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Inhibitor Kit/Phosphat ASe_ Inhibitor _Cocktail_I

" in MedChemExpress (MCE) Product Catalog:

146

Inhibitors & Agonists

61

MCE Kits

3

Inhibitory Antibodies

1

Natural
Products

21

Recombinant Proteins

22

Isotope-Labeled Compounds

3

Antibodies

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-104068

    Histone Acetyltransferase Epigenetic Reader Domain Cancer
    Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 µM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 µM. Naphthol AS-E can be used for cancer research.
    Naphthol <em>AS-E</em>
  • HY-15240

    c-Kit c-Met/HGFR Cancer
    c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC50s of <200 nM.
    c-<em>Kit</em>-IN-1
  • HY-18302

    c-Kit Inflammation/Immunology
    c-Kit-IN-5 is potent inhibitor of c-Kit, with IC50s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit over KDR, p38, Lck, and Src. c-Kit-IN-5 also exhibits desirable pharmacokinetic properties .
    c-<em>Kit</em>-IN-5-1
  • HY-101034

    CHMFL-ABL-Kit-155

    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis .
    CHMFL-ABL/<em>KIT</em>-155
  • HY-128589

    c-Kit Cancer
    CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM .
    CHMFL-<em>KIT</em>-033
  • HY-128602

    c-Kit Cancer
    c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively .
    c-<em>Kit</em>-IN-2
  • HY-132451S

    Isotope-Labeled Compounds Others
    (R,S)-4-Hydroxy Cyclophosphamide-d4 Preparation Kit is the deuterium labeled (R,S)-4-Hydroxy Cyclophosphamide Preparation Kit[1].
    (R,S)-4-Hydroxy Cyclophosphamide-d4 Preparation <em>Kit</em>
  • HY-RS07319

    Small Interfering RNA (siRNA) Others

    KIT Human Pre-designed siRNA Set A contains three designed siRNAs for KIT gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    KIT Human Pre-designed siRNA Set A
    KIT Human Pre-designed siRNA Set A
  • HY-RS07320

    Small Interfering RNA (siRNA) Others

    Kit Mouse Pre-designed siRNA Set A contains three designed siRNAs for Kit gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Kit Mouse Pre-designed siRNA Set A
    Kit Mouse Pre-designed siRNA Set A
  • HY-RS07321

    Small Interfering RNA (siRNA) Others

    Kit Rat Pre-designed siRNA Set A contains three designed siRNAs for Kit gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Kit Rat Pre-designed siRNA Set A
    Kit Rat Pre-designed siRNA Set A
  • HY-KT001

    E3 Ligase Ligand-Linker Conjugates Cancer
    E3 Ligase Ligand-Linker Conjugate Kit is a series of synthesized compounds that incorporate an E3 ligase ligand and a linker used in PROTAC technology.
    E3 Ligase Ligand-Linker Conjugate <em>Kit</em>
  • HY-P99462

    CDX 0159

    c-Kit Inflammation/Immunology
    Barzolvolimab (CDX 0159) is a humanized anti-KIT IgG1 monoclonal antibody. Barzolvolimab specificity and potently inhibits KIT activation by SCF. Barzolvolimab can reduce skin mast cells and disease activity in chronic inducible urticaria .
    Barzolvolimab
  • HY-145557

    CGT9486; PLX 9486

    c-Kit Cancer
    Bezuclastinib (CGT9486) is an orally active, highly selective tyrosine kinase inhibitor with potent activity against KIT D816V. Bezuclastinib can be used for the research of nonadvanced systemic mastocytosis (NonAdvSM) .
    Bezuclastinib
  • HY-18317

    VEGFR RET c-Kit Cancer
    JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively .
    JNJ-38158471
  • HY-15198

    Raf PDGFR FLT3 c-Kit Cancer
    KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities .
    KG5
  • HY-103299
    KG-501
    10+ Cited Publications

    Naphthol AS-E Phosphate

    Epigenetic Reader Domain Inflammation/Immunology
    KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.
    KG-501
  • HY-N11690

    Na+/K+ ATPase Cardiovascular Disease Cancer
    Oleandrigenin is a potent cardiotonic steroid. Oleandrigenin shows Na +/K +-ATP-ase inhibiting and cytotoxic activities .
    Oleandrigenin
  • HY-139996

    PROTACs Ligands for E3 Ligase Cancer
    Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD + acute myeloid leukemia .
    Pomalidomide-C5-Dovitinib
  • HY-132166

    c-Kit Cancer
    M4205 is a c-KIT inhibitor, with an IC50 of 10 nM for c-KIT V654A. M4205 has high activity on c-KIT mutations in exon 11, 13, 17.
    M4205
  • HY-112802

    c-Kit Cancer
    AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. AZD3229 inhibits c-KIT with an IC50 value of 223.3 nM .
    AZD3229
  • HY-101443
    ISCK03
    2 Publications Verification

    c-Kit Inflammation/Immunology
    ISCK03 is a SCF/c-Kit and CD117-specific inhibitor. ISCK03 significantly inhibits c-Kit phosphorylation at 10 μM .
    ISCK03
  • HY-16961
    Sitravatinib
    1 Publications Verification

    MGCD516; MG-516

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib
  • HY-16961A

    MGCD516 malate; MG-516 malate

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib malate
  • HY-15652

    ONO-6818; ONO-PO-736

    Elastase Inflammation/Immunology
    Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
    Freselestat
  • HY-156619

    c-Kit Cancer
    Labuxtinib is c-kit tyrosine kinase inhibitor .
    Labuxtinib
  • HY-15652A

    ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate

    Elastase Inflammation/Immunology
    Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
    Freselestat quarterhydrate
  • HY-10873
    N-Desethyl Sunitinib
    5 Publications Verification

    SU-12662

    Drug Metabolite Cancer
    N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
    N-Desethyl Sunitinib
  • HY-138813
    N-Desethyl Sunitinib hydrochloride
    5 Publications Verification

    SU-12662 hydrochloride

    Drug Metabolite Cancer
    N-Desethyl Sunitinib (SU-12662) (hydrochloride) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
    N-Desethyl Sunitinib hydrochloride
  • HY-112452

    VEGFR FGFR PDGFR c-Kit Apoptosis Cancer
    SU11652 is a potent receptor tyrosine kinase (RTK) inhibitor. SU11652 also inhibits several members of the split kinase family of RTKs, including VEGFR, FGFR, PDGFR, and Kit. SU11652 can be uesd for spontaneous cancers expressing Kit mutations research .
    SU11652
  • HY-112802A

    c-Kit Cancer
    AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
    AZD3229 Tosylate
  • HY-13838

    c-Fms c-Kit Cancer
    PLX647 is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, respectively. PLX647 shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively) .
    PLX647
  • HY-10873S

    Isotope-Labeled Compounds Drug Metabolite Cancer
    N-Desethyl Sunitinib-d5 is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].
    N-Desethyl Sunitinib-d5
  • HY-13838A

    c-Fms c-Kit Inflammation/Immunology Cancer
    PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively) .
    PLX647 dihydrochloride
  • HY-50946
    Imatinib Mesylate
    65+ Cited Publications

    STI571 Mesylate; CGP-57148B Mesylate

    c-Kit Bcr-Abl PDGFR Autophagy Cancer
    Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
    Imatinib Mesylate
  • HY-112616

    NAMPT Drug-Linker Conjugates for ADC Cancer
    NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
    NAMPT inhibitor-linker 2
  • HY-G0017

    Norimatinib; Imatinib metabolite N-Desmethyl imatinib

    Drug Metabolite Others
    N-Desmethyl imatinib (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
    N-Desmethyl imatinib
  • HY-G0017A

    Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate

    Drug Metabolite Others
    N-Desmethyl imatinib mesylate (Norimatinib mesylate) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
    N-Desmethyl imatinib mesylate
  • HY-110071

    c-Kit Cancer
    APcK110 is a potent Kit inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis .
    APcK110
  • HY-112615

    Drug-Linker Conjugates for ADC Cancer
    NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
    NAMPT inhibitor-linker 1
  • HY-16749A
    Pexidartinib hydrochloride
    65+ Cited Publications

    PLX-3397 hydrochloride

    c-Fms c-Kit Apoptosis Cancer
    Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity .
    Pexidartinib hydrochloride
  • HY-10209
    Masitinib
    5 Publications Verification

    AB1010

    c-Kit PDGFR Src FGFR FAK Apoptosis Cancer
    Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .
    Masitinib
  • HY-10209A
    Masitinib mesylate
    5 Publications Verification

    AB-1010 mesylate

    c-Kit PDGFR Src FGFR Apoptosis Cancer
    Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity .
    Masitinib mesylate
  • HY-101561
    Avapritinib
    5 Publications Verification

    BLU-285

    c-Kit PDGFR Cancer
    Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib
  • HY-10501
    SU14813
    1 Publications Verification

    PDGFR VEGFR c-Kit Cancer
    SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
    SU14813
  • HY-10501A
    SU14813 maleate
    1 Publications Verification

    PDGFR VEGFR c-Kit Cancer
    SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
    SU14813 maleate
  • HY-16749
    Pexidartinib
    65+ Cited Publications

    PLX-3397

    c-Fms c-Kit Apoptosis Cancer
    Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity .
    Pexidartinib
  • HY-10527
    Telatinib
    1 Publications Verification

    Bay 57-9352

    c-Kit PDGFR VEGFR Cancer
    Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
    Telatinib
  • HY-10527C
    Telatinib mesylate
    1 Publications Verification

    Bay 57-9352 mesylate

    VEGFR PDGFR c-Kit Cancer
    Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively .
    Telatinib mesylate
  • HY-148794

    IkT-148009

    c-Met/HGFR Cancer
    Risvodetinib is a potent protein tyrosine kinase inhibitor. Risvodetinib involves in synthesis of Abelson protein kinases (c-Abl1, c-Abl2, and c-kit) inhibitor .
    Risvodetinib
  • HY-18179

    PDGFR VEGFR FLT3 c-Kit Cancer
    AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.
    AZD2932

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