kasumi-1

Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

HSP70-IN-1 is a heat shock protein (HSP) inhibitor that suppresses the growth of Kasumi-1 cells with an IC50 of 2.3 μM.

Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), respectively.

2-Deoxy-D-glucose (2-DG) is an analog of glucose, an inhibitor of glycolysis. 2-Deoxy-D-glucose has antiviral activity, as well as inhibitory cell proliferation and apoptosis-inducing activity.

Pulrodemstat (CC-90011) is an orally active, selective, and highly efficient lysine-specific demethylase-1 (LSD1) inhibitor with anticancer activity. It inhibits HNSCC cell proliferation and migration by triggering apoptosis and inhibiting head and neck squamous cell carcinoma growth.

I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.

MG-T-19, a TIM-3 inhibitor (KD=0.26 μM), significantly inhibited the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9, and increased the production of TNF-α and IFN-γ in PBMCs, which reactivated the tumor-attacking ability of T cells.

LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 1.2 nM. It effectively inhibits the proliferation of cancer cells MV4-11, Kasumi-1, and NCI-H526 with IC50 values of 5, 4, and 11 nM, respectively. Furthermore, LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM and induces differentiation in MV4-11 cells. In mouse models, this compound demonstrates antitumor activity.

BAY-364 (BAY-299N) functions as an inhibitor targeting the second bromine domain in TAF1, demonstrating inhibitory effects on TAF1 in Kasumi-1 cells, CD34+ cells, and K562 cells with respective IC50 values of 1.0 µM, 10.4 µM, and 10.0 µM.

MGTA-117 is a humanized monoclonal antibody that targets CD117. It carries an amanitin payload and is used to synthesize antibody-drug conjugates (ADC). MGTA-117 demonstrates potent antitumor activity, enhancing survival in three acute myeloid leukemia (AML) xenograft models [Kasumi-1, AML PDX 1, and AML PDX 2]. It is applicable for AML, myelodysplastic syndromes with excess blasts (MDS-EB), and preconditioning for hematopoietic stem cell transplantation (HSCT) in gene therapy.