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Results for "

selective,covalent

" in MedChemExpress (MCE) Product Catalog:

37

Inhibitors & Agonists

12

Peptides

1

Natural
Products

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111512
    PF-06795071

    		MAGL Neurological Disease Inflammation/Immunology
    PF-06795071 is a potent and selective covalent MAGL inhibitor with an IC50 of 3 nM .
    PF-06795071
  • HY-146223
    AZD4625

    		Ras Cancer
    AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
    AZD4625
  • HY-139881
    BTK inhibitor 19

    		Btk Cancer
    BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
    BTK inhibitor 19
  • HY-150298
    Soquelitinib

    CPI-818

    		 Itk Inflammation/Immunology Cancer
    Soquelitinib (CPI-818) is a highlyl selective covalent ITK inhibitor. Soquelitinib decreases DNA replication and cell cycle signaling .
    Soquelitinib
  • HY-158007
    (RS)-G12Di-1

    		Ras Cancer
    (RS)-G12Di-1 is a selective, covalent inhibitor of K-Ras-G12D .
    (RS)-G12Di-1
  • HY-123963
    C-178
    4 Publications Verification

    		 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 .
    C-178
  • HY-12833
    AMZ30
    1 Publications Verification

    		 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.
    AMZ30
  • HY-124700
    LYPLAL1-IN-1
    1 Publications Verification

    		 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 .
    LYPLAL1-IN-1
  • HY-142161
    ABD957
    1 Publications Verification

    		 MAGL Cancer
    ABD957 is a potent and selective covalent inhibitor of the ABHD17 family of depalmitoylases, with an IC50 of 0.21 µM for ABHD17B. ABD957 can block N-Ras signaling and the growth of NRAS-mutant AML cells .
    ABD957
  • 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 .
    FGFR4-IN-5
  • HY-19706
    ARS-853
    2 Publications Verification

    		 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 .
    ARS-853
  • HY-139361
    Sulfopin
    1 Publications Verification

    PIN1-3

    		 PIN1 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 .
    Sulfopin
  • HY-154854
    BBDDL2059

    		Histone Methyltransferase Cancer
    BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research .
    BBDDL2059
  • HY-P2203A
    SAHM1 TFA

    		Notch
    SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.
    SAHM1 TFA
  • HY-P2265
    SAH-SOS1A

    		Ras Cancer
    SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
    SAH-SOS1A
  • HY-P2265A
    SAH-SOS1A TFA

    		Ras Cancer
    SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
    SAH-SOS1A TFA
  • HY-P10212
    AVLX-125

    UCCB01-125

    		 iGluR Neurological Disease
    AVLX-125 (UCCB01-125) is a PSD-95 and PDZ domain inhibitor with Kd value of 10 nM. AVLX-125 can be used in the study of inflammatory pain .
    AVLX-125
  • HY-147515
    FGFR4-IN-11

    		FGFR Cancer
    FGFR4-IN-11 (Compound 30) is a potent, selective, covalent FGFR4 inhibitor with an IC50 of 2.1 nM. FGFR4-IN-11 significantly inhibits the FGF19/FGFR4 signaling pathway and shows antitumor activity .
    FGFR4-IN-11
  • HY-144733
    ERα antagonist 1

    		Estrogen Receptor/ERR Apoptosis Cancer
    ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
    ERα antagonist 1
  • HY-151523
    KRas G12R inhibitor 1

    		Ras Cancer
    KRas G12R inhibitor 1 (compound 3) is a KRas G12R selective covalent inhibitor that exploits the strong nucleophilicity of mutant cysteines and binds irreversibly in the Switch II region of K-Ras. KRas G12R inhibitor 1 can be used in cancer research .
    KRas G12R inhibitor 1
  • HY-155020
    Antitumor agent-101

    		Histone Methyltransferase GLP Receptor Cancer
    Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model .
    Antitumor agent-101
  • HY-P2261
    STAD 2

    		PKA Infection
    STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .
    STAD 2
  • HY-112161
    Branebrutinib
    1 Publications Verification

    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 . Branebrutinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Branebrutinib
  • 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 .
    MKK7-COV-9
  • HY-130149
    Adagrasib
    Maximum Cited Publications
    19 Publications Verification

    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 .
    Adagrasib
  • 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 .
    CDK12-IN-E9
  • HY-151968
    KRAS G12C inhibitor 57

    		Ras Cancer
    KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis .
    KRAS G12C inhibitor 57
  • HY-146223A
    (3R,10R,14aS)-AZD4625

    		Others Cancer
    (3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
    (3R,10R,14aS)-AZD4625
  • 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 .
    CBP/p300-IN-12
  • HY-142682
    SCP1-IN-1

    		Others Neurological Disease Cancer
    SCP1-IN-1 (compound SH T-62) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-1 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-1 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity .
    SCP1-IN-1
  • HY-142683
    SCP1-IN-2

    		Others Neurological Disease Cancer
    SCP1-IN-2 (Compound SH T-65) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-2 promotes REST degradation and reduces transcriptional activity. A high level of REST protein drives the tumor growth in some glioblastoma cells. SCP1-IN-2 has the potential for the research of glioblastoma whose growth is driven by REST transcription activity .
    SCP1-IN-2
  • HY-P2203
    SAHM1
    1 Publications Verification

    		 Notch Inflammation/Immunology
    SAHM1, a peptide mimetic of a dominant negative form of mastermind-like (MAML), inhibits canonical Notch transcription complex formation. SAHM1 can be used for the research of allergic airway inflammation in mice .
    SAHM1
  • HY-P1368
    Stressin I

    Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)

    		 CRFR Endocrinology
    Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) is a potent CRF1 receptor-selective agonist with a Ki of 1.7 nM. Stressin I induces increases in adrenocorticotropic hormone (ACTH) levels in rats .
    Stressin I
  • HY-P1368A
    Stressin I TFA

    Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41) TFA

    		 CRFR Endocrinology
    Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, Ki is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats .
    Stressin I TFA
  • HY-150022
    GRK5-IN-4

    CCG-265328

    		 G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research . GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GRK5-IN-4
  • HY-145836
    FGFR4-IN-8

    		FGFR Cancer
    FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
    FGFR4-IN-8
  • HY-P2266
    SAH-EZH2

    		Histone Methyltransferase Cancer
    SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .
    SAH-EZH2

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