promyelocytic

XMD8-92 is an effective and specific BMK1 ERK5 inhibitor (Kd: 80 nM).

Nordalbergin, a coumarin isolated from the bark of Dalbergia sissoo, significantly induces the differentiation of HL-60 cells.

Clofilium tosylate is a potassium channel blocker. It induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3.

Ginsenoside F5 is a natural product from Panax ginseng C. A. Mey, remarkably inhibits the growth of HL-60 cells by the apoptosis pathway

Aphidicolin, an antibiotic derived from the mold Cephalosporium aphidicola, is a potent inhibitor of DNA (deoxyribonucleic acid) synthesis, effectively hindering the proliferation of herpes simplex virus[2]. It targets DNA polymerase α and δ, disrupting mitotic cell division by affecting DNA polymerase activity[1]. Additionally, aphidicolin enhances apoptosis when combined with arabinosyl nucleosides in a human promyelocytic leukemia cell line[3].

Calcitriol Impurities D (24-Homo Calcitriol) is a hormonal form of the vitamin that promotes the differentiation of HL-60 human promyelocytic leukemia cells into monocytes.Calcitriol Impurities D has bone resorption activity and inhibits the replication of human immunodeficiency virus in human cells.Calcitriol Impurities D has antiviral activity and can be used to treat AIDS and viral infections. 25-dihydroxyvitamin D3 has antiviral activity and can be used in the treatment of AIDS and viral infections.

Colletochlorin B is a natural differentiation inducer of human promyelocytic leukemia cells.

GSK-3β inhibitor 3 is a potent, selective, and irreversible covalent inhibitor of glycogen synthase kinase 3β (GSK-3β) with an IC50 of 6.6 μM, and can be used to study acute promyelocytic leukemia.

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinaseJ. Med. Chem.50(9)2213-2224(2007) 2.Popescu, R., Heiss, E.H., Ferk, F., et al.Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cellsMutation Research709-71060-66(2011) 3.Moore, A.S., Blagg, J., Linardopoulos, S., et al.Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemiasLeukemia24(4)671-678(2010) 4.Wilkinson, R.W., Odedra, R., Heaton, S.P., et al.AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosisClin. Cancer. Res13(12)3682-3688(2007) 5.Yang, J., Ikezoe, T., Nishioka, C., et al.AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivoBlood110(6)2034-2040(2007)

O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin, formed from indomethacin in isolated rabbit hepatocytes. O-Desmethyl-N-deschlorobenzoyl indomethacin (600 μM) decreases the viability of HL-60 leukemia cells when cultured with glucose oxidase. It has also been used in the synthesis of prostaglandin D2 receptor antagonists.

HDAC3 inhibitor is an allosteric inhibitor of histone deacetylase 3 (HDAC3; Ki = 0.16 nM). It is selective for HDAC3 over HDAC1 and HDAC2 (IC50s = 0.95, 11.81, and 95.45 nM, respectively, using recombinant HDACs). In addition, it is selective for acute myeloid, monocytic, and lymphoblastic leukemia cell lines (EC50s = 36.37, 76.64, and 151.7 nM, respectively) over chronic myeloid, acute promyelocytic, and acute lymphoblastic cells (EC50s = 2,160, >10,000, and >10,000 nM, respectively).

Aspergillin PZ is a fungal metabolite originally isolated from A. awamori. It induces morphological deformation of P. oryzae conidia when used at a concentration of 89 nM. Aspergillin PZ is active against S. epidermidis (MIC = 20 μM) but not S. aureus, E. coli, or B. cereus (MICs = >20 μM). It is cytotoxic to HL-60 promyelocytic leukemia cells (IC50 = 56.61 μM) but not THP-1 acute monocytic leukemia or PC3 prostate cancer cells (IC50s = >80 μM).

1. Toosendanin possesses hepatotoxicity. 2. Toosendanin has effects on the growth, cell cycle arrest, induction of apoptosis and the involved signaling pathway in human promyelocytic leukemia HL-6 cells. 3. Toosendanin is an effective insecticide for Ae.

(-)-Syringaresinol (DL-Syringaresinol) is derived from the stems of Annona Montana. (-)-Syringaresinol inhibits the proliferation of human promyelocytic HL-60 cells through G1 arrest and induction of apoptosis and possesses anti-cancer activity.

Episyringaresinol 4'-O-β-D-glncopyranoside ((-)-Syringaresinol 4-O-β-D-glucopyranosi) inhibits the proliferation of human promyelocytic HL-6 cells through G(1) arrest and induction of apoptosis, and may be a potential chemotherapeutic agent for cancer treatment.

Yadanziolide C induces differentiation with cultured HL-60 promyelocytic leukemia cells.

Dehydrocrebanine has strong activity against promyelocytic leukemia cells (HL-60) with an IC50 of 2.14 ug mL. It also shows potent antimalarial activity with an IC50 value of 70 ng ml.

Desmethylrocaglamide is a novel inducer of cellular differentiation using HL-60 promyelocytic cells, it may be a drug for the prevention and therapy of cancer. It also has insecticidal activity.

(+)-Norglaucine shows cytotoxic activity toward the tumor cell lines B16-F10 (mouse melanoma), HepG2 (human hepatocellular carcinoma), K562 (human chronic myelocytic leukemia) and HL-60 (human promyelocytic leukemia) and non-tumor peripheral blood mononuc