antileukemic activity

KPT-251 is a selective nuclear export inhibitor.

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.

Anticancer agent 110 is an anticancer compound with cytotoxic, antitumor, and antileukemic activity that triggers DNA damage and apoptosis and is used in the study of chronic granulocytic leukemia.

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

RUNX1/ETO-IN-1 is an inhibitor targeting the oncogenic fusion protein RUNX1-ETO, specifically affecting the NHR2 oligomerization domain. It binds directly to NHR2 (KD,app = 39 μM). By inducing apoptosis and promoting differentiation, RUNX1/ETO-IN-1 exhibits antileukemic activity in RUNX1/ETO translocation acute myeloid leukemia (AML) cells. Its near-neutral charge under physiological pH conditions grants it excellent cell membrane permeability.

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].

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

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

Hisphen shows antileukemic activity.

Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.

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.

S-(N-PhenethylthiocarbaMoyl)-L-cysteine (PEITC-Cys) is an anticarcinogenic agent that exhibits antileukemic activity by inhibiting DNA synthesis in HL60 cells [1] and acts as an inhibitor of P450 [2].

AZD-1897 is a highly efficient ATP-competitive pan-PIM inhibitor with anticancer and antileukemic activity, inhibiting PIM1, PIM2, and PIM3, which can be used to study multiple myeloma.

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.

(+)SHIN2, an isomer of (-)SHIN2, is an inhibitor of serine hydroxymethyltransferase (SHMT) with antileukemic effects and shows synergistic activity with Methotrexate in in vivo xenotransplantation models [1].

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].

Triptonide (Standard) is a reference standard for research and analysis in studies involving Triptonide. 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.

Avarone ((+)-Avarone) is a sesquiterpene quinone that can be isolated from Dysidea avara. It exhibits cytotoxic properties and demonstrates antileukemic activity.

Microhelenin C has significant antileukemic activity.

Bruceantinoside A is a naturally occurring quassinoid glucoside belonging to the triterpenoid glycoside class, isolated from the fruits of Brucea genus species including Brucea javanica and Brucea antidysenterica. Bruceantinoside A exhibits antileukemic and cytotoxic activities and is employed as a bioactive research compound in cancer biology. Its complex structure and bioactivity make it valuable for mechanistic studies of natural product-derived anticancer agents.

Dehydrobruceantinol shows bitter taste and has antileukemic activity.

Eucannabinolide exhibits in vivo antileukemic activity.

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

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