antileukemic

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

K00135 (IMIDAZOPYRIDAZIN 1) is a selective inhibitor of Pim kinases and can be used in studies about gastric cancer and antileukemic therapeutics.

Mezerein is a chemical compound with antileukemic properties and acts as a PKC activator. It effectively inhibits the growth of yeast expressing PKC alpha (IC 50 = 1190 nM), PKC beta1 (IC 50 = 908 nM), and PKC delta (IC 50 = 141 nM). However, it does not inhibit the growth of yeast expressing PKC.

Eucannabinolide exhibits in vivo antileukemic activity.

ZLD115 (compound 44), a derivative of FB23, functions as an inhibitor of the Fat Mass and Obesity-associated Protein (FTO) and demonstrates antiproliferative properties as an antileukemic agent against leukemic cell lines [1].

Dehydrobruceantinol shows bitter taste and has antileukemic activity.

Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential, and could be used to treat neurodegenerative diseases. Pinusolide attenuates blockade of insulin signaling by enhancing IRS-1 tyrosine phosphorylation by the activating the AMPK pathway, indicates the targeting of AMPK represents a new therapeutic strategy for hyperglycemia-induced insulin resistance and type 2 diabetes.

Stem bromelain (EC 3.4.22.32), a cysteine proteinase from pineapple (Ananas comosus) stem, is a significant type of bromelain known for its fibrinolytic, antiedematous, antithrombotic, and anti-inflammatory properties. It also demonstrates in vivo antitumoral, antileukemic, and antimetastatic activities [1] [2].

Caspase-3 activator 3 (compound 2h) effectively induces apoptosis in HL-60 and K562 cells by substantially activating caspase-3, demonstrating antileukemic activity with IC50 values of 42.89 μM and 33.61 μM, respectively [1].

Yadanzioside P has antileukemic and antitumor activities.

Tagitinin F possesses antileukemic activity; it also shows in vitro leishmanicidal activities against Leishmania braziliensis promastigotes and amastigotes.

Bruceantinoside A has antileukemic activity.

Botryodiplodin, an antibiotic, has antileukemic activity from Botryodiplodia theobromae. It has the property of turning the skin of the individual in various shades of pink 2-3 hrs after application. It is a toxic metabolite of Penicillium carneo-lutescen

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.

S-(N-PhenethylthiocarbaMoyl)-L-cysteine (PEITC-Cys) is an anticarcinogenic agent. S-(N-PhenethylthiocarbaMoyl)-L-cysteine shows antileukemic activity which inhibits DNA synthesis in HL60 cells [1]. S-(N-PhenethylthiocarbaMoyl)-L-cysteine is an inhibitor of P450 [2].

HDAC-IN-49 is a potent, non-selective inhibitor of HDAC (HDAC), demonstrating IC50 values of 13 nM for HDAC1, 14 nM for HDAC2, 21 nM for HDAC3, 1880 nM for HDAC4, and 10 nM for HDAC6. This compound exhibits significant antileukemic activity while maintaining low cytotoxicity towards healthy cells.

Yadanzioside G has antileukemic activity.

ATH686 is an potent and selective Inhibitor of FLT3.

Yadanzioside C has antileukemic activity.

UM729, a novel pyrimidoindole, exhibits an additive effect with AhR antagonists to inhibit differentiation in the majority of AML specimens and works synergistically with Ahr suppressors to hinder AML cell differentiation. It, along with SR1, can serve as a standardized additive in culture media, facilitating research into self-renewal mechanisms and the discovery of new antileukemic drugs via cell-based assays for primary human AML cells.

Microhelenin C has significant antileukemic activity.

(+)-Nortrachelogenin is a lignan isolated from Wikstroemia indica C.A. Meyer (Thymelaeaceae). (+)-Nortrachelogenin possesses antileukemic activity.

Moflomycin is an anthracycline derivative. It exhibits a higher antileukemic activity compared to other anthracyclines.

GCN2iB is a GCN2 inhibitor. GCN2iB may be useful for the treatment of cancer. The inhibition of GCN2 sensitizes cancer cells with low basal-level expression of asparagine synthetase (ASNS) to the antileukemic agent L-asparaginase (ASNase) in vitro and in vivo.

Idarubicin, a potent anthracycline antileukemic agent, is orally active in its application. It functions by inhibiting topoisomerase II, thus interfering with DNA replication and RNA transcription. Furthermore, Idarubicin induces DNA damage, inhibits DNA synthesis, and suppresses c-myc expression. It also demonstrates inhibitory effects on the growth of bacteria and yeasts [1] [2] [3] [4] [5].

Gilteritinib-d8 is a deuterated compound of Gilteritinib. Gilteritinib has a CAS number of 1254053-43-4. Gilteritinib is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preClinicalal studies, gilteritinib showed strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 Clinicalal trials for acute myeloid leukemia.

PD166326, a pyridopyrimidine-type inhibitor of receptor tyrosine kinases, demonstrates antileukemic activity with IC50 values of 6 nM for Src and 8 nM for Abl. [1] [2].

Yadanzioside A has antileukemic activity.

Deacetyleupaserrin is an antileukemic sesquiterpene lactone.

Yadanzioside F has antileukemic activity.

STAT5-IN-2 is an inhibitor of STAT5 with antileukemic effects (EC50s: 9 μM and 5 μM in K562 and KU812 cells, respectively).

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.

KPT-251 is a selective nuclear export inhibitor.

(-)SHIN2 is the isomer of (+)SHIN2 . (+)SHIN2 is an inhibitor of serine hydroxymethyltransferase (SHMT) with antileukemic effect. (+)SHIN2 synergisty with and Methotrexate in vivo xenotransplantation models [1] .

Hisphen shows antileukemic activity.

5,10-Dideazaaminopterin is an antileukemic drug.

NL-1 is a mitoNEET inhibitor with antileukemic effect.

Hepsulfam is an anticancer agent. It also displays excellent antileukemic activity (a median IC50: 0.91 μg/mL in a panel of different tumors).

1. Triptonide (PG 492) is effective in the treatment of autoimmune diseases and has potent antileukemic and antitumor activities. 2. Triptonide possesses anti-inflammatory activity, upregulate the expression of IL-37, and this expression was suppressed by ERK1/2 and p38 MAPK inhibitors.

5,10-Dideazafolic acid is an antileukemic drug.

Gilteritinib hemifumarate (ASP2215 hemifumarate) is a potent ATP-competitive dual FLT3 (IC50: 0.29 nM) and AXL (IC50: 0.73 nM) inhibitor for the treatment of relapsed or refractory FLT3 mutant AML.