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.

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

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1 2 4 6 (IC50=36 47 510 1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

Thapsigargin is a natural product, an inhibitor of sarcoplasmic endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

Ribociclib (LEE011) is an orally available, and highly specific CDK4 6 inhibitor (IC50:10 39 nM).

Tetracycline (Tetracyclin) is a broad-spectrum antibiotic with inhibitory activity against a wide range of Gram-positive and Gram-negative bacteria, as well as Mycoplasma, Mycoplasma, and Rickettsia. Tetracycline is commonly used in anti-infective studies.

Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.

Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM). Cytarabine inhibits DNA polymerase and induces cell cycle arrest, autophagy, and apoptosis. Cytarabine has antitumor activity.

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.

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.

PIM-1 CK2-IN-2 (compound 3aA) is an inhibitor of the PIM-1 CK2 enzymes. This compound can induce the mitochondrial apoptosis pathway in CCRF-CEM cells and is utilized in cancer research.

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].

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]

Lasioglossin-III, an antimicrobial peptide, is derived from the venom of wild bees. It exhibits significant antibacterial activity against both Gram-positive and Gram-negative bacteria, as well as antifungal and antitumor properties. Lasioglossin-III demonstrates cytotoxic effects on three cancer cell lines (HeLa S3, CRC SW 480, and CCRF-CEM T), with IC50 values of 4, 18, and 5 μM, respectively.

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].

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

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

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).

Dihydroevocarpine (1-methyl-2-tridecylquinolin-4-one) induces AML cytotoxicity, apoptosis and G0 G1 blockade, and inhibits tumor growth by inhibiting mTORC1 2 activity and the mTOR pathway in an acute myeloid leukemia (AML) xenograft model.

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].

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