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histone H3 phosphorylation

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15217
    CHR-6494
    Maximum Cited Publications
    8 Publications Verification

    		 Haspin Kinase Cancer
    CHR-6494 is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer .
    CHR-6494
  • HY-141539
    SETDB1-TTD-IN-1
    5 Publications Verification

    		 Histone Methyltransferase Akt Cancer
    SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (Kd of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer .
    SETDB1-TTD-IN-1
  • HY-16018A
    Ilorasertib hydrochloride

    ABT-348 hydrochloride

    		 Aurora Kinase PDGFR VEGFR Cancer
    Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
    Ilorasertib hydrochloride
  • HY-16018
    Ilorasertib

    ABT-348

    		 Aurora Kinase VEGFR PDGFR Cancer
    Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
    Ilorasertib
  • HY-118034
    MTBT
    1 Publications Verification

    		 p38 MAPK Apoptosis Cancer
    MTBT is an anticancer agent and p38 MAPK activator. MTBT can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. MTBT increases the phosphorylation of histone H3 serine in cancer cells, thereby arresting the cell cycle in the M phase. The specific inhibitor of p38 MAPK, Adezmapimod (HY-10256), can abrogate the cell cycle arrest induced by MTBT .
    MTBT
  • HY-126249
    AAPK-25

    		Aurora Kinase Polo-like Kinase (PLK) Apoptosis Cancer
    AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM .
    AAPK-25
  • HY-110350
    CHR-6494 TFA

    		Haspin Kinase Cancer
    CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer .
    CHR-6494 TFA
  • HY-125090
    PHA-680626

    		Aurora Kinase c-Myc Bcr-Abl Histone Methyltransferase Apoptosis Cancer
    PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells .
    PHA-680626
  • HY-178485
    SJY26

    		PI3K HDAC Akt Histone Methyltransferase Cancer
    SJY26 is a PI3K/HDAC dual-target inhibitor with IC50s of 0.59 nM (PI3Kα and PI3Kδ), 2.02 nM (PI3Kγ), 12.69 nM (PI3Kβ) and 114 nM (HDAC1). SJY26 exhibits potent broad-spectrum anti-proliferative activity, and is particularly sensitive to Jurkat and PC9R cells. SJY26 inhibited the migration of PC9R cells, arrested the cell cycle and induced cell apoptosis. SJY26 reduces AKT phosphorylation, and decreases histone H3 deacetylation (Ac-H3). SJY26 can be used for the studies of non-small cell lung cancer and leukemia .
    SJY26
  • HY-117688
    WJ35435

    		HDAC Topoisomerase Apoptosis Cancer
    WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer .
    WJ35435
  • HY-125158
    HOI-07

    		Aurora Kinase Apoptosis Cancer
    HOI-07 is a selective Aurora B kinase inhibitor. HOI-07 blocks phosphorylation of histone H3 on Ser10 in lung cancer cells. HOI-07 induces cell-cycle arrest, and apoptosis. HOI-07 has antitumor activity, and suppresses the tumor growth of A549, 143B and KHOS xenografts .
    HOI-07
  • HY-156091
    PI3Kα/HDAC6-IN-1

    		PI3K HDAC Cancer
    PI3Kα/HDAC6-IN-1 (compound 21j) is a dual PI3Kα/HDAC6 inhibitor with IC50 of 2.9 and 26 nM, respectively. PI3Kα/HDAC6-IN-1 also inhibits AKT(Ser473) phosphorylation and induces the accumulation of acetylated α-tubulin without affecting acetylated histones H3 and H4. PI3Kα/HDAC6-IN-1 efficiently inhibits L-363 cell line (IC50=0.17 μM) and has good anti-cancer activity .
    PI3Kα/HDAC6-IN-1
  • HY-182720
    FT108

    		HDAC Microtubule/Tubulin Cancer
    FT108 is a selective HDAC6 inhibitor with an IC50 of 0.026 μM. FT108 exhibits only modest in vitro activity against HDAC3 and HDAC8 with IC50 values of 6.68 and 4.07 μM. FT108 increases acetylation of tubulin and has little to no effect on acetylated histone H3 levels. FT108 lacks activity against myeloproliferative neoplasm cell lines, and does not suppress JAK2 phosphorylation or its downstream targets pSTAT3 and pSTAT5 .
    FT108
  • HY-179374
    Aurora kinase/HDAC-IN-1

    		Aurora Kinase HDAC Apoptosis Cancer
    Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model .
    Aurora kinase/HDAC-IN-1

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