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.

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.

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.

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).

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.

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

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.

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.

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.

Tubulin polymerization-IN-43 is an inhibitor of tubulin polymerisation.Tubulin polymerization-IN-43 has multiple effects, disrupting the cellular microtubule network by targeting the colchicine locus and promoting cell cycle arrest and apoptosis in leukaemia cells. Tubulin polymerisation-IN-43 has multiple effects, promoting leukaemia cell cycle arrest in G2 M phase and apoptosis by targeting Colchicine sites to disrupt the cellular microtubule network.

Daunomycinone (NSC-109351) is a glycan of daunomycin, an antibiotic-class compound representing tumour-inhibiting anthracyclines, used in cancer and leukaemia treatment.

Rilmenidine hemifumarate (S-3341 hemifumarate) is a novel, orally active and selective I1 imidazoline receptor and α2-adrenoceptor agonist that induces autophagy, regulates the proliferation of leukaemia cells, stimulates the pro-apoptotic protein Bax, and induces autophagy in human leukaemia K5 cells. induces disruption of the mitochondrial pathway and apoptosis in human leukaemia K562 cells.

MAX-40279 hemifumarate is a potent dual inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemifumarate has shown investigational potential in acute myeloid leukaemia (AML).

MAX-40279 hemiadipate is a potent, dual FLT3 kinase and FGFR kinase inhibitor. MAX-40279 hemiadipate has shown investigational potential in acute myeloid leukaemia (AML).

XY153 (compound 8l) is a BD2-selective BET inhibitor that binds BRD4 BD2 with an IC50 of 0.79 nM, BRD3 BD2 with an IC50 of 5.31 nM, and BRD2 BD2 with an IC50 of 5.09 nM. XY153 is used to study acute myeloid leukaemia and cancer.

VEGFR-2-IN-26 (compound 5h) is a potent VEGFR-2 inhibitor (IC50: 15.5 nM) that exhibits significant anti-proliferative effects on leukemia, CNS, non-small lung, ovarian, renal, prostate, and breast cancer cells.

Purinostat mesylate is a selective HDAC inhibitor. purinostat mesylate inhibits type I and type IIb HDACs (IC50: 0.81-11.5 nM). purinostat mesylate affects the cell cycle of LAMA84 and 188 BL-2 cells and induces apoptosis, showing a strong anti-leukaemic effect in vivo. purinostat mesylate has been used to study lymphocytic leukaemia. Purinostat mesylate can be used to study lymphocytic leukaemia.

PI3K-IN-35 (Compound 6l) is a highly selective inhibitor of PI3K, targeting PI3K-α (IC50: 13.98 μM), PI3K-β (IC50: 7.22 μM), and PI3K-δ (IC50: 10.94 μM). It blocks the cell cycle in the G2 M phase and induces apoptosis, making it useful for studying leukemia.

Nelarabine (GW 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

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.