ccrf-cem

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

cis-4-Br-2,5-F2-PCPA (S1024) inhibits LSD1 and LSD2 with Ki values of 94 nM and 8.4 μM, respectively. It inhibits LSD1 cell proliferation and increases dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells, particularly where there is aberrant expression of LSD1 in cancer stem cells [1].

KDM1 CDK1-IN-1 (compound 4) is a potent inhibitor of KDM1 (IC50: 0.096 μM) and CDK1 (IC50: 0.078 μM), blocking the cell cycle of HOP-92 cells in the G2 M phase and inducing apoptosis. It is highly cytotoxic to CCRF-CEM cells (IC50: 16.34 μM), HOP-92 cells (IC50: 3.45 μM), and Hep-G2 cells (IC50: 7.79 μM).

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

Arborinine shows mild in vitro antibacterial activity, it possesses moderate levels of anti-hepatitis C virus(HCV) activities with the IC50 values being 6.4 ± 0.7 ug/ml. Arborinine shows antifeedant activity against Spodoptera frugiperda. Arborinin shows

TAS-103 is a dual inhibitor of DNA topoisomerase I II, utilized in cancer research.

C24 dihydro Ceramide is a sphingolipid that has been found in the stratum corneum of human skin.[1] It is found in higher concentrations in female sebum compared to male sebum.[2] C24 dihydro Ceramide levels positively correlate with cytotoxicity in CCRF-CEM, MOLT-4, COG-LL-317h, and COG-LL-332h T cell acute lymphoblastic leukemia (ALL) cell lines.[4] Levels of C24 dihydro ceramide are increased by 149.49-fold in dihydroceramide desaturase 1 (DEGS1) knockdown UM-SCC-22A human head and neck squamous carcinoma cells in vitro.[4] C24 dihydro Ceramide levels are also increased in INS-1 β-cells incubated with glucose and palmitate.[5]

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

Antitumor agent-119 (compound 13K), a 2-benzoxazolyl hydrazone derivative, exhibits anticancer capabilities by impeding the proliferation of Burkitt, CCRF-CEM, HeLa, and HT-29 cells, with respective IC50 values of 30 nM, 140 nM, 100 nM, and 40 nM [1].

Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective topoisomerase II inhibitor that blocks the CCRF-CEM cell cycle in the G2 phase and induces DNA double-strand breaks (DSB). It exhibits antiproliferative activity on various tumor cell lines and has potential for cancer research [1].

Isoscopoletin (7-Methoxyesculetin) is a predicted metabolite generated by BioTransformer1 that is produced by the metabolism of 6, 7-dimethoxy-2h-chromen-2-one.

Anticancer agent 64 (compound 5m) exhibits potent cytotoxicity against CCRF-CEM cells with an IC50 value of 2.4 μM, induces apoptosis by activating caspase 3 and 7 and causing PARP cleavage, and significantly disrupts mitochondrial membrane potential, thereby contributing to its anticancer efficacy [1].