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BTK<sup> C481S </sup> Ba/F3

" in MedChemExpress (MCE) Product Catalog:

1771

Inhibitors & Agonists

5

Screening Libraries

3

Fluorescent Dye

9

Biochemical Assay Reagents

25

Peptides

14

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34

Natural
Products

50

Recombinant Proteins

1276

Isotope-Labeled Compounds

42

Antibodies

13

Click Chemistry

51

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-E70134

    Endo F3

    Others Metabolic Disease
    Endo-β-N-acetylglucosaminidase D (Endo F3) cleaves free or Asparagine-linked triantennary oligosaccharides or α1-6 fucosylated biantennary oligosaccharides, as well as triamnnosyl chitobiose core structures .
    Endo-β-N-acetylglucosaminidase F3
  • HY-N0600

    Interleukin Related IFNAR Inflammation/Immunology
    Ginsenoside F3, a component of PPTGs (an minor saponin in the leaves of Panax ginseng), has immunoenhancing activity by regulating production and gene expression of type 1 cytokines (IL-2, IFN-gamma) and type 2 cytokines (IL-4 and IL-10) .
    Ginsenoside F3
  • HY-P99271

    Anti-Human F3 Recombinant Antibody

    ADC Antibody Cancer
    Tisotumab (Anti-Human F3 Recombinant Antibody) is a human IgG1 monoclonal antibody and ADC antibody. Tisotumab targets tissue factor (TF). Tisotumab can be used to synthesize antibody-drug conjugates (ADCs) targeting tissue factor (TF), Tisotumab vedotin (HY-152963). Tisotumab can be used for the research of solid tumors .
    Tisotumab
  • HY-P10997

    DNA/RNA Synthesis Cancer
    F3 peptide is a fragment of the human high mobility group protein 2 (HMGB2), and can specifically bind to nucleolin expressed on the membrane of cancer cells, neovasculature, and endothelium. F3 peptide can be used as an effective ligand to improve their druggability of macromolecular drugs or nanoparticles, and so on [3].
    F3 peptide
  • HY-147580

    Btk Cancer
    BTK-IN-10 is a potent BTK inhibitor with IC50s of <5 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022012509A1; example 111) .
    BTK-IN-10
  • HY-147582

    Btk Cancer
    BTK-IN-12 is a potent BTK inhibitor with IC50s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8) .
    BTK-IN-12
  • HY-RS23308

    Small Interfering RNA (siRNA) Others

    F3 Rat Pre-designed siRNA Set A contains three designed siRNAs for F3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    F3 Rat Pre-designed siRNA Set A
    F3 Rat Pre-designed siRNA Set A
  • HY-RS16867

    Small Interfering RNA (siRNA) Others

    F3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for F3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    F3 Mouse Pre-designed siRNA Set A
    F3 Mouse Pre-designed siRNA Set A
  • HY-RS04643

    Small Interfering RNA (siRNA) Others

    F3 Human Pre-designed siRNA Set A contains three designed siRNAs for F3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    F3 Human Pre-designed siRNA Set A
    F3 Human Pre-designed siRNA Set A
  • HY-153705

    Btk Cancer
    BTK-IN-25 (compound 71) is a potent inhibitor of BTK, and inhibits BTK(C481S) with an IC50 value of 0.77 nM. BTK-IN-25 inhibits BTK in DOHH2 cells with an IC50 value of 1 nM .
    BTK-IN-25
  • HY-153951S

    Btk Inflammation/Immunology Cancer
    BTK-IN-26 (compound 18) is a potent inhibitor of Bruton's tyrosine kinase (BTK) and its C481 mutant, with IC50 values of 0.7 and 0.8 nM for BTK and BTK C481S, respectively. BTK-IN-26 can be used for cancer and autoimmune diseases research .
    BTK-IN-26
  • HY-151211

    Btk Inflammation/Immunology Cancer
    BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC50s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia .
    BTK-IN-16
  • HY-P99271A

    Anti-Human F3 Recombinant Antibody (powder)

    ADC Antibody Cancer
    Tisotumab (Anti-Human F3 Recombinant Antibody) (powder) is a human IgG1 monoclonal antibody and ADC antibody. Tisotumab (powder) targets tissue factor (TF). Tisotumab (powder) can be used to synthesize antibody-drug conjugates (ADCs) targeting tissue factor (TF), Tisotumab vedotin (HY-152963). Tisotumab (powder) can be used for the research of solid tumors .
    Tisotumab (powder)
  • HY-176131

    Btk Inflammation/Immunology Cancer
    AMX5160 (36) is an orally active BTK inhibitor, with an IC50 of 0.98 nM against mutant BTK C481S. AMX5160 (36) can be used in the research for leukemia, lymphoma, multiple sclerosis, and other autoimmune diseases .
    AMX5160
  • HY-144170

    RET Btk Cancer
    RET-IN-14 (compound 49) is a potent RET inhibitor with IC50s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research
    RET-IN-14
  • HY-130983

    Btk Ligands for Target Protein for PROTAC Cancer
    N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively . N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM .
    N-piperidine Ibrutinib hydrochloride
  • HY-112215
    Nemtabrutinib
    4 Publications Verification

    ARQ-531; MK-1026

    Btk Inflammation/Immunology Cancer
    Nemtabrutinib (ARQ 531) 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-169228

    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-136531

    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 .
    XMU-MP-3
  • HY-W591307

    PROTAC Linkers Cancer
    P131 is a PROTAC molecule comprised of Pomalidomide-based cereblon ligand and IBT6A, linked by a PEG 3 chain. P131 can degrade both wild-type and C481S mutant BTK with nanomolar potencies.
    P131
  • HY-172479

    Liposome Cancer
    DSPE-PEG2000-F3 is a PEG compound which composed of DSPE and a nucleolin targeting peptide (F3). F3 peptide can specifically bind to cell surface nucleolin and undergo an effective cell surface to nucleus transport. DSPE-PEG2000-F3 can be used for drug delivery .
    DSPE-PEG2000-F3
  • HY-172479A

    Liposome Cancer
    DSPE-PEG3400-F3 is a PEG compound which composed of DSPE and a nucleolin targeting peptide (F3). F3 peptide can specifically bind to cell surface nucleolin and undergo an effective cell surface to nucleus transport. DSPE-PEG3400-F3 can be used for drug delivery .
    DSPE-PEG3400-F3
  • HY-172478

    Liposome Cancer
    DSPE-PEG1000-F3 is a PEG compound which composed of DSPE and a nucleolin targeting peptide (F3). F3 peptide can specifically bind to cell surface nucleolin and undergo an effective cell surface to nucleus transport. DSPE-PEG1000-F3 can be used for drug delivery .
    DSPE-PEG1000-F3
  • HY-172480

    Liposome Cancer
    DSPE-PEG5000-F3 is a PEG compound which composed of DSPE and a nucleolin targeting peptide (F3). F3 peptide can specifically bind to cell surface nucleolin and undergo an effective cell surface to nucleus transport. DSPE-PEG5000-F3 can be used for drug delivery .
    DSPE-PEG5000-F3
  • HY-174850

    Btk Cancer
    CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
    CFON-026
  • HY-160142

    PROTACs Btk Syk MEK ERK Cancer
    UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers .
    UBX-382
  • HY-12083

    Bcr-Abl Cancer
    PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba?F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML) .
    PPY-A
  • HY-175541

    PROTACs Btk Cancer
    TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)) .
    TQ-3959
  • HY-163366

    Trk Receptor Cancer
    TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC50 values of 0.55 nM, 25.1 nM and 5.4 nM against TRK WT, TRK G595R and TRK G667C, respectively. TRK-IN-2 shows antiproliferative activity with IC50 values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKA WT, Ba/F3-ETV6-TRKB WT, Ba/F3-LMNA-TRK G595R and Ba/F3-LMNA-TRKA G667C, respectively .
    TRK-IN-28
  • HY-176259

    PROTACs Galectin Apoptosis Cancer
    F3-PEG8-RiboTAC is a RiboTAC that can specifically degrade the mRNA of the oncogene LGALS1. F3-PEG8-RiboTAC can induce tumor cell apoptosis and inhibit invasion. F3-PEG8-RiboTAC has anti-tumor activity and can be used in the research of tumors such as leukemia and triple-negative breast cancer. (RNase L ligand (HY-177030); RNA binder (HY-177031); Linker (HY-W019798)) .
    F3-PEG8-RiboTAC
  • HY-174129

    Btk Apoptosis Cancer
    TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTK WT), >40,000 nM (BTK C481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis .
    TM471-1
  • HY-19834
    Fenebrutinib
    10+ Cited Publications

    GDC-0853

    Btk Cancer
    Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research .
    Fenebrutinib
  • HY-122562
    MT-802
    3 Publications Verification

    PROTACs Btk Cancer
    MT-802 is a BTK PROTAC degrader. MT-802 degrades wild-type BTK (DC50 = 14.6 nM) and BTK mutants including E41K, C481S (DC50 = 14.9 nM), C481R, C481Y, C481T, C481F, L528W, and inhibits their Y223 phosphorylation. BI-4732 can be used for the study of Ibrutinib (HY-10997)-resistant chronic lymphocytic leukemia (CLL). (Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-141371), E3 ligase ligand-linker conjugate (HY-176340)) .
    MT-802
  • HY-124153

    Btk Cardiovascular Disease Inflammation/Immunology
    GNE-431 is a potent, selective and noncovalent “pan-BTK inhibitor against C481R, T474I and T474Ms mutants. GNE-431 shows potency against wild-type BTK (IC50= 3.2 nM) and potency against C481S mutant (IC50= 2.5 nM). GNE-431 is proming for rasearch of haematological disorders and autoimmune diseases .
    GNE-431
  • HY-164397

    Anaplastic lymphoma kinase (ALK) Apoptosis Cancer
    XMU-MP-5 is a selective inhibitor for ALK. XMU-MP-5 inhibits ALK-mutated Ba/F3 cell with IC50s of 4-50 nM, and induces apoptosis in EML4-ALK Ba/F3. XMU-MP-5 exhibits antitumor efficacy in mice .
    XMU-MP-5
  • HY-170928

    EGFR Anaplastic lymphoma kinase (ALK) Cytochrome P450 Cancer
    DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .
    DA-0157
  • HY-P990411

    Transmembrane Glycoprotein Inflammation/Immunology
    Anti-F3/Factor III/Tissue Factor/CD142 Antibody is a CHO-expressed human antibody targeting F3/Factor III/Tissue Factor/CD142. The Anti-F3/Factor III/Tissue Factor/CD142 Antibody has a huIgG4SP type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-F3/Factor III/Tissue Factor/CD142 Antibody can be referred to as Human IgG4 kappa, Isotype Control (HY-P99003).
    Anti-F3/Factor III/Tissue Factor/CD142 Antibody
  • HY-162881

    EGFR Cancer
    DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI50 value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .
    DS06652923
  • HY-126920

    FLT3 Apoptosis Cancer
    AFG206 is a first-generation ATP competitive “type II” FLT3 inhibitor. AFG206 potently inhibits cell proliferation (IC50 around 0.1 µM) via induction of Apoptosis in FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells. AFG206 is promising for research of acute myeloid leukemia .
    AFG206
  • HY-18960
    CHZ868
    5+ Cited Publications

    JAK Cancer
    CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
    CHZ868
  • HY-175302

    Trk Receptor Apoptosis Cancer
    TRK-IN-32 is a potent TRK inhibitor. TRK-IN-32 potently inhibits TRK WT, TRK G595R and TRK G667C with IC50 values of 0.08 nM, 2.14 nM and 0.68 nM, respectively. TRK-IN-32 also demonstrates antiproliferative activity against a panel of Ba/F3 cell lines transformed with wild type, xDFG, solvent-front as well as gatekeeper mutant TRK fusion proteins. TRK-IN-32 induces apoptosis of Ba/F3-TRKA WT and Ba/F3-TRKA G667C cells.TRK-IN-32 can be used for the study of various cancers (such as thyroid cancer, secretory breast carcinoma) .
    TRK-IN-32
  • HY-174330A

    Trk Receptor Cancer
    TRK-IN-31 hydrochloride is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 hydrochloride has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 hydrochloride significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
    TRK-IN-31 hydrochloride
  • HY-174330

    Trk Receptor Cancer
    TRK-IN-31 is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
    TRK-IN-31
  • HY-153220

    PROTACs Btk Cancer
    NX-2127 (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells . (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383)
    NX-2127
  • HY-104010A
    Asciminib hydrochloride
    10+ Cited Publications

    ABL001 hydrochloride

    Bcr-Abl Cancer
    Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM .
    Asciminib hydrochloride
  • HY-104010
    Asciminib
    10+ Cited Publications

    ABL001

    Bcr-Abl Cancer
    Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM .
    Asciminib
  • HY-149965

    Trk Receptor Apoptosis Cancer
    TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKA G595R, TRKA F589L, and TRKA G667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells .
    TRK-IN-23
  • HY-163004

    Trk Receptor Cancer
    Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
    Type II TRK inhibitor 2
  • HY-159642

    FGFR Cancer
    TYRA-300 is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM in Ba/F3. TYRA-300 exhibits antitumor efficacy against urothelial cancers and solid tumors .
    TYRA-300
  • HY-W081348

    Prion Protein Transmembrane Glycoprotein Neurological Disease
    1-(4-Methoxyphenyl)-3-methyl-1H-pyrazol-5(4H)-one (Compound 2) has antiprion activity in ScN2a and F3 cells with IC50 values of 13 nM and 25 nM, respectively .
    1-(4-Methoxyphenyl)-3-methyl-1H-pyrazol-5(4H)-one

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