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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-118034
    MTBT

    		p38 MAPK Cancer
    MTBT is an anticancer agent and p38 activator with antiproliferative and apoptosis-inducing (apoptosis) activities. MTBT increases the phosphorylation of histone H3 serine in cancer cells, thereby arresting the cell cycle in the M phase. SB203580 (HY-10256), a specific inhibitor of p38 MAPK, abolished MTBT-induced cell cycle arrest .
    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-15217
    CHR-6494
    5+ Cited Publications

    		 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-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-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-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-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-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

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