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Results for "Allosteric Inhibitors" in MCE Product Catalog:

119

Inhibitors & Agonists

1

Screening Libraries

4

Peptides

5

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-115466
    MLT-748

    MALT1 Inflammation/Immunology
    MLT-748 is a potent, selective and allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM.
  • HY-124587
    MLT-747

    MALT1 Inflammation/Immunology
    MLT-747 is a potent, selective, allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 14 nM.
  • HY-100524
    LRE1

    Adenylate Cyclase Cancer
    LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase.
  • HY-101796
    NSC-70220

    Others Cancer
    NSC-70220 is a selective and allosteric SOS1 inhibitor. NSC-70220 inhibits allosteric site activation, and partially inhibited catalytic site activation. NSC-70220 has an anticancer effect.
  • HY-12683
    BPTES

    Glutaminase Cancer
    BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
  • HY-103269
    BAI1

    Bcl-2 Family Apoptosis Cancer
    BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
  • HY-18296
    AKT-IN-1

    Akt Cancer
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
  • HY-116009
    RMC-4550

    Phosphatase Cancer
    RMC-4550 is a potent, selective and allosteric inhibitor of SHP2, with an IC50 of 0.583 nM.
  • HY-15857
    CW-069

    Kinesin Cancer
    CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC50 of 75 μM.
  • HY-13449
    TAK-733

    MEK Cancer
    TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
  • HY-17537
    APY29

    IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-18928
    FAK inhibitor 5

    FAK Cancer
    FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
  • HY-100519
    NVS-PAK1-1

    PAK Cancer
    NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
  • HY-14846A
    Litronesib Racemate

    LY2523355 Racemate

    Kinesin Others
    Litronesib Racemate (LY2523355 Racemate) is the racemate of litronesib. Litronesib is a selective, allosteric inhibitor of kinesin Eg5.
  • HY-112094
    WNK-IN-11

    Others Others
    WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC50 of 4 nM for WNK1.
  • HY-111446
    EPAC 5376753

    Others Cancer Metabolic Disease Cardiovascular Disease
    EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells.
  • HY-18601
    (±)-BI-D

    HIV HIV Integrase Infection
    (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
  • HY-15599
    SSR128129E

    SSR

    FGFR Cancer
    SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-15713
    NMS-873

    p97 Cancer
    NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with an IC50 value of 30 nM.
  • HY-15252
    Reparixin L-lysine salt

    Repertaxin L-lysine salt

    CXCR Cancer Inflammation/Immunology Endocrinology
    Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
  • HY-114397
    SHP394

    Phosphatase Cancer
    SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC50 of 23 nM.
  • HY-114169
    WRG-28

    Discoidin Domain Receptor Cancer
    WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.
  • HY-101068
    TOFA

    RMI14514; MDL14514

    Acetyl-CoA Carboxylase Cancer
    TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
  • HY-15599A
    SSR128129E free acid

    SSR free acid

    FGFR Cancer
    SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-12408
    6H05

    Ras Cancer
    6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • HY-12682
    Glutaminase C-IN-1

    Compound 968

    Glutaminase Cancer
    Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
  • HY-112128
    USP7-IN-3

    Deubiquitinase Cancer
    USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor.
  • HY-12408A
    6H05 (TFA)

    Ras Cancer
    6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • HY-111184
    PIK-108

    PI3K Cancer
    PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.
  • HY-15251
    Reparixin

    Repertaxin; DF 1681Y

    CXCR Inflammation/Immunology Endocrinology Cancer
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
  • HY-122913
    Borussertib

    Akt Cancer
    Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt wt.
  • HY-12042
    Pimasertib

    AS703026; MSC1936369B

    MEK Cancer
    Pimasertib (AS703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2, used for cancer treatment.
  • HY-19715
    SGC707

    Histone Methyltransferase Cancer
    SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM.
  • HY-17601
    Alofanib

    RPT835

    FGFR Apoptosis Cancer Cardiovascular Disease
    Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity.
  • HY-16062
    ARQ 621

    Kinesin Cancer
    ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.
  • HY-104010
    Asciminib

    ABL001

    Bcr-Abl Cancer
    Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
  • HY-18652
    Ro 5126766

    CH5126766

    MEK Raf Cancer
    Ro 5126766 (CH5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
  • HY-108708
    GeA-69

    PARP Cancer
    GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM.
  • HY-100018
    BAY1125976

    Akt Cancer
    BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
  • HY-136311
    NCT-504

    Others Neurological Disease
    NCT-504 is a selective allosteric inhibitor of PIP4Kγ, with an IC50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease.
  • HY-18286
    NCGC00229600

    TSH Receptor Endocrinology
    NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
  • HY-15198
    KG5

    Raf PDGFR FLT3 c-Kit Cancer
    KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
  • HY-115502
    BCI

    (E)-BCI

    Phosphatase Cancer Inflammation/Immunology
    BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.
  • HY-114368A
    Kira8 Hydrochloride

    AMG-18 Hydrochloride

    IRE1 Inflammation/Immunology
    Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • HY-114368
    Kira8

    AMG-18

    IRE1 Inflammation/Immunology
    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • HY-15301
    CC0651

    E1/E2/E3 Enzyme Cancer
    CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27 Kip1, as confirmed by dose-response analysis.
  • HY-137067
    IMT1B

    LDC203974

    Others Cancer
    IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.
  • HY-50862
    Akt1 and Akt2-IN-1

    Akt Cancer
    Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.
  • HY-114304
    COH000

    E1/E2/E3 Enzyme Cancer
    COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
  • HY-119377
    UPGL00004

    Glutaminase Cancer
    UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
  • HY-115502A
    BCI hydrochloride

    (E)-BCI hydrochloride

    Phosphatase Cancer Inflammation/Immunology
    BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.
  • HY-124646
    KIRA-7

    IRE1 Inflammation/Immunology
    KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect.
  • HY-10219
    Rapamycin

    Sirolimus; AY-22989

    mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Cancer
    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-10299
    GSK-923295

    Kinesin Apoptosis Cancer
    GSK-923295 is a special, allosteric inhibitor of centromere-associated protein-E (CENP-E) kinesin motor ATPase activity, with Ki of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.
  • HY-112942A
    CMP-Sialic acid sodium salt

    CMP-Neu5Ac sodium salt

    Others Metabolic Disease
    CMP-Sialic acid sodium salt (CMP-Neu5Ac sodium salt) is an allosteric inhibitor of UDP-GlcNAc 2-epimerase, the enzyme that initiates sialic acid synthesis. CMP-Sialic acid sodium salt provides a substrate for Golgi sialyltransferases.
  • HY-14691
    Refametinib

    BAY 869766; RDEA119

    MEK Cancer
    Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
  • HY-10355
    AKT inhibitor VIII

    AKTi-1/2

    Akt Apoptosis Cancer Metabolic Disease
    AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.
  • HY-12429
    Beclabuvir

    BMS-791325

    HCV Infection
    Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM. 
  • HY-16743
    Ibiglustat

    Venglustat; SAR402671; GZ402671

    Others Metabolic Disease
    Ibiglustat (Venglustat), a potential therapy for PD Parkinson’s disease, SRT in Fabry’s and Gaucher’s, is a selective, allosteric inhibitor of glucosylceramide synthase (GCS) with ability to cross the blood-brain barrier.
  • HY-103575A
    MFZ 10-7 hydrochloride

    mGluR Neurological Disease
    MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5. MFZ 10-7 hydrochloride inhibits cocaine-taking and cocaine-seeking behavior in rats.
  • HY-117571
    BPN14770

    Phosphodiesterase (PDE) Neurological Disease
    BPN14770 is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.
  • HY-119751
    Hematein

    Casein Kinase Akt Wnt Apoptosis Cancer
    Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.
  • HY-70074
    CCG-63802

    RGS Protein Cancer Inflammation/Immunology
    CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM.
  • HY-136173
    TNO155

    Phosphatase Cancer
    TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
  • HY-10519
    BMS-345541

    IKK Cancer
    BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
  • HY-16743A
    Ibiglustat (L-Malic acid)

    Venglustat (L-Malic acid); SAR402671 (L-Malic acid); GZ402671 (L-Malic acid)

    Others Metabolic Disease
    Ibiglustat L-Malic acid (Venglustat L-Malic acid), a potential therapy for PD Parkinson’s disease, SRT in Fabry’s and Gaucher’s, is a selective, allosteric inhibitor of glucosylceramide synthase (GCS) with ability to cross the blood-brain barrier.
  • HY-10518
    BMS-345541 hydrochloride

    IKK Cancer
    BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
  • HY-10358
    MK-2206 dihydrochloride

    MK-2206 (2HCl)

    Akt Autophagy Apoptosis Cancer
    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy.
  • HY-119339
    SX-682

    CXCR Cancer Inflammation/Immunology Endocrinology
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
  • HY-18370
    HIF-2α-IN-3

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent.
  • HY-10219S
    Rapamycin-d3

    Sirolimus-d3; AY-22989-d3

    mTOR FKBP Autophagy Cancer
    Rapamycin-d3 (Sirolimus-d3) is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-13965
    Parmodulin 2

    ML161

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
  • HY-15756
    PTP1B-IN-4

    Phosphatase Metabolic Disease
    PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes.
  • HY-114334
    Glutaminase-IN-1

    CB839 derivative

    Glutaminase Cancer
    Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
  • HY-127111
    NDI-091143

    ATP Citrate Lyase Cancer
    NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate.
  • HY-131902
    MLT-231

    MALT1 Cancer
    MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.
  • HY-136128
    H3B-120

    Potassium Channel Cancer
    H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity.
  • HY-103320A
    Calhex 231 hydrochloride

    CaSR Metabolic Disease
    Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca 2+-induced accumulation of [ 3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment.
  • HY-119374
    BRM/BRG1 ATP Inhibitor-1

    Others Cancer
    BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM[1] .
  • HY-10046
    Plerixafor

    AMD 3100; JM3100; SID791

    CXCR HIV Virus Protease Cancer Infection Endocrinology Inflammation/Immunology
    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
  • HY-133512
    NCGC00249987

    Phosphatase Cancer
    NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC50s of 3 μM and 6.9 μM for Eya2 ED and MBP-Eya2 FL. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells.
  • HY-115452
    G5-7

    JAK Apoptosis Cancer
    G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
  • HY-12062
    PD318088

    MEK Cancer
    PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research.
  • HY-135805A
    (Rac)-JBJ-04-125-02

    EGFR Cancer
    (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M.
  • HY-123872
    MSC1094308

    p97 Others
    MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively.
  • HY-P1259
    PR-39

    Proteasome Bacterial Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-P1259A
    PR-39 TFA

    Proteasome Bacterial Inflammation/Immunology
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-122559
    BMS-984923

    mGluR Neurological Disease
    BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling.
  • HY-B0520A
    Benztropine mesylate

    Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate

    Dopamine Receptor mAChR Histamine Receptor Cancer Neurological Disease
    Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
  • HY-P1045
    187-1, N-WASP inhibitor

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-P1045A
    187-1, N-WASP inhibitor TFA

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-124634
    PZ-2891

    Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
  • HY-10118
    Filibuvir

    HCV DNA/RNA Synthesis Infection
    Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively. Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation.
  • HY-N0240
    Herbacetin

    Others Cancer
    Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects. Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis.
  • HY-117282
    JG-98

    HSP Apoptosis Cancer
    JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.
  • HY-100213
    EAI045

    EGFR Cancer
    EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
  • HY-124308
    PS315

    PKC Cancer
    PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity.
  • HY-137092
    IACS-13909

    Phosphatase Cancer
    IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.
  • HY-136789
    BDTX-189

    EGFR Cancer
    BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
  • HY-117287
    BMS-986165

    JAK Interleukin Related IFNAR Inflammation/Immunology
    BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. BMS-986165 inhibits IL-12/23 and type I IFN pathways.
  • HY-122630
    TH-257

    LIM Kinase (LIMK) Cancer
    TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM.
  • HY-130608
    Mutated EGFR-IN-3

    EGFR Cancer
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
  • HY-108232
    MK-2206

    Akt Autophagy Apoptosis Cancer
    MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities.
  • HY-A0009
    Galanthamine hydrobromide

    Galantamine hydrobromide

    AChE nAChR Neurological Disease
    Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
  • HY-131043
    NVS-PAK1-C

    PAK Cancer
    NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50 values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC50=270 nM) and phosphorylated PAK2 (IC50=720 nM).
  • HY-19719A
    Miransertib hydrochloride

    ARQ-092 hydrochloride

    Akt Parasite Cancer Infection
    Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib hydrochloride is effective against Leishmania.
  • HY-19719
    Miransertib

    ARQ-092

    Akt Parasite Cancer Infection
    Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib is effective against Leishmania.
  • HY-120327
    KY-226

    Phosphatase Metabolic Disease Neurological Disease
    KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
  • HY-12755
    ML141

    CID-2950007

    Ras Apoptosis Cancer
    ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines.
  • HY-135805
    JBJ-04-125-02

    EGFR Cancer
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
  • HY-125269
    TED-347

    YAP Cancer
    TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.
  • HY-103565
    AMN082

    mGluR Neurological Disease
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-103693
    NAZ2329

    Phosphatase Cancer
    NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
  • HY-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase MicroRNA Infection Inflammation/Immunology Neurological Disease
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
  • HY-12545
    Brevetoxin-3

    PbTx-3

    Sodium Channel Inflammation/Immunology
    Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
  • 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.