aml

Revumenib (SNDX-5613) is a potent and selective oral inhibitor of menin-KMT2A interaction with Ki of 0.149 nM and IC50 between 10 and 20 nM, which can be used in the study of acute leukemia with MLL gene rearrangement.

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

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.

Nrf2-IN-1 is an nuclear factor-erythroid 2-related factor 2 (Nrf2) inhibitor. Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML).

ML390 exerts its potent differentiation effect on multiple leukemia models.

Pipobroman (Vercyte) is an anti-cancer drug that probably acts as an alkylating agent. Pipobroman has well documented clinical activity in polycythemia vera (PV) and essential thrombocythemia (ET). Pipobroman allows, within 3 months, to attain a response in more than 90% of patients, without clinically relevant toxicities. The 10-years risk of thrombosis of patients treated with Pipobroman is about 15%, The anti-proliferative activity of Pipobroman on bone marrow megakaryocytes seems of particular value in lowering the occurrence of post-PV and post-ET MMM, whose risk is the lowest registered with available treatments. The 10-year risk of acute leukemia with Pipobroman is 5% in PVand 3% in ET, which is only slightly higher than that expected as a natural evolution of the disease. In conclusion, the use of Pipobroman is a definite alternative to hydroxyurea in patients with PV and ET at high risk of thrombosis.

GS87 is a highly specific inhibitor of GSK3 (glycogen synthase kinase 3) that induces extensive differentiation of AML cells.

Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) with antitumor activity, showing potential as a first-in-class candidate in AML [Acute Myeloid Leukemia].

Pulrodemstat benzenesulfonate (CC-90011 benzenesulfonate) is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity.

N-Desmethyltamoxifen hydrochloride is the primary metabolite of tamoxifen in humans.

Unesbulin (PTC596) is an orally active, selective inhibitor of B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1).

TL02-59 is a selective inhibitor of Fgr in Src-family kinase (IC50 = 0.03 nM). TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia cell growth.

UC-514321 directly targets STAT3/5 and represses TET1 expression. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.

CDKI-73 is a potent CDK9 inhibitor (Ki: 4 nM). It shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).The inhibition of CDK9 induces apoptosis and potentiates the effect of cisplatin.

Enocitabine is a nucleoside analog. Enocitabine inhibits the replication of human cytomegalovirus(HCMV) and it also has antileukemic and antiviral activities. Enocitabine is also a potent DNA replication inhibitor and a DNA chain terminator.

PNU-159682, a metabolite of anthracycline nemorubicin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity.

Ro 08-2750 is a non-peptide, reversible nerve growth factor (NGF) inhibitor that binds to NGF with an IC50 of approximately 1 µM. It is also a selective MSI RNA-binding activity inhibitor, exhibiting an IC50 of 2.7 μM. Additionally, Ro 08-2750 selectively inhibits NGF binding to p75NTR over TRKA.

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

AVN-944 (VX-944)(VX-944) is a selective, noncompetitive inhibitor of human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.

Piclamilast (RP 73401) is a PDE4 inhibitor.

G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.

GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.

BTSA1 is a BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.

IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain.