leukemic

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

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.

TCS-PIM-1-4a (SMI-4a), a Pim inhibitor, blocks mTORC1 activity through activation of AMPK and kills a wide range of both myeloid and lymphoid cell lines (IC50=0.8-40 μM).

Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist, used to treat hypertension.

Aminopterin (4-Aminofolic acid) is a synthetic folic acid derivative whose metabolite is a competitive inhibitor of dihydrofolate reductase

m-3M3FBS is a phospholipase C (PLC) activator.

Scoulerine is an inhibitor of ß-site amyloid precursor protein cleaving enzyme 1(BACE1). Scoulerine a potent antimitotic compound that inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.

Toddaculine may be beneficial for the prevention and treatment of osteoporosis, it can not only inhibit the differentiation of osteoclasts via activation of the NF-κB, ERK 1/2, and p38 MAPK signaling pathways, but can induce differentiation and mineralization of osteoblasts by regulating differentiation factors. Toddaculine also may serve as a pharmacological prototype for the development of novel anti-leukemic agents, it displays a dual effect as a cell differentiating agent and apoptosis inducer in U-937 cells.

Piribedil (Trivastan) is a dopamine D2 agonist, used in the treatment of Parkinson's disease.

ICCB280 was capable of inducing differentiation and apoptosis of ATRA-resistant patient blasts strongly signify that the activity of this compound can overcome resistance to other current therapies for AML with an unfavorable prognosis.

KPT-251 is a selective nuclear export inhibitor.

Coralyne chloride is a protoberberine with strong anticancer activity. It can be used to prepare Coralyne derivatives, a fluorescent DNA-based molecular rectifier built into DNA duplexes through site-specific insertion. It acts as a topoisomerase I toxic molecule, inducing topoisomerase I-mediated DNA cleavage.

ATH686 is an potent and selective Inhibitor of FLT3.

NL-1, a mitoNEET inhibitor, exhibits antileukemic effects.

nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a reversible inhibitor of arginase with anti-leukemic activity, effective in treating endothelial dysfunction, immunosuppression, and metabolism regulation.

BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.

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].

LeuRS-IN-1 is an orally active and potent Mycobacterium tuberculosis leucyl-tRNA synthetase inhibitor with anti-leukemic and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in leukemia research.

Dihydro-5-azacytidine (DHAC) is an active nucleoside analog with anti-leukemic activity that inhibits cell growth and induces DNA hypomethylation.Dihydro-5-azacytidine is used in the study of leukemia and tumors.

1,4-Anthraquinone is an anticancer drug that blocks nucleoside transport, inhibits macromolecule synthesis, induces DNA fragmentation, and decreases the growth and viability of L1210 leukemic cells in the same nanomolar range as daunorubicin in vitro.1,4-

LeuRS-IN-1 hydrochloride is an orally active and highly potent inhibitor of Mycobacterium tuberculosis leucyl-tRNA synthetase with anti-leukemic activity and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in the study of leukemia.

AKE-72 is a Pan-BCR-ABL inhibitor with anti-leukemic activity.AKE-72 inhibits the proliferation of Ba/F3 cells expressing natural BCR-ABL or its T315I mutant.

Forodesine hydrochloride (BCX-1777 hydrochloride), a potent inhibitor of human lymphocyte proliferation, effectively induces apoptosis in leukemic cells by elevating dGTP levels. This compound is an orally active, highly potent purine nucleoside phosphorylase (PNP) inhibitor, demonstrating IC50 values between 0.48 to 1.57 nM across human, mouse, rat, monkey, and dog PNP.

Eltanexor (ONO-7706) is an orally active exportin-1 (XPO1) inhibitor. It has effective anti-leukemic activity. Eltanexor inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor causes caspase-dependent apoptosis in a panel of leukemic cell lines.