myeloproliferative neoplasms

Bomedemstat ditosylate (IMG-7289 ditosylate) is an orally active lysine-specific demethylase 1 (LSD1) inhibitor with antitumor activity that potentiates the response to PD-1 inhibition in a homozygous model of SCLC, inhibits cancer cell proliferation, and induces apoptosis. Bomedemstat ditosylate can be used to study myeloproliferative neoplasms and myelofibrosis.

Flonoltinib (JAK2/FLT3-IN-1) is an orally active and potent JAK2/FLT3 inhibitor, inhibiting JAK2, FLT3, JAK1, and JAK3. Flonoltinib has anti-cancer activity and can be used for studying myeloproliferative neoplasms.

5MPN is an orally active and selective inhibitor of 6-phosphofructokinase-2-kinase (PFKFB4) that competitively inhibits the F6P binding site and inhibits the proliferation of myeloma cells, and can be used in the study of myeloproliferative neoplasms.

JAK2 JH2 binder-1 is a potent and selective JAK2 JH2 binder (Ki: 37.1 nM). JAK2 JH2 binder-1 has the potential to be used in the study of various myeloproliferative neoplasms.

BVB-808 is a selective Jak2 type 1 inhibitor. Janus kinases are critical components of signaling pathways that regulate hematopoiesis. Mutations of the non-receptor tyrosine kinase JAK2 are found in many BCR-ABL-negative myeloproliferative neoplasms. Preclinical results support that JAK2 inhibitors could show efficacy in treating chronic myeloproliferative neoplasms. JAK2 has also been postulated to play a role in BCR-ABL signal transduction. Therefore, inhibitors of JAK2 kinases are turning into therapeutic strategies for treatment of chronic myelogenous leukemia (CML).

ZT55, an orally active, highly-selective JAK2 inhibitor with an IC50 of 0.031 μM, inhibits proliferation of JAK2 V617F-expressing HEL cell lines, induces apoptosis and cycle arrest, and effectively inhibits HEL xenograft tumor growth in mice models. Suitable for studies on myeloproliferative neoplasms, polycythemia vera, and primary thrombocythemia, ZT55 offers promising applications.

Ropeginterferon alfa-2b (Ropeginterferon alfa-2b-njft), a monopegylated interferon-alpha (IFN-α), is used in the study of myeloproliferative neoplasms [1].

Compound A8, known as JAK2-IN-9, is a selective JAK2 inhibitor with an IC50 of 5 nM. It effectively inhibits the phosphorylation of JAK2, STAT3, and STAT5, possesses metabolic stabilities, and induces apoptosis. This compound is utilized in the study of myeloproliferative neoplasms (MPNs) [1].

Bomedemstat (IMG-7289), an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor, shows activity in mouse myeloproliferative neoplasm (MPN) models. This compound exhibits antineoplastic effects and can be used for acute myeloid leukemia (AML) and myelofibrosis (MF) research.