HL60

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

Tectol has anti-plasmodial activity, it as a moderately active growth inhibitor with an IC50 3.44±0.20μM. It exhibited significant activity against human leukemia cell lines HL60 and CEM. Tectol may cause itchy dermatitis, the dermatitis appeared on the n

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM 78.7 nM 197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2 PLK3 (IC50s: 5 56 nM).

Evocarpine shows antimycobacterial, and vasorelaxant effects, it can inhibit Ca2+ influx through voltage-dependent calcium channels.

Mitoxantrone dihydrochloride (NSC-301739) is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor.

Novobiocin Sodium (Albamycinsodium) binds to DNA gyrase and blocks adenosine triphosphatase (ATPase) activity. Novobiocin sodium is an antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin.

Phloretin (NSC-407292) is a well-known inhibitor of eukaryotic urea transporters, blocks VacA-mediated urea and ion transport. Phloretin is a dihydrochalcone, a type of natural phenols. It can be found in apple tree leaves and the Manchurian apricot. It promotes potent antioxidative activities in peroxynitrite scavenging and the inhibition of lipid peroxidation. It has been found to inhibit the growth of several cancer cells and induce apoptosis of B16 melanoma and HL60 human leukemia cells.

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.

Ch55 (3,5-Di-tert-butylchalcone) is an effective inducer of the differentiation of HL60 cells (EC50 = 200 nM) and shows high affinity with RAR-α and RAR-β receptors. Ch55 can be used in studies about cancer.

Pellitorine (Pellitorin) is an extract of Tetradium daniellii, and acts as a TRPV1 antagonist.

Sophoraflavanone G (Kushenol F) (Kushenol F), isolated from Sophora flavescens, induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways.

DC1 is an ADC cytotoxin, similar to the small groove-binding DNA alkylating agent CC-1065. DC1 can be used to synthesize antibody-drug conjugates targeted to the treatment of cancer. DC1Sme is a DC1 derivative with IC50 values of Ramos, Namalwa, HL60 s

DC10SMe is a DNA alkylating agent that can be used in the synthesis of antibody-drug conjugates (ADC). The IC50 of DC10SMe for Ramos, Namalwa and HL60 s cancer cells were 15 pM, 12 pM and 12 pM, respectively.

DC41SMe is a DC1 derivative that is cytotoxic to Ramos, Namalwa and HL60 s with IC50s ranging from 18-25 pM. DC1 is a simplified analogue of CC-1065, an antibody conjugate of cytotoxic DNA alkylation molecules, used for targeted treatment of cancer.

The IC50 of DC44SMe for Ramos, Namalwa and HL60 s cancer cells was 2.0 nM, 2.8 nM and 1.9 nM, respectively. DC44SMe can be used for targeted treatment of cancer. DC44SMe is a phosphate prodrug of DC44 and can be used in the synthesis of antibody-drug co

The IC50s of DC4SMe on Ramos, Namalwa and HL60 s cancer cells were 1.9 nM, 2.9 nM and 1.8 nM, respectively. DC4SMe can be used for targeted therapy of tumors. DC4SMe is a phosphate prodrug of the cytotoxic DNA alkylating agent DC4 and can be used in the

RWJ 50271 is a selective lymphocyte function-associated antigen-1 intercellular adhesion molecule-1(LFA-1 ICAM-1) interaction inhibitor( IC50 of 5.0 μM in HL60 cells).

SGD-1882 (PBD dimer) is a cytotoxic conjugate that is a target for mouse and human hematopoietic stem cells (HSC) and acute myeloid leukemia cells.

HDAC-IN-79 (compound 4) is an orally active dual inhibitor of xanthine oxidase and HDAC, exhibiting potent anti-hyperuricemia and antitumor activities in vivo (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM). Among leukemia cells, it is most effective in inhibiting the growth of HL60 cells (IC50=0.706 μM) and induces both apoptosis and autophagy. HDAC-IN-79 also modulates the expression levels of biomarkers associated with intracellular HDAC inhibition.

4-Iodo-SAHA (1k), an orally active inhibitor of both class I and class II histone deacetylase (HDAC), exhibits EC50 values of 1.1, 0.95, 0.12, 0.24, 0.85, and 1.3 μM for Skbr3, HT29, U937, JA16, and HL60 cell lines, respectively. This compound holds potential for cancer research purposes [1].

6-Hydroxycoumarin (6-hydroxychromen-2-one) exhibits cytotoxicity against human HL60, HCT116, COLO205 cells with activity value of 35 uM, 42 uM, 37 respectively. 6-Hydroxycoumarin is a human CA9, CA12 inhibitor.

CAY10503 is a proapoptotic, antiproliferative compound that is able to arrest cell cycle progression in the G0-G1 phase. CAY10503 inhibits the growth of HL60, multidrug resistant HL60R, and K562 cells with IC50 values of 7.0, 23, and 20 μM, respectively. Accumulation of HL60 cells in G0-G1 occurred within eight hours following treatment with 50 μM CAY10503, whereas 10 μM CAY10503 required 96 hours for cell cycle arrest to appear. CAY10503 also induces differentiation of HL60 cells into the following positive cells: CD14 (monocytic marker) as well as CD11b and CD11c (granulocytic markers). Approximately 60% of HL60 cells exposed to 10 μM CAY10503 expressed these markers within 72 hours.

Gracillin can induce cell cycle arrest, oxidative stress, and apoptosis in HL60 cells, and has the potential to be developed as an antitumor agent. Gracillin can be selected as lead compounds for the development of new drugs against I. multifiliis.