u937

ML390 exerts its potent differentiation effect on multiple leukemia models.

Meisoindigo (Natura-α) is a derivative of indigo natural, might induces apoptosis and myeloid differentiation of acute myeloid leukemia (AML).

6-OAU (GTPL5846)(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.

NIBR189 is a potent and selective antagonist of EBI2 (GPR183) receptor (IC50 of 11 and 15 nM for human and mouse EBI2 receptors, respectively)

m-3M3FBS is a phospholipase C (PLC) activator.

AI-10-47 (1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47) is a small molecule inhibitor of CBFβ-RUNX binding(IC50 : 3.2 μM).

Periplocymarin is a cardiac glycoside with anticancer potential isolated from Periploca sepium and Periploca graeca.

Bindarit (AF2838)is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

RIPK1-IN-9 is a potent and selective inhibitor of RIPK1, a dihydronaphthone compound, which inhibits U937 and L929 cells with an IC50 of 2 nM and 1.3 nM, respectively.

Eicosapentaenoic Acid is an ω-3 fatty acid and an inhibitor of fatty acid synthase (FASN). Eicosapentaenoic Acid promotes DNA demethylation in the reexpression of the tumor suppressor gene CCAAT/ enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates the RAS/ERK/C/EBPβ pathway in U937 leukemia cells through demethylation of the CpG island of H-RAS intron 1. Eicosapentaenoic Acid promotes the relaxation of vascular smooth muscle cells and vasodilation.

Apoptosis Inhibitor was a novel inhibitor of programmed cell death associate with caspase-3 inhibition.

1alpha-Hydroxy VD4 can effectively induce the differentiation of monoblastic leukaemia U937, P39/TSU, and P31/FUJ cells.

ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. It positively modulates murine DCs, induces NSC proliferation, and constitutes a promising therapeutic agent for various neurologic disorders[4][5]. It also activates apoptotic proteins in human lymphoma U937 cells[3].

TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM), blocking ubiquitin binding and disrupting both mono-ubiquitin signaling and overall protein ubiquitination. TAK-243 exhibits antitumor activity and promotes apoptosis.

Verlukast is an (R)-enantiomer of MK-571 and a potent and selective LTD4 receptor antagonist. Verlukast showed [3H]leukotriene D4 binding in guinea-pig (IC50 = 3.1 +/- 0.5 nM) and human (IC50 = 8.0 +/- 3.0 nM) lung homogenates and dimethyl sulfoxide diffe

YL-5092 is an inhibitor of YT521-B homology (YTH) domain-containing protein 1 (YTHDC1). It inhibits acute myeloid leukemia cells with an IC50 of 0.28-2.87 μM. YL-5092 exhibits antitumor activity in xenograft mice models using MOLM-13 or U937 cells.

CK2-IN-14 (Compound 10b) is an inhibitor of cyclin-dependent kinase 2α with an IC50 of 36.7 nM. It effectively hinders the growth of cancer cell lines 786-O and U937, with GI50 values of 7.3 μM and 7.5 μM, respectively.

(Rac)-Nanatinostat ((Rac)-CHR-3996, example 44) is a potent HDAC inhibitor with an IC50 of less than 330 nM. It exhibits anticancer properties, effectively inhibiting the growth of HeLa, U937, and HUT cells.

H052 is a selective inhibitor of Staphylococcus aureus α-hemolysin (Hla). It binds to the Hla monomer, disrupting its interaction with the host cell membrane, thereby blocking pore formation and inhibiting calcium influx, cytotoxicity, and inflammatory response. H052 exhibits inhibitory activity against Hla-induced calcium influx (EC50 = 30 nM in U937 cells) and holds potential for research into lung infections caused by S. aureus.

HDAC11-IN-3 (Compound A9) is a selective inhibitor of HDAC11, exhibiting an IC50 value of 4.1 nM. It demonstrates inhibitory effects on U937 and OCI-AML2 acute myeloid leukemia (AML) cell lines with an IC50 of 10 μM. This compound shows significant anti-AML activity by inducing apoptosis, cell cycle arrest, and differentiation. HDAC11-IN-3 upregulates the iron transport proteins transferrin (TF) and transferrin receptor (TFRC), and activates the p62-Keap1-Nrf2-HMOX1 pathway, which collectively increases intracellular iron levels and induces ferroptosis in AML cells. HDAC11-IN-3 can be utilized for AML research either alone or in combination with Cytarabine.

RIPK1-IN-13 (compound 28) is a selective inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1), showing a pKi of 7.66 as measured by the ADP-Glo kinase assay. It exhibits inhibitory effects in human leukemia U937 cells with a pIC50 of 7.2.

Leuxinostat, an inhibitor of HDAC, exhibits an IC50 of 30 nM against hHDAC6. It suppresses the proliferation of THP1, K562, U937, and MEK1 cells, while also inducing apoptosis in leukemia cells NB4 and MOLT-4. Additionally, Leuxinostat inhibits the expansion of hematopoietic stem cells and demonstrates anti-leukemic activity in a zebrafish model.

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].