myeloid leukemia

KPT-251 is a selective nuclear export inhibitor.

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

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

DD1 (HUN85111) is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.

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

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

AES-350 is a potent and orally active HDAC6 inhibitor (IC50 and Ki of 0.0244 μM and 0.035 μM, respectively), also exhibiting activity against HDAC-3, -8, and -11 in an enzymatic assay with IC50 values of 0.187 μM, 0.245 μM, and >1 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.

TL-895 is an ATP-competitive, and highly selective irreversible inhibitor of Bruton's Tyrosine Kinase(BTK). TL-895 showed good potency with an IC50 of 1.5 nM and a Ki of 11.9 nM.

MIK665 (S-64315) is a small-molecule inhibitor and a myeloid cell leukemia sequence 1 (MCL1) inhibitor (IC50 = 1.81 nM) with high selectivity and cell permeability. Used in experimental research, this compound exhibits antitumor activity in hematologic malignancies such as acute myeloid leukemia.

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.

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

S63845 is a selective myeloid leukemia 1(MCL1) inhibitor that binds to human MCL1 with a Kd of 0.19 nM.

H3B-8800 is a small-molecule inhibitor and an SF3B1-targeted inhibitor with oral bioactivity and cell permeability. This compound directly binds to the SF3b complex, exhibiting anticancer activity in transfusion-dependent myelodysplastic syndromes and SF3B1-mutant acute myeloid leukemia.

STM2457 is an inhibitor of the RNA methyltransferase METTL3 (IC50=16.9 nM) with selective and oral activity.STM2457 can be used in acute myeloid leukemia (AML) studies.

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.

DMAPT (Dimethylamino Parthenolide) is an orally active NF-κB inhibitor and a Parthenolide (PTL) analogue with an LD50 value of 1.7 μM for primary acute myeloid leukemia cells. It has potential anti-tumor and anti-metastatic effects.

Milademetan (DS-3032) is an orally active and potent MDM2 inhibitor with antitumor activity that induces G1 cell cycle arrest, senescence, and apoptosis.Milademetan is used in the study of acute myeloid leukemia and solid tumors.

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).

dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, binding to MCL1 with a KD of 30 nM and activating the apoptosis mechanism by degrading MCL1.

MRT199665 is an effective and ATP-competitive, selective MARK/SIK/AMPK inhibitor (IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively). MRT199665 suppresses the phosphorylation of S

MI-192 is a selective HDAC2 and HDAC3 inhibitor with IC50 values of 30 nM and 16 nM, respectively. It exhibits greater selectivity for HDAC2/3 over other HDAC isomers and induces apoptosis in myeloid leukemic cells, indicating potential therapeutic use in leukemia and as an anti-stroke agent [1] [2].

AGI-14100 is a novel and orally available mIDH1 inhibitor.AGI-14100 is used for the treatment of primary human myeloid leukemia.

F-14512 (free base) is a topoisomerase II inhibitor for the study of acute myeloid leukemia.