μM). c-Myc inhibitor 5 shows inhibition on c-MYC expression rather than other G4-driven oncogenes .
    c-Myc inhibitor 5
  • HY-121802
    Dynarrestin
    1 Publications Verification

    		 Hedgehog Cancer
    Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-dependent processes in cells without affecting ATP hydrolysis and interfering with ciliogenesis. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells .
    Dynarrestin
  • HY-154313
    Spiclomazine

    Clospirazine

    		 Ras Cancer
    Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .
    Spiclomazine
  • HY-D1459
    BODIPY 665/676

    		Fluorescent Dye Metabolic Disease
    BODIPY 665/676 is a lipophilic radical-sensitive fluorescent probe that can be used to study radical-driven lipid autoxidation .
    BODIPY 665/676
  • HY-116785
    BRD32048

    		DNA/RNA Synthesis Cancer
    BRD32048 is a direct binder of ETV1 with a KD of 17.1 μM. BRD32048 modulates both ETV1-mediated transcriptional activity and invasion of ETV1-driven cancer cells. BRD32048 inhibits ETV1 acetylation and promotes its degradation. BRD32048 acts as a top candidate ETV1 perturbagen .
    BRD32048
  • HY-100849
    JAK 3i

    		JAK Inflammation/Immunology
    JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM). JAK3i forms a covalent bond with a cysteine in JAK3, but not the closely related kinase domains in JAK1, JAK2, or TYK2. JAK3i abolishes IL-2-driven T-cell proliferation in vivo and has the potential for  autoimmune disease research .
    JAK 3i
  • HY-112929
    DT-061
    5+ Cited Publications

    		 Phosphatase Cancer
    DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis .
    DT-061
  • HY-141896
    RET-IN-7

    		RET Cancer
    RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
    RET-IN-7
  • HY-124267
    Zgwatinib

    SOMG-833

    		 c-Met/HGFR Cancer
    Zgwatinib (SOMG-833) is a potent, selective, and ATP-competitive c-MET inhibitor, with an IC50 of 0.93 nM against c-MET, over 10,000-fold more potent compared with 19 tyrosine kinases (including c-MET family members and highly homologous kinases). Zgwatinib potently inhibits c-MET-driven cell proliferation. Zgwatinib as a potential candidate agent for c-MET-driven human cancers research .
    Zgwatinib
  • HY-115866
    COX-2-IN-6

    		COX Cancer
    COX-2-IN-6 (compound 10) is an orally active, gut-restricted and selective cyclooxygenase-2 (COX-2) inhibitor for colorectal Chemoprevention of cancer. COX-2-IN-6 selectively targets COX-2 with an IC50 of 0.84 μM and a Ki of 69 nM. COX-2-IN-6 also inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM .
    COX-2-IN-6
  • HY-134978A
    (+)SHIN2

    		SHMT Cancer
    (+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, whose target can be traced with 13C-serine. (+)SHIN2 increases survival in NOTCH1-driven mouse primary acute lymphoblastic leukemia (T-ALL) in vivo with a synergistic effect with Methotrexate (HY-14519) . (+)SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (+)SHIN2
  • HY-108417
    Debio 0617B

    		STAT JAK Bcr-Abl Cancer
    Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors .
    Debio 0617B
  • HY-125102
    AZ12253801

    		IGF-1R Cancer
    AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
    AZ12253801
  • HY-151335
    KU-177

    		HSP Cancer
    KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research .
    KU-177
  • HY-N9362
    Emodinanthrone

    		Antibiotic Infection
    Emodinanthrone, an anthraquinone, is a sprecursor of Emodin (HY-14393) with antibiotic activity. Emodinanthrone inhibits respiration-driven solute transport at micromolar concentrations in membrane vesicles of Escherichia coli .
    Emodinanthrone
  • HY-122878
    HS-131

    		HSP Cancer
    HS-131, a near infrared dye tethered Hsp90 inhibitor, is able to detect oncogene-driven breast cancers, including multiple different molecular subtypes of human breast cancers .
    HS-131
  • HY-P3277
    KRpep-2d

    		Ras Cancer
    KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .
    KRpep-2d
  • HY-P3277A
    KRpep-2d TFA

    		Ras Cancer
    KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .
    KRpep-2d TFA
  • HY-151881
    SOS1-IN-15

    		Ras Cancer
    SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer .
    SOS1-IN-15
  • HY-107730
    NPY5RA-972

    		Neuropeptide Y Receptor Neurological Disease
    NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor .
    NPY5RA-972
  • HY-19350
    BML-210
    1 Publications Verification

    		 HDAC Apoptosis Cancer
    BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice .
    BML-210
  • HY-157083
    mCMY020

    		YAP Cancer
    mCMY020 is a covalent inhibitor of TEAD. mCMY020 effectively reduces YAP (Yes-associated protein)-driven transcription and selectively slows the proliferation of Hippo-deficient cancer cells. mCMY020 can be used in cancer research .
    mCMY020
  • HY-131968
    BMS-986202

    		JAK Cytochrome P450 Inflammation/Immunology
    BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium .
    BMS-986202
  • HY-19706
    ARS-853
    2 Publications Verification

    		 Ras Apoptosis Cancer
    ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .
    ARS-853
  • HY-124674A
    CCT365623 hydrochloride

    		Monoamine Oxidase EGFR Akt TGF-beta/Smad Cancer
    CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties .
    CCT365623 hydrochloride
  • HY-136270
    Gartisertib
    2 Publications Verification

    VX-803; M4344; ATR inhibitor 2

    		 ATM/ATR Cancer
    Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
    Gartisertib
  • HY-P2471
    Neurogranin (48-76), mouse

    		Calmodulin Neurological Disease
    Neurogranin (48-76), mouse is a peptide corresponding to residues 48-76 of Neurogranin. Neurogranin, a calmodulin-binding protein, is exclusively expressed in the post-synapse, and mediates NMDAR driven synaptic plasticity by regulating the calcium-calmodulin (Ca 2+-CaM) pathway .
    Neurogranin (48-76), mouse
  • HY-136579
    ASN007

    ERK-IN-3

    		 ERK Cancer
    ASN007 (ERK-IN-3) is a potent and orally active inhibitor of ERK. ASN007 inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 can be used for the research of cancers driven by RAS mutations .
    ASN007
  • HY-136579A
    ASN007 benzenesulfonate

    ERK-IN-3 benzenesulfonate

    		 ERK Cancer
    ASN007 (ERK-IN-3) benzenesulfonate is a potent and orally active inhibitor of ERK. ASN007 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 benzenesulfonate can be used for the research of cancers driven by RAS mutations .
    ASN007 benzenesulfonate
  • HY-139361
    Sulfopin
    1 Publications Verification

    PIN1-3

    		 PIN1 Cancer
    Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors .
    Sulfopin
  • HY-13323
    CX-5461
    Maximum Cited Publications
    30 Publications Verification

    		 DNA/RNA Synthesis Cancer
    CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
    CX-5461
  • HY-P99217
    Rilotumumab

    AMG 102

    		 c-Met/HGFR Cancer
    Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
    Rilotumumab
  • HY-W423595
    BEBT-109

    		EGFR Cancer
    BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .
    BEBT-109
  • HY-14460
    AM679

    		FLAP Inflammation/Immunology
    AM679 is a potent, selective 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 2 nM in a human FLAP membrane binding assay. AM679 markedly reduces the respiratory syncytial virus-driven ocular pathology as well as the synthesis of cysteinyl leukotrienes (CysLTs) in the eye .
    AM679
  • HY-P99450
    Avdoralimab

    IPH 5401; Anti-C5aR1 mAb

    		 Complement System Inflammation/Immunology Cancer
    Avdoralimab (IPH 5401) is a fully human IgGκ monoclonal antibody that targets the complement C5a receptor 1 (C5aR1) that prevents its binding to C5a. Avdoralimab can be used for complement-driven inflammatory diseases and solid tumours research .
    Avdoralimab
  • HY-163299
    pan-KRAS-IN-5

    		Ras Apoptosis Cancer
    pan-KRAS-IN-5 (compound 15a) is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 induces cell cycle arrest and promptes apoptosis in KRAS-driven cancer cells .
    pan-KRAS-IN-5
  • HY-106228
    HLF1-11

    		Fungal Bacterial Glutathione Peroxidase Infection
    HLF1-11, a human lactoferrin-derived peptide, is a broad spectrum antimicrobial agent. HLF1-11 inhibits human MPO activity. HLF1-11 also directs GM-CSF-driven monocyte differentiation toward macrophages, and enhances immune responses .
    HLF1-11
  • HY-123952
    RTC-5

    TRC-382

    		 EGFR Cancer
    RTC-5 (TRC-382) is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling .
    RTC-5
  • HY-128777
    WEHI-9625
    1 Publications Verification

    		 VDAC Apoptosis Cancer
    WEHI-9625 is a tricyclic sulfone, first-in-class inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. WEHI-9625 is completely inactive against both human BAK and the closely related apoptosis effector BAX .
    WEHI-9625
  • HY-145010
    SN-011
    2 Publications Verification

    		 STING Inflammation/Immunology
    SN-011 is a potent and selective mouse and human STING inhibitor, with an IC50 of 76 nM for STING signaling. SN-011 competes with cyclic dinucleotide (CDN) for the binding pocket of the STING dimer, blocking CDN binding and STING activation. SN-011 can be used for the research of STING-driven autoimmune and inflammatory disease .
    SN-011
  • HY-144110
    HCV-IN-37

    		HCV Infection
    HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage .
    HCV-IN-37
  • HY-122866
    ZT-12-037-01

    		Ras Cancer
    ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM .
    ZT-12-037-01
  • HY-108440
    Shz-1

    		Others Cardiovascular Disease
    Shz-1, a small cardiogenic molecule, induces various cardiac-specific genes including sarcomeric tropomyosin in P19CL6 cells. Shz-1 induces Nkx2.5 expression in mouse. Shz-1 activates the axolotl TPM4 promoter-driven ectopic expression in C2C12 cells .
    Shz-1
  • HY-144131
    RET-IN-11

    		Apoptosis RET Cancer
    RET-IN-11 is a potent and selective RET inhibitor with IC50s of 6.20 nM, 18.68 nM for RET and RET V804M, respectively. RET-IN-11 shows anti-proliferation and migration activity in CCDC6-RET-driven LC-2/ad cells. RET-IN-11 induces cell apoptosis .
    RET-IN-11
  • HY-147007
    β-catenin-IN-3

    		β-catenin Wnt Cancer
    β-catenin-IN-3 (compound C2) is a potent and selective β-catenin inhibitor with a KD value of 54.96 nM. β-catenin-IN-3 acts by targeting a cryptic allosteric modulation site of β-catenin. β-catenin-IN-3 can significantly reduce viability of β-catenin-driven cancer cells .
    β-catenin-IN-3
  • HY-155537
    YK-029A

    		EGFR Cancer
    YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFR T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models .
    YK-029A

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