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Results for "

covalently

" in MCE Product Catalog:

201

Inhibitors & Agonists

3

Screening Libraries

4

Dye Reagents

1

Peptides

14

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-132196
    BTK inhibitor 18

    Btk Inflammation/Immunology
    BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities.
  • HY-136605
    DGY-06-116

    Src Cancer
    DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC50 of 8340 nM.
  • HY-U00279
    Nitracrine

    DNA/RNA Synthesis Cancer
    Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor drug. Nitracrine has cytotoxicity towards most cells.
  • HY-100338
    CNX-500

    Btk Cancer
    CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.
  • HY-132234
    M-1211

    Epigenetic Reader Domain Cancer
    M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
  • HY-117430
    Hymeglusin

    F-244; 1233A; L-659699

    Antibiotic Cancer Infection Metabolic Disease
    Hymeglusin, as a fungal β-lactone antibiotic, is a HMG-CoA synthase inhibitor (IC50 = 0.12 μM). Hymeglusin covalently modifies the active Cys 129 residue of the enzyme.
  • HY-134761
    EN4

    c-Myc Cancer
    EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.
  • HY-100003
    ML-210

    Glutathione Peroxidase Ferroptosis Cancer
    ML-210 is a selective and covalent glutathione peroxidase 4 (GPX4) inhibitor with an EC50 of 30 nM. ML-210 binds the GPX4 selenocysteine residue. ML-210 has anti-cancer activity.
  • HY-12903
    Macozinone

    PBTZ169

    Bacterial Infection
    Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect.
  • HY-14645
    (-)-DHMEQ

    Dehydroxymethylepoxyquinomicin

    NF-κB Cancer Inflammation/Immunology
    (-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity.
  • HY-131704
    FGFR4-IN-5

    FGFR Cancer
    FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research.
  • 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-19706
    ARS-853

    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.
  • HY-114436
    MRTX-1257

    Ras Cancer
    MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
  • HY-13563
    Batabulin

    T138067

    Microtubule/Tubulin Apoptosis Cancer
    Batabulin (T138067) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death.
  • HY-13563A
    Batabulin sodium

    T138067 sodium

    Microtubule/Tubulin Apoptosis Cancer
    Batabulin sodium (T138067 sodium) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin sodium affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death.
  • HY-139504
    CC-99677

    MAPKAPK2 (MK2) Inflammation/Immunology
    CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). CC-99677 is extracted from patent WO2020236636, compound 1.
  • HY-100433
    PACMA 31

    Others Cancer
    PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues.
  • HY-120129
    Ancremonam

    BOS-228; LYS-228

    Bacterial Infection
    Ancremonam (LYS-228) is a low toxicity, potent and single-agent monobactam antibiotic targeting penicillin binding protein 3 with potent activity against Enterobacteriaceae. Ancremonam kills bacteria by inhibiting cell wall synthesis through covalent modification of the active-site serine of penicillin binding protein 3.
  • 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-131014
    FM-479

    JAK Inflammation/Immunology
    FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases. FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
  • HY-13821
    Epoxomicin

    BU-4061T

    Proteasome Apoptosis Cancer Inflammation/Immunology
    Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
  • 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-124704
    Chst15-IN-1

    Others Neurological Disease
    Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair.
  • HY-129610
    KB02-SLF

    PROTACs FKBP Cancer
    KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.
  • HY-129917
    KB02-JQ1

    PROTACs Epigenetic Reader Domain Cancer
    KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.
  • HY-123587
    PR-924

    Proteasome Apoptosis Cancer
    PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities.
  • HY-108568
    15-Deoxy-Δ-12,14-prostaglandin J2

    15d-PGJ2; 15-Deoxy-Δ12,14-PGJ2

    PPAR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-136351
    THZ-P1-2

    Autophagy Cancer
    THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
  • HY-101257B
    YKL-5-124 TFA

    CDK Cancer
    YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-101257
    YKL-5-124

    CDK Cancer
    YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-N6825
    Hydroxy-α-sanshool

    TRP Channel Endogenous Metabolite Neurological Disease
    Hydroxy-​α-​sanshool is an alkylamide isolated from pepper, acts as a TRPA1 covalent and TRPV1 non-covalent agonist, with EC50s of 69 and 1.1 µM, respectively.
  • HY-119935
    JAK3 covalent inhibitor-1

    JAK Inflammation/Immunology
    JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs.
  • HY-139878
    MLKL-IN-1

    Mixed Lineage Kinase Inflammation/Immunology
    MLKL-IN-1 is a covalent MLKL inhibitor with a KD of 50 μM.
  • HY-10544
    Tegobuvir

    GS 333126; GS-9190

    HCV Infection
    Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
  • HY-10836
    Cruzain-IN-1

    Others Others
    Cruzain-IN-1 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.
  • HY-18081
    PF 750

    FAAH Autophagy Metabolic Disease
    PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile.
  • HY-112906
    C-176

    STING Inflammation/Immunology
    C-176 is a strong and covalent mouse STING inhibitor.
  • HY-132879
    TAK-020

    Btk Inflammation/Immunology
    TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
  • HY-100944
    Conduritol B epoxide

    Glucosidase Neurological Disease
    Conduritol B epoxide is an irreversible covalently bound acid β-glucosidase (GCase) inhibitor.
  • HY-108691
    PF-06465469

    Itk Cancer
    PF-06465469 is a covalent inhibitor of ITK with an IC50 of 2 nM.
  • HY-139881
    BTK inhibitor 19

    Btk Cancer
    BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
  • HY-12457
    Rachelmycin

    CC-1065; NSC 298223

    Antibiotic Cancer Infection
    Rachelmycin (CC-1065; NSC 298223) is a potent naturally antibiotic isolated from Streptomyces zelensis. Rachelmycin binds non-covalently and covalently (N-3 adenine adduct) in the minor groove of B-form DNA. Rachelmycin has exceptionally potent antitumor activity.
  • HY-139865
    142I5

    Apoptosis Cancer
    142I5 is a potent ML-IAP Lys-covalent inhibitor with an IC50 value of 11 nM.
  • HY-52101A
    FMK

    Ribosomal S6 Kinase (RSK) Cancer
    FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
  • HY-18930
    NU6300

    CDK Cancer
    NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
  • HY-111512
    PF-06795071

    MAGL Inflammation/Immunology Neurological Disease
    PF-06795071 is a potent and selective covalent MAGL inhibitor with an IC50 of 3 nM.
  • HY-139715
    IMD-ferulic

    NF-κB Cancer
    IMD-ferulic is a covalently linked NF-κB modulator that improves the adjuvanticity of small molecule immune potentiators.
  • HY-128925
    AMAS

    ADC Linkers Cancer
    AMAS is a nonclaevable heterobifunctional crosslinker with NHS ester and maleimide groups that allows covalent conjugation of amine- and sulfhydryl-containing molecules.
  • HY-126256
    PRMT5-IN-1

    Histone Methyltransferase Cancer
    PRMT5 IN-1, a hemiaminal, is a covalent protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
  • HY-101790
    ZM223

    NEDD8-activating Enzyme Cancer
    ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active.
  • HY-18012
    Spebrutinib

    AVL-292; CC-292

    Btk Cancer
    Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC50 of 0.5 nM.
  • HY-W053709
    Tetrazine-Amine

    (4-(1,2,4,5-tetrazin-3-yl)phenyl)methanamine; Tetrazine-NH2

    Others Cancer
    Tetrazine-Amine is a tetrazine linker that can be used to covalently label live cells through a cycloaddition.
  • HY-19564
    JX06

    PDHK Apoptosis Cancer
    JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity.
  • HY-100739
    RA190

    Proteasome Cancer
    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
  • HY-117203A
    CDK12-IN-E9

    CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
  • HY-112166
    Rilzabrutinib

    PRN1008

    Btk Cancer Metabolic Disease
    Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
  • HY-18605
    K-Ras G12C-IN-2

    Ras Cancer
    K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
  • HY-16596
    CNX-1351

    PI3K Cancer
    CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
  • HY-107985
    FT671

    Deubiquitinase Cancer
    FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.
  • HY-136848
    SM1-71

    MAP3K Src FGFR Ribosomal S6 Kinase (RSK) LIM Kinase (LIMK) Cancer
    SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.
  • HY-10243
    Vaniprevir

    MK-7009

    HCV HCV Protease Infection
    Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.
  • 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-103618
    THZ531

    CDK Cancer
    THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.
  • HY-101790A
    ZM223 hydrochloride

    NEDD8-activating Enzyme Cancer
    ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.
  • HY-133738
    M-808

    Epigenetic Reader Domain Cancer
    M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC50 value of 2.6 nM.
  • HY-125826
    Heptasaccharide Glc4Xyl3

    Metabolic Disease
    Heptasaccharide Glc4Xyl3, a covalent inhibitor of endo-xyloglucanases, is used for the identification and analysis of diverse xyloglucan-active enzymes in nature.
  • HY-138065
    Iodoacetyl-LC-biotin

    Apoptosis Others
    Iodoacetyl-LC-biotin is a biotinylated electrophile probe that can be used to investigate the scope and characteristics of protein covalent binding to subcellular proteomes.
  • HY-132197
    CBP/p300-IN-12

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.
  • HY-128889
    FXIa-IN-1

    Factor Xa Cardiovascular Disease
    FXIa-IN-1 (compound EP-7041) is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.
  • HY-139612
    JDQ-443

    NVP-JDQ443

    Ras Cancer
    JDQ-443 (example 1a) is a covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1).
  • HY-133740
    MS117

    Histone Methyltransferase Cancer
    MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM.
  • HY-136259
    ML188

    SARS-CoV Virus Protease Infection
    ML188, a first in class probe, is a selective non-covalent SARS-CoV 3CLpro inhibitor with an IC50 of 1.5 μM. Antiviral activity.
  • HY-122577
    EN40

    Aldehyde Dehydrogenase (ALDH) Cancer
    EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC50 value of 2 uM
  • HY-139603
    MYF-01-37

    YAP Cancer
    MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction.
  • HY-112161
    Branebrutinib

    BMS-986195

    Btk Cancer
    Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC50 of 0.1 nM.
  • HY-116856
    SRPKIN-1

    SRPK Cancer Cardiovascular Disease
    SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC50s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect.
  • HY-118653
    SAR629

    Others Metabolic Disease
    SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation.
  • HY-W018161
    Hexadecanedioic acid

    Endogenous Metabolite Others
    Hexadecanedioic acid is covalently linked to Sepharose 4B, shows better performance in terms of specificity than dye-based resins and could be used for depletion of SA from plasma samples.
  • HY-U00447
    PK11000

    MDM-2/p53 DNA Alkylator/Crosslinker Cancer
    PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 by covalent cysteine modification, without compromising DNA binding.
  • HY-128771
    K-Ras G12C-IN-4

    Ras Cancer
    K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRAS G12C.
  • HY-43521
    Ibrutinib-MPEA

    Others Cancer
    Ibrutinib-MPEA (Compound 20) is ibrutinib derivative. Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) that has been used to treat haematological malignancies.
  • HY-N9460
    Sibiromycin

    DNA Alkylator/Crosslinker Antibiotic Cancer
    Sibiromycin is a naturally produced glycosylated pyrrolobenzodiazepines (PBDs). Sibiromycin is also a potent antitumor antibiotic that binds covalently to DNA in the minor groove at the NH2 of guanine.
  • HY-102087
    JPM-OEt

    Cathepsin Cancer
    JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.
  • HY-128661
    IDH1 Inhibitor 2

    Isocitrate Dehydrogenase (IDH) Metabolic Disease
    IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.
  • HY-129655
    Sulfo-SMPB sodium

    ADC Linkers Cancer
    Sulfo-SMPB sodium is a non-cleavable, heterobifunctional chemical cross-linking reagent which contains N-hydroxysuccinimide (NHS) ester and maleimide groups, allowing covalent conjugation of amine- and sulfhydryl-containing molecules.
  • HY-100002
    ML162

    Glutathione Peroxidase Ferroptosis Cancer
    ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines
  • HY-13943
    CNX-774

    Btk Cancer
    CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC50 of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification.
  • HY-114277A
    Sotorasib racemate

    AMG-510 racemate

    Ras Cancer
    Sotorasib (AMG-510) racemate is the racemate of Sotorasib (AMG-510). AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
  • HY-139001
    JKE-1716

    Glutathione Peroxidase Ferroptosis Others
    JKE-1716 is a potent and selective nitrolic acid-containing GPX4 inhibitor. JKE-1716 is able of inducing ferroptosis selectively through covalent GPX4 inhibition.
  • 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-124645
    QL-X-138

    Btk MNK Influenza Virus Cancer Infection
    QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK. QL-X-138 shows IC50s of 9.4 nM, 107.4 nM and 26 nM for BTK, MNK1 and MNK2 kinases respectively. QL-X-138 also shows anti-dengue virus 2 activity, with an IC50 of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies.
  • HY-12872
    Nazartinib

    EGF816

    EGFR Cancer
    Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively.
  • HY-123963
    C-178

    STING Inflammation/Immunology
    C-178 is a potent and selective covalent inhibitor of STING. C-178 binds to Cys91 and suppresses the STING responses elicited by distinct bona fide activators in mouse but not human.
  • HY-128867
    bio-THZ1

    CDK Cancer
    bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM.
  • HY-16293
    Lurbinectedin

    PM01183

    DNA Alkylator/Crosslinker DNA/RNA Synthesis Cancer
    Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
  • HY-108317
    ABL127

    Others Cancer
    ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
  • HY-132966
    ASP2453

    Ras Cancer
    ASP2453 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.
  • HY-132913
    Cyclopropenone probe 1

    Others Cancer
    Cyclopropenone probe 1 can specifically and efficiently modify a triple-negative breast cancer driver, glutathione S-transferase pi-1 (GSTP1), by covalently binding at the catalytic active site.
  • HY-12872A
    Nazartinib mesylate

    EGF816 mesylate

    EGFR Cancer
    Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively.
  • HY-15714
    NMS-859

    p97 Cancer
    NMS-859 is a potent, covalent VCP (p97) inhibitor, with IC50s of 0.37 and 0.36 μM for wild-type VCP in the presence of 60 μM and 1 mM ATP in cells, respectively.
  • HY-125930A
    T-2513 hydrochloride

    Topoisomerase DNA/RNA Synthesis Cancer
    T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
  • HY-125930
    T-2513

    Topoisomerase DNA/RNA Synthesis Cancer
    T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
  • HY-112596A
    H3B-6545 hydrochloride

    Estrogen Receptor/ERR Cancer
    H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.
  • HY-132882
    ARN19689

    Others Inflammation/Immunology
    ARN19689 is a potent, selective, orally active and non-covalent inhibitor of N‑Acylethanolamine-Hydrolyzing Acid Amidase (NAAA), with an IC50 of 42 nM. ARN19689 is a promising pharmacological tool to be further investigated in the field of inflammatory conditions.
  • HY-80013A
    THZ1 Hydrochloride

    CDK Cancer
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-107093
    MBC-11

    Others Cancer
    MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 has the potential for tumor-induced bone disease (TIBD) research.
  • HY-112596
    H3B-6545

    Estrogen Receptor/ERR Cancer
    H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.
  • HY-136430
    JCN037

    JGK037

    EGFR Cancer
    JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.
  • HY-107150
    Reproxalap

    ADX-102; NS-2

    Others Inflammation/Immunology
    Reproxalap (ADX-102) is a reactive aldehyde species (RASP) sequestering agent for the treatment of dry eye. Reproxalap (ADX-102) covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal.
  • HY-107985A
    (R)-FT671

    Others Others
    (R)-FT671 is the R-isomer of FT671. FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.
  • HY-80013
    THZ1

    CDK Cancer
    THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-131015
    HaXS8

    Others Others
    HaXS8 is a dimerizer that can promote a covalent and irreversible intracellular dimerization of HaloTag and SNAP-tagged proteins of interest. HaXS8 does not interfere with PI3K/mTOR signaling.
  • HY-126322
    DVD-445

    Others Cancer
    DVD-445 (Compound 7) is a potent peptidomimetic covalent thioredoxin reductase 1 (TrxR1) inhibitor with an IC50 of 0.60 μM for rat TrxR1. DVD-445 has good anticancer application.
  • HY-127104
    FMF-04-159-2

    CDK Cancer
    FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively.
  • HY-N5024
    Gambogenic acid

    Histone Methyltransferase Cancer
    Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination.
  • HY-135146
    GSK-3484862

    DNA Methyltransferase Cancer
    GSK-3484862 is a non-covalent inhibitor for Dnmt1. GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates global demethylation in murine embryonic stem cells.
  • HY-135659
    BSH-IN-1

    Bacterial Infection
    BSH-IN-1 is a potent and covalent inhibitor of gut bacterial recombinant bile salt hydrolases (BSHs) with IC50s of 108 nM and 427 nM for B. longum BSH (Gram positive) and B. theta BSH (Gram negative), respectively.
  • 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-107093B
    MBC-11 triethylamine

    Others Cancer
    MBC-11 triethylamine is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 triethylamine has the potential for tumor-induced bone disease (TIBD) research.
  • HY-12833
    AMZ30

    Others Others
    AMZ30 is a selective, covalent inhibitors of protein phosphatase methylesterase-1(PME-1; IC50=600 nM); selectively inactivates PME-1 and reduces the demethylated form of PP2A in living cells.
  • HY-132817
    Gunagratinib

    ICP-192

    FGFR Cancer
    Gunagratinib (ICP-192) is a low toxicity and orally active pan-FGFR (fibroblast growth factor receptors) inhibitor that potently and selectively inhibits FGFR activities irreversibly by covalent binding. Gunagratinib can be used for the research of cancer.
  • HY-107093A
    MBC-11 trisodium

    Others Cancer
    MBC-11 trisodium is a first-in-class conjugate of the bone-targeting bisphosphonate HEDP covalently linked to the antimetabolite Ara-C. MBC-11 trisodium has the potential for tumor-induced bone disease (TIBD) research.
  • HY-19024
    Merbarone

    NSC 336628

    Topoisomerase Cancer
    Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent.
  • HY-14879A
    Avibactam sodium

    NXL-104

    Bacterial Antibiotic Infection
    Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
  • HY-14879B
    Avibactam sodium hydrate

    NXL-104 hydrate

    Bacterial Antibiotic Infection
    Avibactam sodium hydrate (NXL-104 hydrate) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
  • HY-80003
    QL47

    Btk Cancer Infection
    QL47, a broad-spectrum antiviral agent, inhibits dengue virus and other RNA viruses. QL47 selectively inhibits eukaryotic translation. QL47 is a potent covalent inhibitor of BTK with an IC50 of 7 nM.
  • HY-124700
    LYPLAL1-IN-1

    Others Metabolic Disease
    LYPLAL1-IN-1 (Compound 11) is an selective covalent small-molecule inhibitor of Lysophospholipase-like 1 (LYPLAL1) with an IC50 of 0.006 μM. LYPLAL1-IN-1 increases glucose production.
  • 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-138683
    STING-IN-3

    STING Inflammation/Immunology
    STING-IN-3 is an inhibitor of stimulator of interferon genes (STING). STING-IN-3 efficiently inhibits both hsSTING and mmSTING through covalently target the predicted transmembrane cysteine residue 91 and thereby block the activation-induced palmitoylation of STING.
  • HY-138682
    STING-IN-2

    STING Inflammation/Immunology
    STING-IN-2 (C-170) is a potent and covalent STING inhibitor. STING-IN-2 efficiently inhibits both mouse STING (mmSTING) and human STING (hsSTING). STING-IN-2 can be used for autoinflammatory disease research.
  • HY-112215
    ARQ 531

    MK-1026

    Btk Cancer Inflammation/Immunology
    ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
  • HY-141550
    BPK-25

    Others Inflammation/Immunology
    BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP.
  • HY-P2270
    Phalloidin-TRITC

    Arp2/3 Complex Others
    Phalloidin-TRITC is a TRITC labeled, red fluorescence probe for F-actin. Phalloidin, bound to actin filaments, reacts covalently with amino acids Glu-llT, Met-ll9, and Met355, which are very close to the nucleotide binding site.
  • HY-139361
    Sulfopin

    PIN1-3

    Others 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.
  • HY-14879
    Avibactam free acid

    NXL-104 free acid

    Bacterial Antibiotic Infection
    Avibactam free acid (NXL-104 free acid) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
  • HY-16293S
    Lurbinectedin D3

    PM01183 D3

    DNA Alkylator/Crosslinker DNA/RNA Synthesis Cancer
    Lurbinectedin D3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
  • 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.
  • HY-131045
    HADA hydrochloride

    HCC-Amino-D-alanine hydrochloride

    Others Infection
    HADA hydrochloride (HCC-Amino-D-alanine hydrochloride) is a blue (λem~450 nm) fluorescent D-amino acid (FDAA). FDAAs are efficiently incorporated into the peptidoglycans (PGs) of diverse bacterial species at the sites of PG biosynthesis, allowing specific and covalent probing of bacterial growth with minimal perturbation.
  • HY-136298A
    X77

    SARS-CoV Infection
    X77 is a potent non-covalent inhibitor of the main protease of SARS-CoV-2 (SARS-CoV-2 M pro). X77 binds to SARS-CoV-2 M pro with a Kd value of 0.057 μM.
  • HY-112693
    H-151

    STING Inflammation/Immunology
    H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease.
  • HY-114299
    Salcaprozate sodium

    SNAC

    Others Others
    Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation.
  • HY-102046
    FM-381

    JAK Inflammation/Immunology
    FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
  • HY-133130
    JNJ-42226314

    MAGL Neurological Disease
    JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain.
  • HY-N3417
    Kongensin A

    HSP RIP kinase Apoptosis Cancer Inflammation/Immunology
    Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications.
  • HY-139535
    Luxeptinib

    CG-806

    FLT3 Btk Cancer
    Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells.
  • HY-111350
    FT827

    Deubiquitinase Cancer
    FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 µM). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 µM.
  • 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-105129
    Pimonidazole hydrochloride

    Others Cancer
    Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor. Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia .
  • HY-141514
    MSA-2 dimer

    STING Cancer Inflammation/Immunology
    MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide.
  • HY-123847
    KPT-6566

    Others Cancer
    KPT-6566, a potent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain. Anti-cancer activity.
  • HY-N0191
    Andrographolide

    Andrographis

    NF-κB SARS-CoV Influenza Virus Autophagy Cancer Infection Inflammation/Immunology
    Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
  • HY-105129A
    Pimonidazole

    Others Cancer
    Pimonidazole is a novel hypoxia marker for complementary study of tumor hypoxia and cell proliferation in tumor. Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after reduction of its nitro group, it can be used for qualitative and quantitative assessment of tumor hypoxia .
  • HY-106628
    Sudoxicam

    COX Inflammation/Immunology
    Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity.
  • HY-17600
    Acalabrutinib

    ACP-196

    Btk Cancer
    Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
  • HY-133118
    6RK73

    Deubiquitinase Cancer
    6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer.
  • HY-10586
    5-Azacytidine

    Azacitidine; 5-AzaC; Ladakamycin

    Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic Cancer Infection
    5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
  • HY-135747
    Gut restricted-7

    GR-7

    Bacterial Infection
    Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice.
  • HY-141480
    GSK-3β inhibitor 3

    GSK-3 Apoptosis Cancer
    GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia.
  • HY-122723
    GOT1 inhibitor-1

    Others Cancer
    GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
  • HY-109195
    Vebicorvir

    ABI-H0731

    HBV Infection Inflammation/Immunology
    Vebicorvir (ABI-H0731) is a first-generation hepatitis B virus (HBV) core protein inhibitor. Vebicorvir (ABI-H0731) suppresses covalently closed circular DNA (cccDNA) formation in two de novo infection models with EC50s from 1.84 μM to 7.3 μM.
  • HY-15816A
    Ulixertinib hydrochloride

    BVD-523 hydrochloride; VRT752271 hydrochloride

    ERK Cancer
    Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.
  • HY-124069
    M-525

    Epigenetic Reader Domain Cancer
    M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity.
  • HY-14380
    PF-3845

    FAAH Autophagy Inflammation/Immunology Cancer
    PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a Ki of 0.23 µM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition.
  • HY-136298
    (Rac)-X77

    SARS-CoV Infection
    (Rac)-X77 is a racemate of X77. X77 is a potent non-covalent inhibitor of the main protease of SARS-CoV-2 (SARS-CoV-2 M pro). X77 binds to SARS-CoV-2 M pro with a Kd value of 0.057 μM.
  • HY-101257A
    CDK7-IN-1

    CDK Cancer
    CDK7-IN-1, an analog of YKL-5-124, is a cyclin-dependent kinase 7 (cdk7) inhibitor, with an IC50 of less than 100 nM, extracted from patent WO 2016105528 A2, Compound 215.
  • HY-122054
    BPK-29

    Others Cancer
    BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
  • HY-112937
    GNE-6640

    Deubiquitinase Cancer
    GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.
  • HY-Y0469
    1-Aminohydantoin hydrochloride

    Others Others
    1-Aminohydantoin hydrochloride is a major metabolite of nitrofurantoin in animal tissues and can be used as a standard for the determination of residues of veterinary agents in meat, milk et.al. 1-Aminohydantoin hydrochloride covalently binds to tissue proteins and is released from the tissues under slightly acidic conditions and derivatized with 2-nitrobenzaldehyde to form nitrophenyl derivatives of AHD before detection.
  • HY-122054A
    BPK-29 hydrochloride

    Others Cancer
    BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
  • HY-A0004
    Decitabine

    5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716

    DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog Cancer
    Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.
  • HY-15772A
    Osimertinib mesylate

    AZD-9291 mesylate; Mereletinib mesylate

    EGFR Cancer
    Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-103046
    UbcH5c-IN-1

    E1/E2/E3 Enzyme Inflammation/Immunology
    UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
  • HY-15772
    Osimertinib

    AZD-9291; Mereletinib

    EGFR Cancer
    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-12680
    PRN694

    Itk Inflammation/Immunology
    PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo.
  • HY-138565
    K-975

    YAP Cancer
    K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma.
  • HY-136606
    SARS-CoV MPro-IN-1

    SARS-CoV Infection
    SARS-CoV MPro-IN-1 is a SARS-CoV-2 3CLpro covalent inhibitor, with an IC50 of 40 nM. SARS-CoV MPro-IN-1 shows good anti-SARS-CoV-2-infection activity in cell culture with an EC50 of 0.33 μM. SARS-CoV MPro-IN-1 has the potential for COVID-19 research.
  • HY-117570
    KSC-34

    Others Neurological Disease
    KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family.
  • HY-15816
    Ulixertinib

    BVD-523; VRT752271

    ERK Cancer
    Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.
  • HY-129589
    Thailanstatin A

    ADC Cytotoxin Cancer
    Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC.
  • HY-134205A
    CBR-470-1

    Keap1-Nrf2 Metabolic Disease Neurological Disease
    CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP +-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.
  • HY-116090
    Conoidin A

    Parasite Infection Neurological Disease Cardiovascular Disease
    Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease.
  • HY-15772S
    Osimertinib D6

    AZD-9291 D6; Mereletinib D6

    EGFR Cancer
    Osimertinib D6 (AZD-9291 D6) is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
  • HY-106991A
    Amustaline dihydrochloride

    S-303 dihydrochloride

    HIV Bacterial Infection
    Amustaline (S-303) dihydrochloride, a nucleic acid-targeted alkylator, is an efficient pathogen inactivation agent for blood components containing red blood cells. Amustaline dihydrochloride has three components: an acridine anchor (an intercalator that targets nucleic acids non-covalently), an effector (a bis-alkylator group that reacts with nucleophiles), and a linker (a small flexible carbon chain containing a labile ester bond that hydrolyzes at neutral pH to yield non-reactive breakdown products).
  • 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-15317
    RI-1

    RAD51 Cancer
    RI-1 is a RAD51 inhibitor, with IC50s ranging from 5 to 30 μM. RI-1 binds covalently to the surface of RAD51 protein at cysteine 319. RI-1 inactivates RAD51 by directly binding to a protein surface that serves as an interface between protein subunits in RAD51 filaments. RI-1 can disrupt homologous recombination in human cells.
  • HY-113466
    4-Hydroxynonenal

    4-HNE

    Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite Cancer Neurological Disease Cardiovascular Disease
    4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
  • HY-100848
    TX1-85-1

    EGFR Cancer
    TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
  • HY-109010
    Poseltinib

    HM71224; LY3337641

    Btk BMX Kinase Toll-like Receptor (TLR) Metabolic Disease
    Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling.
  • HY-13509
    CCG-50014

    RGS Protein Inflammation/Immunology
    CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.
  • HY-N1912
    Andropanolide

    NF-κB Inflammation/Immunology
    Andrographolide (Andro) is a small antagonist for NF-κB activation by covalent modifying reduced cysteine 62 of p50. Andrographolide is a bicyclic diterpenoid lactone mainly produced from the plant Andrographis (Andrographis paniculate). Andrographolide suppresses the activation of NF-κB in stimulated endothelial cells, which reduces the expression of cell adhesion molecule E-selectin and prevents E-selectin-mediated leukocyte adhesion, but has no effect on IκBα degradation, p50 and p65 nuclear translocation.
  • 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-128892
    EN6

    Autophagy Proton Pump Neurological Disease
    EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H + ATPase (v-ATPase). EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner.
  • HY-10865
    LY2183240

    FAAH Autophagy Neurological Disease
    LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
  • HY-128851
    Coenzyme A

    Endogenous Metabolite Cancer Neurological Disease
    Coenzyme A is is an obligatory cofactor in all living cells synthesised from pantothenate (Vitamin B5), adenosine triphosphate (ATP) and cysteine. Covalent binding of Coenzyme A to Peroxiredoxin 5 (Prdx5) results in complete inhibition of its peroxidase activity, which is reversed by reduction with DTT.Coenzyme A and its thioester derivatives are key players in major catabolic and anabolic pathways and the regulation of gene expression. Many human pathologies, including cancer, diabetes and neurodegeneration, have been associated with abnormal biosynthesis and homeostasis of CoA and its derivatives.
  • HY-111553
    TAS0728

    EGFR Cancer
    TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity.
  • HY-137516
    LC-2

    PROTACs Ras Cancer
    LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.
  • HY-126247
    BI-2852

    Ras Cancer
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRAS G12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRAS G12D versus KRAS wt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
  • HY-129550
    BI-4020

    EGFR Cancer
    BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties.
  • HY-101522
    CHMFL-EGFR-202

    EGFR BMX Kinase Btk MEK Cancer
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.