trail

API-1 (NSC-177223) 是Akt PKB 抑制剂，可同 PH 结构域相结合并抑制 Akt 膜易位，有效降低 Akt 的磷酸化水平。它可选择性的抑制PKB，对 PKC 和 PKA 的激活无抑制作用。它可以和 TNF 相关的凋亡诱导配体协同作用从而诱导细胞凋亡。

Lexatumumab (HGS-ETR 2) 是一种靶向 TRAIL 受体 2 的人激动性单克隆抗体，具有抗癌活性， 在恶性间皮瘤中诱导细胞凋亡 (apoptosis)。Lexatumumab 可用于研究恶性胸膜间皮瘤 (MPM)。

Irigenin 可通过特异性和选择性地阻断 Extra Domain A 域的 C-C 环上α9β1和α4β1整合素结合位点，介导其抗转移作用。可通过增强胃癌细胞中促凋亡分子的表达来敏化 TRAIL 诱导的凋亡，具有抗癌作用。

TIC10 Isomer (ONC201 isomer) 是一种 TIC10 的异构体。它不能诱导 TRIAL 表达的生物学活性。

Conatumumab (AMG 655) 是一种靶向人死亡受体 5 (DR5，TRAILR2) 的单克隆激动剂抗体 ，对长型 DR5 的 Kd 为 1 nM, 对短型 DR5 的 Kd 0.8 nM。Conatumumab 通过半胱天冬酶激活在多种肿瘤类型中诱导细胞凋亡。Conatumumab 可用于研究晚期实体肿瘤。

Tigatuzumab (CS-1008) 是一种靶向 death receptor 5 (DR5) 的人源化单克隆抗体，是 TRAIL-R2 激动剂，具有抗肿瘤活性，可诱导癌细胞凋亡，可用于研究胰腺癌。

Mapatumumab (HGS-ETR1) 是一种针对 TNF 相关凋亡诱导配体受体 1 （TRAIL-R1）的全人源激动性单克隆抗体，具有抗癌活性，可诱导癌细胞凋亡。

ONC206 是一种 ONC201 的类似物，是一种多巴胺 D2- 样受体 (DRD2 3 4) 的选择性拮抗剂，其拮抗作用在纳摩尔级别。它具有广谱抗肿瘤活性。

TIC10 (ONC-201) 是一种有口服活性的， 可透过血脑屏障的，肿瘤坏死因子相关的凋亡诱导配体 TRAIL 诱导剂。它通过抑制 Akt 和 ERK，从而激活 Foxo3a 并显著诱导细胞表面 TRAIL。

Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM.

LBW242 is a 3-mer and Smac mimetic and is an effective and orally active proapoptotic IAP inhibitor. LBW242 has activity against multiple myeloma and potentiates TRAIL- and anticancer drug-mediated cell death of ovarian cancer cells. LBW242 displays effec

Bioymifi (DR5 Activator) 是一种有效的 TRAIL 受体 DR5 激活剂，与 DR5 的胞外结构域 (ECD) 结合，Kd 为 1.2 μM。Bioymifi 可以作为一种新型的 TNF 相关凋亡诱导配体 (TRAIL) 的类似物，可作为单一的诱导剂诱导 DR5 的聚集，刺激细胞凋亡。

Narasin (sodium salt) (HainanMycin) 通过神经胶质瘤细胞中的 ER 应激诱导肿瘤坏死因子相关凋亡诱导配体 (TRAIL) 介导的细胞凋亡，并通过抑制 IκBα 的磷酸化来抑制 NF-κB 信号传导。

CaspPro is a selective activator of caspase 8 that acts by potentiating TRAIL-induced cell death.

LY303511 是 LY294002 的结构类似物，可增强 SHEP-1 神经母细胞瘤细胞的TRAIL 敏感性，还可逆地阻断 MIN6 胰岛瘤细胞中的K+电流，IC50为64.6±9.1 μM。

Azadirone is a limonoid tetranortriterpene. Azadirone can sensitize cancer cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) through ROS-ERK-CHOP-mediated up-regulation of DR4 and DR5 signaling, down-regulation of cell survival prot

Clitocine 是一种来从蘑菇中提取的一种腺苷类似物，是一种有效的转录通读剂，是一种无义突变的抑制剂，具有抗癌活性，可诱导携带 p53 无义突变等位基因的细胞产生 p53 蛋白。Clitocine 通过促进 Mcl-1 降解来增强 TRAIL 介导的人结肠癌细胞凋亡。

Hexyl decanoate, the first trail pheromone compound identified in a stingless bee, Trigona recursa. Hexyl decanoate is dominant component of gland secretions.

PBOX-15 is a novel microtubule-targeting agent that induces apoptosis, upregulates death receptors, and enhances TRAIL-mediated apoptosis in multiple myeloma cells. It also inhibits T cell migration through post-translational modification of tubulin. Pbox

Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated oncogene 1 (Gli1) and cytosolic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner. Cyclopamine-KAAD also increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures and upregulates expression of the death receptors DR4 and DR5 in LN229 and U251 glioma cells.

Nemadipine A is an L-type calcium channel blocker that induces morphological and growth defects in wild-type C. elegans and those with hypoexpression of egl-19, which encodes the only L-type calcium channel α1-subunit in the C. elegans genome. It also inhibits L-type calcium channels in chick ciliary neurons. Nemadipine A increases TRAIL-induced cytotoxicity and synergistically enhances caspase-8 and caspase-3 activation in a concentration-dependent manner in H1299 lung adenocarcinoma cells. It also decreases Survivin expression when used alone or in combination with TRAIL in A549 cells.

Fluphenazine is a traditional antipsychotic compound that tightly binds the dopamine D2 receptor (Ki = 0.55 nM) and also reversibly inhibits calmodulin at micromolar concentrations. Fluphenazine-N-2-chloroethane is a derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding. It is a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC50 = 100 nM) and in vivo, inactivating approximately 90% of D2 receptors in mice within 4 hours of treatment. Through this action, fluphenazine-B-2-chloroethane can be used to induce catalepsy in mice. It irreversibly inhibits calmodulin at higher doses (IC50 = 10 μM), which can sensitize cancer cells to TRAIL-induced apoptosis.

High affinity XIAP antagonist (Kd = 16 nM for the BIR3 domain of XIAP). Exhibits cytotoxicity in a wide range of cancer cell lines in vitro (EC50 = 13 nM in MDA-MB-231 cells). Also displays antitumor activity in a mouse breast cancer xenograft model. Enhances TRAIL-induced apoptosis in chronic lymphocytic leukemia (CLL) cells. Oost et al (2004) Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J.Med.Chem. 47 4417 PMID:15317454 |Loeder et al (2009) A novel paradigm to trigger apoptosis in chronic lymphocytic leukemia. Cancer Res. 69 8977 PMID:19920200

2-Methylhexacosane is a saturated hydrocarbon and an insect pheromone.1,2It has been found in the cuticle ofM. dasystomusfemales, but not males, where it contributes to the mating behavior of males, as well as inD. melanogasterfemales where it modulates aggression of males towards females. 2-methylhexacosane has also been found in yellow jacket (V. vulgaris) trail extracts.3 1.Spikes, A.E., Pashen, M.A., Millar, J.G., et al.First contact pheromone identified for a longhorned beetle (Coleoptera: Cerambycidae) in the subfamily PrioninaeJ. Chem. Ecol.36(9)943-954(2010) 2.Fernández, d.l.P., Chan, Y.-B., Yew, J.Y., et al.Pheromonal and behavioral cues trigger male-to-female aggression in DrosophilaPLoS Biol.8(11)e1000541(2010) 3.Steinmetz, I., Schmolz, E., and Ruther, J.Cuticular lipids as trail pheromone in a social waspProc. Biol. Sci.270(1513)385-391(2003)