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covalently reversible

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52

Inhibitors & Agonists

6

Fluorescent Dye

1

Biochemical Assay Reagents

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-163624
    Bfl-1-IN-2

    		Bcl-2 Family Cancer
    Bfl-1-IN-2 (Compound 13) is a reversible and covalent inhibitor of Bfl-1 (IC50: 4.3 μM). Bfl-1-IN-2 acts by binding to Cys55 of Bfl-1 .
    Bfl-1-IN-2
  • 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 .
    Chst15-IN-1
  • HY-148535
    Calpain Inhibitor XI

    		Proteasome Neurological Disease
    Calpain Inhibitor XI is a reversible covalent inhibitor of calpain-1. Calpain Inhibitor XI can be used for the research of neurodegenerative disorders .
    Calpain Inhibitor XI
  • HY-170485
    Thrombin inhibitor 13

    		Thrombin Cardiovascular Disease
    Thrombin inhibitor 13 (Compound 13a) is a covalent and reversible inhibitor for thrombin (FIIa) with an IC50 of 0.7 nM. Thrombin inhibitor 13 prolongs the activated partial thromboplastin time (aPTT) and prothrombin time (PT), exhibits antithrombotic and anticoagulant activities .
    Thrombin inhibitor 13
  • HY-157778
    MK-7845

    		SARS-CoV Infection
    MK-7845 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC50 of 8.7 nM .
    MK-7845
  • HY-115902
    FGFR4-IN-7

    		FGFR Apoptosis Cancer
    FGFR4-IN-7 (Compound C3) is a covalent reversible FGFR4 inhibitor with an IC50 value of 0.42 μM. FGFR4-IN-7 induces apoptosis via the FGFR4 signaling pathway blockage. FGFR4-IN-7 can be used for the research of hepatocellular carcinoma (HCC) .
    FGFR4-IN-7
  • 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.
    FM-479
  • HY-161066
    KRAS G13D-IN-1

    		Ras Cancer
    KRAS G13D-IN-1 (compound 41) is a selective and covalently reversible inhibitor of KRAS G13D (IC50: 0.41 nM). The selectivity for KRAS G13D is 29-fold against KRAS wild type. KRAS G13D-IN-1 is an inhibitor of the GDP state and targets the SWII binding pocket of KRAS G13D. KRAS G13D-IN-1 inhibits KRAS binding to GDP and turns on/off downstream signaling cascades .
    KRAS G13D-IN-1
  • HY-143881
    FGFR4-IN-6

    		FGFR Cancer
    FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    FGFR4-IN-6
  • HY-168347
    TH152

    		Atg8/LC3 Others
    TH152 is a reversible, pan ligand for LC3/GABARAP with a KD of 2 µM. LC3/GABARAP is an autophagy associated protein .
    TH152
  • HY-10836
    Cruzain-IN-1

    		Parasite Others
    Cruzain-IN-1 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.
    Cruzain-IN-1
  • HY-116533
    RMM-46

    		MAPKAPK2 (MK2) Cancer
    RMM-46 is a selective and reversible covalent inhibitor for MSK/RSK-family kinases .
    RMM-46
  • HY-112166
    Rilzabrutinib

    PRN1008

    		 Btk Metabolic Disease Cancer
    Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
    Rilzabrutinib
  • HY-129314
    CM-39

    		Aldehyde Dehydrogenase (ALDH) Cancer
    CM-39 is a non-covalent and reversible inhibitor for aldehyde dehydrogenase 1A (ALDH1A) with an IC50 of 0.9 μM .
    CM-39
  • HY-168506
    MSC-1254

    		YAP Cancer
    MSC-1254 is a reversible, selective and covalent TEAD1 inhibitor. MSC-1254 can be used for the study of cancer .
    MSC-1254
  • HY-146649
    LmCPB-IN-1

    		Parasite Cathepsin Infection
    LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pKi of 9.7 .
    LmCPB-IN-1
  • HY-150717
    RSK2-IN-3

    		Ribosomal S6 Kinase (RSK) Cancer
    RSK2-IN-3 (Compound 26) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase .
    RSK2-IN-3
  • HY-19415
    SB-435495

    		Phospholipase Metabolic Disease
    SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM .
    SB-435495
  • HY-19415A
    SB-435495 hydrochloride

    		Phospholipase Metabolic Disease
    SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM .
    SB-435495 hydrochloride
  • HY-19415B
    SB-435495 ditartrate

    		Phospholipase Metabolic Disease
    SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM .
    SB-435495 ditartrate
  • 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 .
    MYF-01-37
  • HY-123564
    Mcl1-IN-7

    		Others Others
    Mcl1-IN-7 (compound 11) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. By covalently targeting the non-catalytic lysine side chain of Mcl-1, it has higher potency than non-covalent counterparts and can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.
    Mcl1-IN-7
  • HY-152009
    SARS-CoV-2 3CLpro-IN-7

    		SARS-CoV Infection
    SARS-CoV-2 3CLpro-IN-7 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC50 value of 1.4 µM .
    SARS-CoV-2 3CLpro-IN-7
  • HY-120631A
    BMS-538305 hydrochloride

    		Others Others
    BMS-538305 hydrochloride is a potent and selective inhibitor of dipeptidyl peptidase IV (DPP-IV), exhibiting strong biological activity by forming a reversible covalent complex with the enzyme. BMS-538305 hydrochloride demonstrates its mechanism of action through the covalent attachment between the nitrile carbon of the inhibitor and the enzyme residue S630, as unveiled by the X-ray crystal structure analysis.
    BMS-538305 hydrochloride
  • HY-103462
    TC-F2

    		FAAH Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
    TC-F2 is a reversible non-covalent binding inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 28 nM. FAAH is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders .
    TC-F2
  • HY-14879A
    Avibactam sodium
    Maximum Cited Publications
    67 Publications Verification

    NXL-104

    		 Beta-lactamase 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 .
    Avibactam sodium
  • HY-14879B
    Avibactam sodium hydrate
    Maximum Cited Publications
    67 Publications Verification

    NXL-104 hydrate

    		 Beta-lactamase Bacterial Antibiotic Infection
    Avibactam sodium (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 .
    Avibactam sodium hydrate
  • HY-112215
    Nemtabrutinib
    3 Publications Verification

    ARQ-531; MK-1026

    		 Btk Inflammation/Immunology Cancer
    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.
    Nemtabrutinib
  • HY-150643
    RSK2-IN-2

    		Ribosomal S6 Kinase (RSK) Cancer
    RSK2-IN-2 (Compound 25) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase. RSK2-IN-2 is also described to inhibit MSK1, MSK2 and RSK3 .
    RSK2-IN-2
  • HY-14879
    Avibactam free acid
    Maximum Cited Publications
    67 Publications Verification

    NXL-104 free acid

    		 Beta-lactamase Bacterial Antibiotic Infection
    Avibactam (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 .
    Avibactam free acid
  • HY-14879C
    Avibactam sodium dihydrate

    NXL-104 dihydrate

    		 Beta-lactamase Bacterial Antibiotic Infection
    Avibactam sodium (NXL-104) dihydrate 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 .
    Avibactam sodium dihydrate
  • 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 .
    JNJ-42226314
  • HY-139535
    Luxeptinib
    1 Publications Verification

    CG-806

    		 FLT3 Btk Apoptosis 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 .
    Luxeptinib
  • HY-150587
    Anti-inflammatory agent 31

    		ERK NF-κB Inflammation/Immunology
    Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver .
    Anti-inflammatory agent 31
  • HY-144323
    YF135

    		PROTACs PERK Cancer
    YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
    YF135
  • HY-102046
    FM-381
    1 Publications Verification

    		 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.
    FM-381
  • HY-160168
    BTK-IN-31

    		Btk Infection Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    BTK-IN-31 (Compound 2) is a selective, non-covalently reversible, and blood-brain barrier (BBB) permeable Btk inhibitor. BTK-IN-31 has research potential in immune disorders, cancer, cardiovascular disease, viral infections, inflammation, metabolic/endocrine dysfunction, and neurological disorders .
    BTK-IN-31
  • HY-164002
    PF-303

    		Btk Others
    PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation .
    PF-303
  • HY-15816A
    Ulixertinib hydrochloride
    25+ Cited Publications

    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 .
    Ulixertinib hydrochloride
  • HY-14879AR
    Avibactam (sodium) (Standard)

    		Beta-lactamase Bacterial Antibiotic Infection
    Avibactam (sodium) (Standard) is the analytical standard of Avibactam (sodium). This product is intended for research and analytical applications. 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 .
    Avibactam (sodium) (Standard)
  • HY-14879S2
    Avibactam sodium salt-13C5

    NXL-104-13C5

    		 Isotope-Labeled Compounds Antibiotic Beta-lactamase Bacterial Infection
    Avibactam sodium salt- 13C5 (NXL-104- 13C5) is 13C labeled Avibactam (sodium). 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 .
    Avibactam sodium salt-13C5
  • HY-15816
    Ulixertinib
    25+ Cited Publications

    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 .
    Ulixertinib
  • HY-169228
    WS-11

    		Btk Cancer
    WS-11 is a non-covalent reversible BTK inhibitor with IC50s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds .
    WS-11
  • HY-150702
    MAGLi 432

    		MAGL Neurological Disease Inflammation/Immunology
    MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease .
    MAGLi 432
  • HY-170649
    RdRP-IN-9

    		SARS-CoV Infection
    RdRP-IN-9 (Compound 6b) is a reversible covalent allosteric inhibitor of RdRp. RdRP-IN-9 demonstrates high anti-coronavirus activity, with an EC 50 value of 0.68 μM against HCoV-OC43 RdRP-IN-9 exerts a more prolonged antiviral effect by reversibly acylating Cys12 in the NiRAN domain of non-structural protein 12 (nsp 12) and exhibits synergistic anti-coronavirus activity with Molnupiravir (HY-135853) .
    RdRP-IN-9
  • HY-152005
    SARS-CoV-2 3CLpro-IN-6

    		SARS-CoV Infection
    SARS-CoV-2 3CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro-IN-6 has potent inhibitory activity for SARS-CoV-2 3CL pro with an IC50 value of 4.9 μM. SARS-CoV-2 3CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19) .
    SARS-CoV-2 3CLpro-IN-6
  • HY-D1804
    Vari Fluor 680-Streptavidin

    		Fluorescent Dye Others
    Vari Fluor 680-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=680 nm/701 nm.
    Vari Fluor 680-Streptavidin
  • HY-D1805
    Vari Fluor 647-Streptavidin

    		Fluorescent Dye Others
    Vari Fluor 647-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=650 nm/665 nm.
    Vari Fluor 647-Streptavidin
  • HY-D1806
    Vari Fluor 594-Streptavidin

    		Fluorescent Dye Others
    Vari Fluor 594-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=590 nm/617 nm.
    Vari Fluor 594-Streptavidin
  • HY-D1807
    Vari Fluor 555-Streptavidin

    		Fluorescent Dye Others
    Vari Fluor 555-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=555 nm/565 nm.
    Vari Fluor 555-Streptavidin

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