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Results for "

mutation

" in MCE Product Catalog:

73

Inhibitors & Agonists

7

Screening Libraries

1

Dye Reagents

6

Peptides

5

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-114231B
    ELX-02 disulfate

    NB-124 disulfate

    Others Metabolic Disease
    ELX-02 disulfate (NB-124 disulfate) is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). ELX-02 disulfate is being developed as a therapy for genetic diseases caused by nonsense mutations.
  • HY-114231C
    ELX-02 sulfate

    NB-124 sulfate

    Others Metabolic Disease
    ELX-02 sulfate (NB-124 sulfate) is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). ELX-02 sulfate is being developed as a therapy for genetic diseases caused by nonsense mutations.
  • HY-134877
    BAY 2476568

    EGFR Cancer
    BAY 2476568 is a potent and selective EGFR inhibitor, with IC50s of < 0.2 nM for wild-type EGFR and several mutations (EGFRR ex20insSVD, EGFRR ex20insASV, EGFRR ex20insNPG).
  • HY-19713
    LJI308

    Ribosomal S6 Kinase (RSK) Cancer
    LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation.
  • HY-132166
    M4205

    c-Kit Cancer
    M4205 is a c-KIT inhibitor, with an IC50 of 10 nM for c-KIT V654A. M4205 has high activity on c-KIT mutations in exon 11, 13, 17.
  • HY-138697
    S65487

    VOB560

    Bcl-2 Family Apoptosis Cancer
    S65487 (VOB560) is a potent and selective Bcl-2 inhibitor. S65487 is also active on BCL-2 mutations, such as G101V and D103Y. S65487 has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 induces apoptosis and has anticaner activities.
  • HY-136531
    XMU-MP-3

    Btk Apoptosis Cancer
    XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis.
  • HY-138697A
    S65487 sulfate

    VOB560 sulfate

    Bcl-2 Family Apoptosis Cancer
    S65487 (VOB560) sulfate is a potent and selective Bcl-2 inhibitor. S65487 sulfate is also active on BCL-2 mutations, such as G101V and D103Y. S65487 sulfate has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 sulfate induces apoptosis and has anticaner activities.
  • HY-131328
    Pirtobrutinib

    LOXO-305

    Btk Cancer
    Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM.
  • HY-118341
    Clitocine

    Apoptosis Bcl-2 Family Cancer
    Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity.
  • HY-N8188
    Dehydrojuncusol

    HCV HCV Protease Infection
    Dehydrojuncusol, a potent HCV inhibitor, targets HCV NS5A and is able to inhibit RNA replication of replicons harboring resistance mutations to anti-NS5A direct-acting antivirals. Dehydrojuncusol significantly inhibits HCV infection when added after virus inoculation of HCV genotype 2a (EC50=1.35 µM).
  • HY-131328A
    (R)-Pirtobrutinib

    (R)-LOXO-305

    Others Others
    (R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib. Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations.
  • HY-136579
    ERK-IN-3

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

    ERK Cancer
    ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK. ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.
  • HY-112823
    Almonertinib

    HS-10296

    EGFR Cancer
    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
  • HY-112823B
    Almonertinib hydrochloride

    HS-10296 hydrochloride

    EGFR Cancer
    Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.
  • HY-50846
    SCH772984

    ERK Cancer
    SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
  • HY-N6615
    Aflatoxin B1

    Bacterial Endogenous Metabolite Cancer Infection
    Aflatoxin B1 (AFB1) is a Class 1A carcinogen, which is a secondary metabolite of Aspergillus flavus and A. parasiticus. Aflatoxin B1 (AFB1) mainly induces the transversion of G-->T in the third position of codon 249 of the p53 tumor suppressor gene, resulting in mutation.
  • HY-15811
    XMD8-87

    ACK1-B19

    Tyrosinase Cancer
    XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively.
  • HY-101243
    XMD16-5

    Tyrosinase Cancer
    XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.
  • HY-135887
    ZX-29

    ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • HY-137458
    Vevorisertib

    ARQ 751

    Akt Cancer
    Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations.
  • HY-128572
    FLT3-IN-6

    FLT3 Cancer
    FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD (FLT3 mutation) with an IC50 of 1.336 nM.
  • HY-112611
    H3B-5942

    Estrogen Receptor/ERR Cancer
    H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations.
  • HY-18634
    NSC319726

    ZMC1

    MDM-2/p53 Cancer
    NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.
  • HY-16662
    Oncrasin-1

    Ras Apoptosis Cancer
    Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.
  • HY-123159
    AKI603

    Aurora Kinase Cancer
    AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
  • HY-112299
    TAS6417

    CLN-081

    EGFR Apoptosis Cancer
    TAS6417 (CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM.
  • HY-N1996
    Chebulagic acid

    COX Lipoxygenase SARS-CoV Influenza Virus Infection Inflammation/Immunology
    Chebulagic acid is a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz, on angiogenesis. Chebulagic acid is a M2 serine to asparagine 31 mutation (S31N) inhibitor and influenza antiviral. Chebulagic acid also against SARS-CoV-2 viral replication with an EC50 of 9.76 μM.
  • HY-10410
    TG101209

    FLT3 JAK RET Autophagy Apoptosis Cancer
    TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
  • HY-139279
    TPX-0131

    ALK Cancer
    TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities.
  • HY-130149
    Adagrasib

    MRTX849

    Ras Cancer
    Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.
  • HY-109189
    Rezivertinib

    BPI-7711

    EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
  • HY-136789
    Tuxobertinib

    BDTX-189

    EGFR Cancer
    Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
  • HY-114491A
    Rineterkib hydrochloride

    Raf ERK Cancer
    Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer.
  • HY-114491
    Rineterkib

    Raf ERK Cancer
    Rineterkib (compound B) is an orally active RAF and ERK1/2 inhibitor in the study of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer.
  • HY-13898
    Taselisib

    GDC-0032; RG-7604

    PI3K Cancer
    Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
  • HY-131003A
    Taletrectinib free base

    DS-6051b free base; AB-106 free base

    ROS Cancer
    Taletrectinib (DS-6051b) free base is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
  • HY-131906
    JAK2-IN-7

    JAK FLT3 Cancer
    JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
  • HY-15338
    TG003

    CDK Cancer
    TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
  • HY-15338A
    (E/Z)-TG003

    CDK Cancer
    (E/Z)-TG003 is a racemic compound of (Z)-TG003 and (E)-TG003. (Z)-TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
  • HY-19314A
    Azvudine hydrochloride

    RO-0622 hydrochloride; FNC hydrochloride

    Reverse Transcriptase HIV HBV HCV Infection
    Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains.
  • HY-19314
    Azvudine

    RO-0622; FNC

    Reverse Transcriptase HIV HBV HCV Infection
    Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains.
  • HY-18674
    K-Ras-IN-1

    Ras Cancer
    K-Ras-IN-1 is a K-Ras inhibitor. K-Ras-IN-1 binds to K-Ras (WT), K-Ras (G12D), K-Ras (G12V), and H-Ras. K-Ras-IN-1 has potential for the research of pancreatic, colon and lung carcinomas.
  • HY-139039
    BSJ-4-116

    PROTACs CDK Cancer
    BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162).
  • HY-131003
    Taletrectinib

    DS-6051b; AB-106

    ROS Cancer
    Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
  • HY-123319A
    Antofloxacin

    Bacterial Infection
    Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species.
  • HY-123319
    Antofloxacin hydrochloride

    Bacterial Infection
    Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species.
  • HY-51424
    PLX-4720

    Raf Cancer
    PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
  • HY-N2533
    Cyanidin 3-sambubioside chloride

    Cyanidin-3-O-sambubioside chloride

    Influenza Virus Angiotensin-converting Enzyme (ACE) Cancer Infection Inflammation/Immunology
    Cyanidin 3-sambubioside chloride (Cyanidin-3-O-sambubioside chloride), a major anthocyanin, a natural colorant, and is a potent NO inhibitor. Cyanidin 3-sambubioside chloride is a H274Y mutation inhibitor, and inhibits influenza neuraminidase activity with an IC50 of 72 μM. Cyanidin 3-sambubioside chloride inhibits angiotensin-converting enzyme (ACE) activity and has antioxidant, anti-angiogenic and antiviral properties.
  • HY-120373
    MB710

    MDM-2/p53 Cancer
    MB710, an aminobenzothiazole derivative, is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds tightly to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1 μM. MB710 shows anticancer activity in p53-Y220C cell lines.
  • HY-104036
    IDH-305

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)).
  • HY-13001
    Quizartinib

    AC220

    FLT3 Ligand for Target Protein for PROTAC Apoptosis Autophagy Cancer
    Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
  • HY-135815
    Mobocertinib

    TAK-788; AP32788

    EGFR Cancer
    Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  • HY-10943
    GNF-7

    Bcr-Abl Ack1 Cancer
    GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-Abl WT and Bcr-Abl T315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.
  • HY-12215
    Lorlatinib

    PF-06463922

    ALK ROS Apoptosis Cancer
    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib has anticancer activity.
  • HY-135815A
    Mobocertinib succinate

    TAK-788 succinate; AP32788 succinate

    EGFR Cancer
    Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  • HY-13593
    Chlorambucil

    CB-1348; WR-139013

    DNA Alkylator/Crosslinker Cancer
    Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease.
  • HY-111373
    RapaLink-1

    mTOR Autophagy Cancer
    RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity.
  • HY-13247
    Setrobuvir

    ANA598

    DNA/RNA Synthesis HCV SARS-CoV Infection
    Setrobuvir (ANA598) is an orally active non-nucleosidic HCV NS5B polymerase inhibitor. ANA-598 inhibits both de novo RNA synthesis and primer extension, with IC50s between 4 and 5 nM. Setrobuvir also shows excellent binding affinity to SARS-CoV-2 RdRp and induces RdRp inhibition.
  • HY-123967
    RNF5 inhibitor inh-02

    Others Inflammation/Immunology
    RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research.
  • HY-132842
    Sunvozertinib

    EGFR Btk Cancer
    Sunvozertinib is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52).
  • HY-126323
    TCMDC-135051

    Parasite Infection
    TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC50=320 nM).
  • HY-126323B
    TCMDC-135051 hydrochloride

    Parasite Infection
    TCMDC-135051 hydrochloride is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 hydrochloride prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 hydrochloride has antiparasiticidal activity (EC50=320 nM).
  • HY-114277
    Sotorasib

    AMG-510

    Ras Cancer
    Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.
  • HY-126323A
    TCMDC-135051 TFA

    Parasite Infection
    TCMDC-135051 TFA is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 TFA prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 TFA has antiparasiticidal activity (EC50=320 nM).
  • HY-51424S
    PLX-4720-d7

    Raf Cancer
    PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of B-Raf V600E with an IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
  • HY-137497
    KRAS inhibitor-9

    Ras Apoptosis Cancer
    KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
  • HY-15814
    HG-7-85-01

    Bcr-Abl PDGFR c-Kit Src JAK Apoptosis Cancer
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.
  • 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.
  • HY-P2307
    Tat-NR2Baa

    iGluR NO Synthase Neurological Disease
    Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
  • HY-P2307A
    Tat-NR2Baa TFA

    iGluR NO Synthase Neurological Disease
    Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
  • HY-16909
    Leptomycin B

    CI 940; LMB

    CRM1 Fungal Antibiotic Cancer Infection
    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.