ccrf-cem

Pheniramine maleate (Trimetose) 是一种具有抗组胺和血管扩张特性的烷基胺衍生物，可与组胺 H1 受体结合，从而抑制磷脂酶 A2 和内皮源性松弛因子一氧化氮的产生。

cis-4-Br-2,5-F2-PCPA (S1024) 抑制 LSD1 和 LSD2，Ki 值分别为 94 nM 和 8.4 μM。癌症干细胞中 LSD1异常表达，cis-4-Br-2,5-F2-PCPA 能够通过增加 CCRF-CEM 细胞中二甲基化组蛋白 H3 的 K4 (H3K4) 水平，抑制 LSD1活性和癌细胞增殖。

KDM1 CDK1-IN-1 (compound 4) 是一种有效的 KDM1 (IC50: 0.096 μM) 和 CDK1 (IC50: 0.078 μM) 抑制剂。KDM1 CDK1-IN-1 能够将 HOP-92 细胞的细胞周期阻滞在 G2 M 期，并诱导其凋亡 (apoptosis)。KDM1 CDK1-IN-1 对 CCRF-CEM 细胞 (IC50: 16.34 μM)、HOP-92 细胞 (IC50: 3.45 μM) 和 Hep-G2 细胞 (IC50: 7.79 μM) 具有较强的细胞毒性。

TAS-103 is a dual inhibitor of DNA topoisomerase I II, used for cancer research. TAS-103 is a dual inhibitor of DNA topoisomerase I II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells[1]. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103[2]. TAS-103 inhibits the viability of HeLa cells, with an IC50 of 40 nM. TAS-103 (10 μM) disrupts signal recognition particle (SRP) complex formation, and induces destabilization of SRP14 and SRP19 and its eventual degradation[3]. TAS-103 (30 mg kg, i.v.) causes significant tumor growth suppression in mice bearing Lewis lung carcinoma (LLC) cells, without obvious body weight loss, and the liposomal TAS-103 is more active than free TAS-103[2]. [1]. Padget K, et al. An investigation into the formation of N- [2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and 6-[2-(dimethylamino)ethylamino]- 3-hydroxy-7H-indeno[2, 1-C]quinolin-7-one dihydrochloride (TAS-103) stabilised DNA topoisomerase I and II cleavable complexes in human leukaemia cells. Biochem Pharmacol. 2000 Sep 15;60(6):817-21. [2]. Shimizu K, et al. Cancer chemotherapy by liposomal 6-[12-(dimethylamino)ethyl]aminol-3-hydroxy-7H-indeno[2,1-clquinolin-7-one dihydrochloride (TAS-103), a novel anti-cancer agent. Biol Pharm Bull. 2002 Oct;25(10):1385-7. [3]. Yoshida M, et al. A new mechanism of 6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one dihydrochloride (TAS-103) action discovered by target screening with drug-immobilized affinity beads. Mol Pharmacol. 2008 Mar;73(3):987-94. Epub 2007 Dec 18.

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

Sertindole (Lu 23-174) 是一种非典型抗精神病药，可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合，Kd 值分别为 2.7、20、0.14 和 6 nM。

Antitumor agent-119（化合物13K）为2-苯并恶唑基腙衍生物，显示抗癌活性。该化合物对Butkitt、CCRF-CEM、HeLa和HT-29细胞系展现出细胞生长抑制作用，其IC50值分别为30 nM、140 nM、100 nM和40 nM。

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) 是一种P-糖蛋白抑制剂，Ki 值为 59 nM。

Topoisomerase II inhibitor 6 (Compound 5) 是色胺酮的衍生物。它是一种有效的拓扑异构酶的选择性抑制剂。Topoisomerase II inhibitor 6 在 G2 期阻断 CCRF-CEM 的细胞周期并诱导 DNA 双链断裂。Topoisomerase II inhibitor 6 对不同的肿瘤细胞系具有抗增殖活性，在癌症疾病研究中具有潜力。

Anticancer agent 64 (化合物 5m) 对 CCRF-CEM 细胞具有细胞毒性，其IC50为2.4 μM。Anticancer agent 64 通过诱导细胞凋亡表现出良好的抗癌活性。Anticancer agent 64 诱导caspase 3和 7 的激活和PARP 的裂解。Anticancer agent 64 具有明显的线粒体去极化作用。

Isoscopoletin (7-Methoxyesculetin) 是艾叶中的一种活性成分。它具有显著的细胞增殖抑制作用，对人类 CCRF-CEM 白血病细胞和耐药亚系 CEM ADR5000 作用的 IC50值分别为 4.0 μM 和 1.6 μM。它具有抑制 HBV 复制的活性。