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Results for "

catalytic domains

" in MedChemExpress (MCE) Product Catalog:

88

Inhibitors & Agonists

1

Screening Libraries

6

Peptides

3

Inhibitory Antibodies

5

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P99415
    Abelacimab

    MAA868

    		 Factor Xa Cardiovascular Disease
    Abelacimab (MAA868) is a fully human IgG1 monoclonal antibody that binds with high affinity to the catalytic structural domain of FXI and locks it in the zymogen conformation, thereby preventing its activation by FXIIa or thrombin. Abelacimab can be used in thromboembolic disease studies .
    Abelacimab
  • HY-128760
    COH34
    1 Publications Verification

    		 Poly(ADP-ribose) Glycohydrolase (PARG) Cancer
    COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors .
    COH34
  • HY-123847
    KPT-6566
    1 Publications Verification

    		 PIN1 Cancer
    KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer .
    KPT-6566
  • HY-112937
    GNE-6640
    5+ Cited Publications

    		 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 USP47 and Ub-MDM2, respectively .
    GNE-6640
  • HY-100671
    L002

    		Histone Acetyltransferase STAT Cardiovascular Disease Inflammation/Immunology Cancer
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment .
    L002
  • HY-100034
    NSC 663284
    5+ Cited Publications

    DA-3003-1

    		 Phosphatase Histone Methyltransferase Cancer
    NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
    NSC 663284
  • HY-G0017
    N-Desmethyl imatinib
    1 Publications Verification

    Norimatinib; Imatinib metabolite N-Desmethyl imatinib; CGP 74588

    		 Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib
  • HY-122886
    XL 188
    1 Publications Verification

    		 Deubiquitinase Cancer
    XL 188 is a potent and selective USP7 inhibitor with IC50 values of 90 nM and 193 nM for USP7 full-length and catalytic domain enzyme, respectively. XL 188 can be used in research of cancer .
    XL 188
  • HY-109143
    Elsubrutinib
    2 Publications Verification

    ABBV-105

    		 Btk Inflammation/Immunology
    Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor. The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease .
    Elsubrutinib
  • HY-76222
    Isatoic anhydride

    		Drug Intermediate Others
    Isatoic anhydride is a single-adduct forming reagent and a monofunctional SHAPE reagent. Isatoic anhydride reacts with the 2'-hydroxyl group of RNA nucleotides via a single reactive group to form a single adduct, without forming cross-links between nucleotides. In SHAPE-JuMP experiments, Isatoic anhydride serves as a control reagent for single-adduct formation, which is used to distinguish true cross-links from single-adduct formation .
    Isatoic anhydride
  • HY-139979
    USP5-IN-1
    3 Publications Verification

    		 Deubiquitinase Cancer
    USP5-IN-1 (compound 64) is a selective competitive inhibitor of USP5 zinc finger ubiquitin binding domain (ZnF-UBD) (KD=2.8 μM). USP5-IN-1 competitively blocks the binding of ubiquitin to ZnF-UBD, inhibits the catalytic activity of USP5, and thus hinders the hydrolysis of ubiquitin chains. USP5-IN-1 can inhibit USP5 cleavage of Lys48-linked diubiquitin substrates in vitro and is a potential USP5 chemical probe and potential inhibitor of USP5-related cancers.
    USP5-IN-1
  • HY-135714
    Bavarostat

    EKZ-001

    		 HDAC Microtubule/Tubulin Neurological Disease Cancer
    Bavarostat (EKZ-001) is a blood-brain barrier-permeable, potent HDAC6 inhibitor and PET radiotracer, with an IC50 as low as 17 nM against human HDAC6. Bavarostat can be labeled with 18F and used as a probe to map HDAC6 distribution and measure target occupancy in the brains of non-human primates. Bavarostat also selectively modulates tubulin acetylation, but not histone acetylation. Bavarostat is applicable for research on Alzheimer's disease, other neurodegenerative disorders, and cancers .
    Bavarostat
  • HY-104001
    BAY-524
    1 Publications Verification

    		 Ser/Thr Kinase Cancer
    BAY-524 is a potent Bub1 kinase inhibitor. BAY-524 inhibits the recombinant catalytic domain of human Bub1 with an IC50 of 450 nM. BAY-524 can be used for the research of anti-cancer in combination with other agents .
    BAY-524
  • HY-148757
    TIM-063

    		CaMK Metabolic Disease
    TIM-063 is a selective and cell-permeable CaMKK inhibitor, ATP competitive inhibitor, can directly target the catalytic domain of CaMKK, with the Ki values of 0.35 μM and 0.2 μM for CaMKKα and CaMKKβ, respectively, the IC50 values are 0.63 μM and 0.96 μM, respectively .
    TIM-063
  • HY-N3103
    p-Coumaric Acid Ethyl Ester

    Ethyl (E)-p-hydroxycinnamate; Ethyl trans-4-hydroxycinnamate

    		 Tyrosinase Inflammation/Immunology
    p-Coumaric Acid Ethyl Ester (Ethyl (E)-p-hydroxycinnamate; Ethyl trans-4-hydroxycinnamate) is a non-competitive, reversible inhibitor of tyrosinase (IC50=4.89 μg/mL, Ki=1.83 μg/mL), which can quench the intrinsic fluorescence of the enzyme. p-Coumaric Acid Ethyl Ester changes the binding affinity of L-tyrosine by inducing conformational changes in the catalytic domain of tyrosinase, and does not bind to the copper ion of the enzyme. p-Coumaric Acid Ethyl Ester is used in the development of medicines, cosmetics and fruit preservation products using pollen .
    p-Coumaric Acid Ethyl Ester
  • HY-P10939A
    Ac-DMLD-CMK TFA

    		Caspase Pyroptosis Inflammation/Immunology Cancer
    Ac-DMLD-CMK TFA is a caspase 3 inhibitor and a GSDME inhibitor. Ac-DMLD-CMK TFA binds directly to the catalytic domain of caspase-3, blocks caspase-3-mediated cleavage of GSDME, inhibits the activation of caspase 3 and Gsdme in the caspase 3-Gsdme signaling pathway, and reduces the levels of pyroptosis and apoptosis as well as the expression of LDH, IL-6, IL-1β and IL-18. Ac-DMLD-CMK TFA alleviates renal function deterioration, renal tubular epithelial cell injury, inflammatory cytokine secretion, pulmonary structural damage, and chemotherapy-induced nephrotoxicity .
    Ac-DMLD-CMK TFA
  • HY-N10159
    1-Benzyl-I3C

    		E1/E2/E3 Enzyme Cancer
    1-Benzyl-I3C is a NEDD4-1 inhibitor with significant anticancer activity. 1-Benzyl-I3C can directly inhibit the ubiquitination activity of NEDD4-1 with an IC50 of 12.3μM, which is significantly better than its precursor compound I3C of 284μM. 1-Benzyl-I3C and its analogs showed good effects in inhibiting the proliferation of human melanoma cells, which is roughly related to their potency as NEDD4-1 enzyme inhibitors. By combining in vitro ubiquitination experiments and thermal stability analysis, 1-Benzyl-I3C was shown to be able to bind to the catalytic HECT domain of NEDD4-1 .
    1-Benzyl-I3C
  • HY-155374
    PP5-IN-1

    		Phosphatase Apoptosis Caspase Cancer
    PP5-IN-1 is a competitive and selective serine/threonine protein phosphatase 5 (PP5) inhibitor with a Ki value of 244 nM. PP5-IN-1 induces extrinsic apoptosis (Apoptosis), disrupts the integrity of complex II, and activates Caspase 8. PP5-IN-1 can be used in research related to clear cell renal cell carcinoma .
    PP5-IN-1
  • HY-N0086R
    N6-Methyladenosine (Standard)
    1 Publications Verification

    6-Methyladenosine (Standard); N-Methyladenosine (Standard)

    		 Endogenous Metabolite Influenza Virus Reference Standards Infection
    N6-Methyladenosine (Standard) is the analytical standard of N6-Methyladenosine. This product is intended for research and analytical applications. N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities. In Vitro: N6-methyladenosine (m6A) is selectively recognized by the human YTH domain family 2 (YTHDF2) protein to regulate mRNA degradation. N6-methyladenosine (m6A), a prevalent internal modification in the messenger RNA of all eukaryotes, is post-transcriptionally installed by m6A methyltransferase (e.g., MT-A70) within the consensus sequence of G(m6A)C (70%) or A(m6A)C (30%). N6-methyladenosine (m6A)-containing RNAs are greatly enriched in the YTHDF-bound portion and diminished in the flow-through portion . N6-methyladenosine (m6A), the most abundant internal RNA modification, functions in diverse biological processes, including regulation of embryonic stem cell self-renewal and differentiation. N6-methyladenosine (m6A) is a large protein complex, consisting in part of methyltransferase-like 3 (METTL3) and methyltransferase-like 14 (METTL14) catalytic subunits .
    N6-Methyladenosine (Standard)
  • HY-P10939
    Ac-DMLD-CMK

    		Caspase Pyroptosis Inflammation/Immunology Cancer
    Ac-DmLD-CMK is a caspase 3 inhibitor and a GSDME inhibitor. Ac-DmLD-CMK binds directly to the catalytic domain of caspase-3, blocks caspase-3-mediated cleavage of GSDME, inhibits the activation of caspase 3 and Gsdme in the caspase 3-Gsdme signaling pathway, and reduces the levels of pyroptosis and apoptosis as well as the expression of LDH, IL-6, IL-1β and IL-18. Ac-DmLD-CMK alleviates renal function deterioration, renal tubular epithelial cell injury, inflammatory cytokine secretion, pulmonary structural damage, and chemotherapy-induced nephrotoxicity .
    Ac-DMLD-CMK
  • HY-122142A
    Pyr-​Pro-​Arg-​pNA (hydrochloride)

    S-2366 (hydrochloride)

    		 APC Factor XI Biochemical Assay Reagents Others
    Pyr-​Pro-​Arg-​pNA (S-2366) hydrochloride is a chromogenic peptidyl substrate, and a noncompetitive inhibitor that occupies the active sites of FXIa and FXIa-LC to block factor IX activation. Pyr-​Pro-​Arg-​pNA hydrochloride functions as a hydrolyzable substrate for FXIa’s catalytic domain, human APC, murine APC, and purified plasma kallikrein .
    Pyr-​Pro-​Arg-​pNA (hydrochloride)
  • HY-G0017S
    N-Desmethyl imatinib-d8

    Norimatinib-d8; Imatinib metabolite N-Desmethyl imatinib-d8; CGP 74588-d8

    		 Isotope-Labeled Compounds Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib-d8
  • HY-156466
    QL-1200186

    		STAT Interleukin Related IFNAR Inflammation/Immunology
    QL-1200186 is a selective, orally active, allosteric inhibitor targeting the tyrosine kinase TYK2 pseudokinase domain JH2 (IC50=0.06 nM, TYK2 JH2), with 164-fold selectivity over TYK1 JH2 (IC50=9.85 nM，TYK1 JH2). QL-1200186 first stabilizes the TYK2 JH2 conformation, inhibits the activity of the JH1 catalytic domain, and blocks the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. QL-1200186 can inhibit the production of Th1/Th17 cell-related cytokines (such as IFNγ, IL-23), reduce immune cell activation, and has no significant effect on JAK1/2/3 kinase activity. QL-1200186 can significantly improve skin inflammation in the Imiquimod (HY-B0180)-induced psoriasis mouse model and reduce the Psoriasis Area and Severity Index (PASI) score. QL-1200186 can be used in the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE) .
    QL-1200186
  • HY-124857
    7DG

    7-Desacetoxy-6,7-dehydrogedunin

    		 PERK Prokineticin Receptor P2X Receptor Caspase NOD-like Receptor (NLR) Pyroptosis Tyrosinase Neurological Disease Metabolic Disease Inflammation/Immunology
    7DG (7-Desacetoxy-6,7-dehydrogedunin) is a PKR inhibitor, P2X7 purinergic receptor inhibitor, and skin-lightening agent. 7DG binds outside the ATP-catalytic domain of PKR, blocks the kinase activity-independent protein-protein interactions of PKR, inhibits the phosphorylation and activity of PKR, disrupts ASC assembly and caspase-1 activation, and suppresses the activation of the NLRP1 inflammasome. 7DG inhibits pyroptosis, suppresses the ATP-P2X7 signaling pathway, and abolishes ATP-induced increases in the expression levels of MITF, tyrosinase, PMEL/gp100, and melanin content. 7DG exerts skin-lightening effects in cultured skin in vitro. 7DG can be used in research related to chronic obstructive pulmonary disease, gout, type 2 diabetes, Alzheimer's disease, and hyperpigmentary skin disorders .
    7DG
  • HY-115383
    Roflupram
    1 Publications Verification

    		 Phosphodiesterase (PDE) Neurological Disease Inflammation/Immunology
    Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors .
    Roflupram
  • HY-168509
    IMPDH-IN-1

    		Bacterial Infection
    IMPDH-IN-1 (compound 44) is a bacterial inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitor. IMPDH-IN-1 specifically binds to the catalytic domain of IMPDH. IMPDH-IN-1 potently inhibits the IMPDH of Pseudomonas aeruginosa, Staphylococcus aureus and Escherichia coli .
    IMPDH-IN-1
  • HY-P10463
    ssK36

    		Histone Methyltransferase Cancer
    ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. ssK36 is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
    ssK36
  • HY-117977
    FCPR03

    		Phosphodiesterase (PDE) Neurological Disease Inflammation/Immunology
    FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects .
    FCPR03
  • HY-153094
    BDM-2

    		HIV HIV Integrase Infection
    BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity .
    BDM-2
  • HY-P10463A
    ssK36 TFA

    		Histone Methyltransferase Cancer
    ssK36 TFA is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2) , and ssK36 TFA is designed for the SETD2 protein, a specific PKMT. ssK36 TFA is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 TFA can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 TFA can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
    ssK36 TFA
  • HY-122735
    Inh2-B1

    		Ser/Thr Kinase Bacterial Infection
    Inh2-B1 is a Ser/Thr protein kinase (STK1) inhibitor. Inh2-B1 specifically inhibits STK1 activity by directly binding to its ATP-binding catalytic domain. Inh2-B1 down-regulates cell wall hydrolase genes and disrupts the biofilm formation of Methicillin-resistant Staphylococcus aureus (MRSA) clearly .
    Inh2-B1
  • HY-N12982
    α-Calacorene

    		Others Others
    α-Calacorene is a sesquiterpene that can be isolated from Réunion vetiver oil .
    α-Calacorene
  • HY-124308
    PS315

    		PKC Cancer
    PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity .
    PS315
  • HY-162094
    CMX410

    		Acyltransferase Bacterial Infection
    CMX410 is an orally active and selective Mycobacterium tuberculosis Pks13 acyltransferase domain inhibitor and anti-bacterial agent. CMX410 reacts with the catalytic serine of the Pks13-AT domain to form a stable β-lactam ring, disables the enzyme’s active site, reduces trehalose monomycolate and trehalose dimycolate levels, triggers cell lysis, and reduces intracellular bacterial burden. CMX410 can be used for the research of tuberculosis .
    CMX410
  • HY-P10416
    Q14

    Q14 peptide

    		 Deubiquitinase Mitophagy Others Neurological Disease
    Q14 is a polypeptide derived from the USP30 (ubiquitin specific peptidase 30) transmembrane (TM) domain with the ability to inhibit the deubiquitination activity of USP30 (IC50=57.2 nM). Q14 reduces USP30 activity by inhibiting the interaction between the USP30 transmembrane domain and its catalytic domain. Q14 peptide contains the LC3 interaction region (LIR) motif, which enables it to bind to the LC3 and accelerate the formation of autophagosomes, thereby promoting mitophagy. Q14 can be used in the study of neurodegenerative diseases as well as mitochondrial quality control and cell metabolism .
    Q14
  • HY-122142
    Pyr-​Pro-​Arg-​pNA

    S-2366

    		 Biochemical Assay Reagents APC Factor XI Inflammation/Immunology
    Pyr-​Pro-​Arg-​pNA (S-2366) is a chromogenic peptidyl substrate, and a noncompetitive inhibitor that occupies the active sites of FXIa and FXIa-LC to block factor IX activation. Pyr-​Pro-​Arg-​pNA functions as a hydrolyzable substrate for FXIa’s catalytic domain, human APC, murine APC, and purified plasma kallikrein .
    Pyr-​Pro-​Arg-​pNA
  • HY-E70696
    EGFR C797S/L858R Recombinant Human Active Protein Kinase

    		EGFR Cancer
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR C797S/L858R protein that can be used to study EGFR C797S/L858R-related functions .
    EGFR C797S/L858R Recombinant Human Active Protein Kinase
  • HY-174443
    PROTAC sEH degrader-2

    		PROTACs Epoxide Hydrolase Neurological Disease Inflammation/Immunology
    PROTAC sEH degrader-2 is a PROTAC targeting degradation agent for soluble epoxide hydrolase (sEH) with pIC50 values of the catalytic domain of 8.37 (human sEH-H) and 7.12 (mouce sEH-H). PROTAC sEH degrader-2 can be used for the research related to inflammation and neuroinflammation, such as Alzheimer's disease . (Structure Note: Pink: sEH-H ligand (HY-174225); Blue: CRBN Ligand (HY-103597); Black: linker; E3 + linker (HY-141011))
    PROTAC sEH degrader-2
  • HY-179421
    PROTAC HDAC6 degrader 7

    		PROTACs HDAC NF-κB NOD-like Receptor (NLR) Interleukin Related TNF Receptor Inflammation/Immunology
    PROTAC HDAC6 degrader 7 is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6 (HDAC6) (IC50 = 118 nM). PROTAC HDAC6 degrader 7 can eliminate both the catalytic and zinc-finger ubiquitin-binding domain. PROTAC HDAC6 degrader 7 inhibits NLRP3 inflammasome assembly and activation, as well as blocks NF-κB signaling, thereby reducing the transcription and release of key inflammatory factors. PROTAC HDAC6 degrader 7 can reduce the mRNA levels of NLRP3, pro-IL-1β, TNF-α, and IL-6. PROTAC HDAC6 degrader 7 can be used for the study of inflammatory bowel disease (IBD) .
    PROTAC HDAC6 degrader 7
  • HY-174301
    USP7-IN-18

    		Deubiquitinase DNA Methyltransferase MDM-2/p53 Cancer
    USP7-IN-18 is a naphthalene derivative. USP7-IN-18 is a selective USP7 inhibitor (IC50 : 130.9 nM), with no or very weak inhibition of the other 8 DUBs including USP47. USP7-IN-18 specifically binds to the catalytic domain of USP7, blocking its deubiquitinase activity. USP7-IN-18 causes degradation of the oncogenic proteins MDM2 and DNMT1, and also degrades the novel target PCLAF. USP7-IN-18 activates the p53-p21 pathway. USP7-IN-18 exerts anti-tumor effects in colon cancer animal models and reshapes the tumor immune microenvironment. USP7-IN-18 achieves both direct cytotoxic and immune-synergistic anti-tumor actions.
    USP7-IN-18
  • HY-153768
    KAT modulator-1

    		Histone Acetyltransferase Cancer
    KAT modulator-1 (Compound 3) is a KAT modulator. KAT modulator-1 can interact with p300 full-length but not with the catalytic domain. KAT modulator-1 can be used for epigenetics research .
    KAT modulator-1
  • HY-12135
    Poloxipan

    		Polo-like Kinase (PLK) PIN1 STAT Cancer
    Poloxipan is a pan-specific polo-like kinase (PLK) inhibitor that can inhibit a non-catalytic region at the C-terminus called the Polo-box domain (PBD) found in kinases. The IC50 values for Poloxipan against the PBDs of PLK-1/2/3 are 3.2 μM, 1.7 μM, and 3.0 μM, respectively. Poloxipan also inhibits other phospho-tyrosine binding domains, such as the forkhead-associated (FHA) domain of CHK-2, the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1), and the phospho-tyrosine binding domains of STAT1/3/5 and lymphocyte-specific protein tyrosine kinase's SH2 domain. Poloxipan can be used in cancer research .
    Poloxipan
  • HY-112800
    cyt-PTPε Inhibitor-1

    		Phosphatase Metabolic Disease
    cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity .
    cyt-PTPε Inhibitor-1
  • HY-E70691
    CLK1 Recombinant Human Active Protein Kinase

    		CDK Cancer
    CLK1 is one of the dual specificity kinases and is the founding member of the 'LAMMER' family of kinases. CLK1 activity is positively regulated by phosphorylation on either tyrosine residues or serine/threonine residues, and is negatively regulated by steric constraints mediated by the N-terminal domain, as well as, by phosphorylation on a subset of serine/threonine residues within the catalytic domain. CLK1 Recombinant Human Active Protein Kinase is a recombinant CLK1 protein that can be used to study CLK1-related functions .
    CLK1 Recombinant Human Active Protein Kinase
  • HY-E70704
    EGFR G719C Recombinant Human Active Protein Kinase

    		EGFR Cancer
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR G719C Recombinant Human Active Protein Kinase is a recombinant EGFR G719C protein that can be used to study EGFR G719C-related functions .
    EGFR G719C Recombinant Human Active Protein Kinase
  • HY-E70706
    EGFR L718Q Recombinant Human Active Protein Kinase

    		EGFR Cancer
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L718Q Recombinant Human Active Protein Kinase is a recombinant EGFR L718Q protein that can be used to study EGFR L718Q-related functions .
    EGFR L718Q Recombinant Human Active Protein Kinase
  • HY-E70695
    EGFR C797S Recombinant Human Active Protein Kinase

    		EGFR Cancer
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S Recombinant Human Active Protein Kinase is a recombinant EGFR C797S protein that can be used to study EGFR C797S-related functions .
    EGFR C797S Recombinant Human Active Protein Kinase
  • HY-E70707
    EGFR L858R Recombinant Human Active Protein Kinase

    		EGFR Cancer
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L858R Recombinant Human Active Protein Kinase is a recombinant EGFR L858R protein that can be used to study EGFR L858R-related functions .
    EGFR L858R Recombinant Human Active Protein Kinase
  • HY-E70708
    EGFR L861Q Recombinant Human Active Protein Kinase

    		EGFR Cancer
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L861Q Recombinant Human Active Protein Kinase is a recombinant EGFR L861Q protein that can be used to study EGFR L861Q-related functions .
    EGFR L861Q Recombinant Human Active Protein Kinase
  • HY-E70705
    EGFR G719S Recombinant Human Active Protein Kinase

    		EGFR Cancer
    EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR G719S Recombinant Human Active Protein Kinase is a recombinant EGFR G719S protein that can be used to study EGFR G719S-related functions .
    EGFR G719S Recombinant Human Active Protein Kinase

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