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25

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T76787	Conatumumab TRAIL-R2 mAb,AMG 655	TNF	Apoptosis
	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。
T8969	API-1 NSC177223	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	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。
T2065	Bioymifi DR5 Activator	Apoptosis; TNF	Apoptosis
	Bioymifi (DR5 Activator) 是一种 TRAIL 受体DR5激活剂，与DR5的胞外结构域结合，Kd 为 1.2 μM，它可诱导 DR5 聚集，导致细胞凋亡。
T7001	TIC10 ONC-201	Apoptosis; TNF	Apoptosis
	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。
T76815	Lexatumumab ETR2-ST01,DR5 mAB,HGS-ETR 2	Apoptosis	Apoptosis
	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)。
T16392	ONC206	Dopamine Receptor	GPCR/G Protein; Neuroscience
	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。
T6705	TIC10 Isomer ONC201 isomer,TIC10 Analogue	Others	Others
	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。
T4423	LY 303511 hydrochloride LY303511 hydrochloride	Potassium Channel; TNF; mTOR	Apoptosis; Membrane transporter/Ion channel; PI3K/Akt/mTOR signaling
	LY 303511 hydrochloride 是LY294002 的一种结构类似物。LY 303511 hydrochloride 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。
T6776	BAY 61-3606 dihydrochloride BAY 61-3606,BAY-61-3606 dihydrochloride	Apoptosis; Syk	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	BAY 61-3606 dihydrochloride (BAY 61-3606) 是一种口服有效的，ATP 竞争性的，可逆的选择性Syk 抑制剂。它降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化，也降低 K-rn 细胞裂解物中 Syk 磷酸化。它作用于乳腺癌细胞，通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。
T4263	BAY 61-3606 2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺,Syk inhibitor IV	Apoptosis; Syk	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	BAY 61-3606 (Syk inhibitor IV) 是一种具有口服活性的，ATP 竞争性的可逆选择性Syk 抑制剂。它作用于乳腺癌细胞，通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。它降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化，也降低 K-rn 细胞裂解物中 Syk 磷酸化。
T33892	PBOX-15
	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
T70352	PH11
	PH11 is a novel Focal Adhesion Kinase (FAK) inhibitor. PH11 restores TRAIL apoptotic pathway in PANC-1 cells through down-regulation of c-FLIP via inhibition of FAK and the phosphatidylinositol-3 kinase (PI3K)/AKT pathways. Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) emerges as one of the most-promising experimental cancer therapeutic drugs and is currently being tested in clinical trials. However, both intrinsic and acquired resistance of human cancer cells to TRAIL...
T23859	CaspPro C-2,C 2,Casp-Pro,Casp Pro,C2
	CaspPro is a selective activator of caspase 8 that acts by potentiating TRAIL-induced cell death.
T26709	Azadirone
	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
T32072	Hexyl decanoate Decanoic acid hexyl ester
	Hexyl decanoate, the first trail pheromone compound identified in a stingless bee, Trigona recursa. Hexyl decanoate is dominant component of gland secretions.
T15723	LBW242	Others	Others
	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
T35729	Nemadipine-A
	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 ...
T11682	Isofistularin-3	Others	Others
	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.
T37837	2-Methylhexacosane
	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: ...
T78715	MS78
	MS78为一种乙酰化靶向嵌合体(AceTAC)，其功能是招募组蛋白乙酰转移酶p300/CBP以乙酰化p53肿瘤抑制蛋白的p53Y220C突变体。通过该作用，MS78能够上调TRAIL凋亡基因，同时下调DNA损伤反应信号通路。此化合物结构包含CBP/p300结合物、p53Y220C结合物及linker。
T70377	BAY 61-3606 HCl
	BAY 61-3606 HCl is a cell-permeable, reversible inhibitor of spleen tyrosine kinase. BAY 61-3606 HCl can inhibit degranulation and block cytokine release from mast cells. Oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema. It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9. This compound has been used i...
T36890	A 410099.1
	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 n...
T2434	LY 303511	Potassium Channel; TNF; mTOR	Apoptosis; Membrane transporter/Ion channel; PI3K/Akt/mTOR signaling
	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。
T36820	Fluphenazine-N-2-chloroethane (hydrochloride)
	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 ...
T35558	KAAD-Cyclopamine
	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 onco...

化合物

Cat.No: T76787

Synonym: TRAIL-R2 mAb,AMG 655

Target: TNF

Cat.No: T8969

Synonym: NSC177223

Target: Akt

Cat.No: T2065

Synonym: DR5 Activator

Target: Apoptosis, TNF

Cat.No: T7001

Synonym: ONC-201

Target: Apoptosis, TNF

Cat.No: T76815

Synonym: ETR2-ST01,DR5 mAB,HGS-ETR 2

Target: Apoptosis

Cat.No: T16392

Target: Dopamine Receptor

Cat.No: T6705

Synonym: ONC201 isomer,TIC10 Analogue

Target: Others

LY 303511 hydrochloride

Cat.No: T4423

Synonym: LY303511 hydrochloride

Target: Potassium Channel, TNF, mTOR

BAY 61-3606 dihydrochloride

Cat.No: T6776

Synonym: BAY 61-3606,BAY-61-3606 dihydrochloride

Target: Apoptosis, Syk

Cat.No: T4263

Synonym: 2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺,Syk inhibitor IV

Target: Apoptosis, Syk

Cat.No: T33892

Cat.No: T70352

Cat.No: T23859

Synonym: C-2,C 2,Casp-Pro,Casp Pro,C2

Cat.No: T26709

Hexyl decanoate

Cat.No: T32072

Synonym: Decanoic acid hexyl ester

Cat.No: T15723

Target: Others

Cat.No: T35729

Isofistularin-3

Cat.No: T11682

Target: Others

2-Methylhexacosane

Cat.No: T37837

Cat.No: T78715

BAY 61-3606 HCl

Cat.No: T70377

Cat.No: T36890

Cat.No: T2434

Target: Potassium Channel, TNF, mTOR

Fluphenazine-N-2-chloroethane (hydrochloride)

Cat.No: T36820

KAAD-Cyclopamine

Cat.No: T35558

Cat. No.	Product Name	Target	Signaling Pathways
T3862	Irigenin	NF-κB; Integrin	Cytoskeletal Signaling; NF-κB
	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。
T30969	Clitocine	Apoptosis; BCL	Apoptosis
	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。
TN4038	Eupatolide	TNF; NOS; NF-κB; ROS; MAPK; Akt; COX; DNA/RNA Synthesis; Nrf2; PDGFR; NO Synthase; Prostaglandin Receptor; Autophagy	Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Cytoskeletal Signaling; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; MAPK; Neuroscience; NF-κB; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	Eupatolide 是从 Inula japonica 的花中分离出来的，具有抗炎活性。 Eupatolide 可用于研究乳腺癌细胞对 TRAIL 的耐药性。
T82578	Desacetylxanthanol
	Desacetylxanthanol (Compound 4)，源自Xanthium strumarium的倍半萜类化合物，展现出抗肿瘤坏死因子相关凋亡诱导配体(TRAIL)活性。
T21577	Narasin (sodium salt) Naracin sodium salt,naransin sodium,海南霉素,HainanMycin	NF-κB	NF-κB
	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。

天然产物

Cat.No: T3862

Target: NF-κB, Integrin

Cat.No: T30969

Target: Apoptosis, BCL

Cat.No: TN4038

Target: TNF, NOS, NF-κB, ROS, MAPK, Akt, COX, DNA/RNA Synthesis, Nrf2, PDGFR, NO Synthase, Prostaglandin Receptor, Autophagy

Desacetylxanthanol

Cat.No: T82578

Narasin (sodium salt)

Cat.No: T21577

Synonym: Naracin sodium salt,naransin sodium,海南霉素,HainanMycin

Target: NF-κB

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