leukaemia

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.

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.

OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.

Evocarpine shows antimycobacterial, and vasorelaxant effects, it can inhibit Ca2+ influx through voltage-dependent calcium channels.

Senexin C is a novel orally active and specific CDK8/19 inhibitor with potential anticancer activity.Senexin C is more metabolically stable and potent than Senexin B. Senexin C inhibits the growth of MV4-11 leukaemia cells.

Vamotinib (PF-114) is an orally active and specific tyrosine kinase inhibitor with antiproliferative and antitumour activity.Vamotinib inhibits the phosphorylation of BCR ABL and BCR ABL-T315I, which promotes apoptosis. Vamotinib is used to study drug-resistant Philadelphia chromosome-positive (Ph+) leukaemia and Alzheimer's disease.

OTUB1 USP8-IN-1 HCL is a potent dual inhibitor of OTUB1 and USP8 with potential antitumour activity, inhibiting both OTUB1 and USP8. OTUB1 USP8-IN-1 may be used in the study of leukaemia.

IDH2R140Q-IN-2 is an orally active and potent IDH2R140Q inhibitor with an IC50 of 29 nM.IDH2R140Q-IN-2 possesses potential antitumour activity, reducing D2HG production in TF-1 cell lines carrying the IDH2R140Q mutation (IC50 of 10 nM) and inhibiting tumour tissue D2HG levels.IDH2R140Q-IN-2 is suitable for the study of acute myeloid leukaemia (AML).

Mitoxantrone dihydrochloride (NSC-301739) is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor.

Cyanoacetamide has inhibitory activity against the myeloid leukaemia cell differentiation protein Mcl-1 and is widely used in biochemical experiments and drug synthesis research.

Ethacrynic acid (Edecrin) is a nonsulfonamide loop diuretic that inhibits the activity of the Na+ K+ 2Cl- cotransporter NKCC2 in the thick ascending limb of the loop of Henle. It also inhibits glutathione S-transferase and Wnt signalling, producing cytotoxicity in chronic lymphocytic leukaemia cells and other tumour cells.

Cytosine (6-Aminopyrimidin-2(1H)-one) is a pyrimidine base that is a fundamental unit of nucleic acids. The deamination of cytosine alone is apparent and the nucleotide of cytosine is the prime mutagenic nucleotide in leukaemia and cancer.

5-Methylindole is a biologically active indole that inhibits a variety of kinases in bacteria and animals and Tryptophan synthase in plants for leukaemia and Alzheimer's disease.

(-)-Agelastatin A is a member of the pyrrole-aminoimidazole marine alkaloid (PAI) family, capable of inhibiting β-catenin, GSK-3β, and osteopontin (OPN), exhibiting antiproliferative activity against various cancers such as leukaemia and breast cancer, and possessing a certain ability to penetrate the central nervous system (CNS).

NCD38 is a selective LSD1 (lysine-specific demethylase 1) inhibitor that activates super-enhancers and myeloid cell development programmes, exhibiting anti-leukaemia activity.

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].

1. Chelidonine (Stylophorin) isolated from Chelidonium majus efficiently induced apoptosis in HeLa cells through possible alteration of p38-p53 and AKT PI3 kinase signalling pathways. 2. Chelidonine is a promising model compound for overcoming MDR and for enhancing cytotoxicity of chemotherapeutics, especially against leukaemia cells, its efficacy needs to be confirmed in animal models. 3. Chelidonine may be a potential therapeutic agent against metastasis of invasive human cancer cells, exhibits antimigratory and antiinvasive effects in MDA-MB-231 cells, by suppressing COL-induced integrin signaling, through inhibiting the formation of the IPP complex and subsequent downregulation of IPP downstream signaling molecules, such as Akt and ERK1 2.

Carboxyamidotriazole Orotate (L-651582 Orotate) is a cytostatic inhibitor of non-voltage-operated calcium channels and associated signaling pathways. As the orotate salt form of Carboxyamidotriazole (CAI), it is an orally bioavailable signal transduction inhibitor with in vitro antileukaemic activity, exhibiting anti-tumor, anti-inflammatory, and antiangiogenic effects.

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

Aclacinomycin A hydrochloride (Aclarubicin HCl) is an anthracycline antibiotic and inhibitor of topoisomerase I II, interfering with DNA transcription and replication, inhibiting tumour invasion and angiogenesis, generating reactive oxygen species (ROS), and inhibiting the catalytic centre of the 20S proteasome. It is indicated for the treatment of relapsed leukaemia and advanced malignant lymphoma.

OICR-0547 is an inactive derivative of OICR-9429 and is commonly used as a negative control for OICR-9429. OICR-9429 is an inhibitor of the interaction between WDR5 and the mixed leukaemia (MLL) protein.

SIAIS178 is a selective PROTAC degrader targeting BCR-ABL with an IC50 of 24 nM. It degrades BCR-ABL protein by recruiting the VHL E3 ubiquitin ligase, inhibiting leukaemia cell growth in vitro and causing regression of K562 xenograft tumours.

Daunorubicin is an anthracycline antibiotic and topoisomerase II inhibitor with anticancer activity, inhibiting DNA and RNA synthesis, and is commonly used to treat acute myeloid leukaemia (AML) and acute lymphoblastic leukaemia (ALL).

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.