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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T9117	BSJ-4-116	CDK; Ligand for E3 Ligase	Cell Cycle/Checkpoint; PROTAC
	BSJ-4-116 是一种高效的选择性 CDK12 降解剂，IC50 为 6 nM，是由 Cereblon 配体和 CDK 配体相连的 PROTAC。它通过提前终止转录来下调 DDR 基因，主要是通过增加聚腺苷酸化，具有抗增殖作用。
T77651	Tubulin polymerization-IN-47	Microtubule Associated	Cytoskeletal Signaling
	Tubulin polymerization-IN-47 是一种 tubulin 聚合抑制剂和有丝分裂抑制剂，具有抗肿瘤活性，对神经母细胞瘤癌细胞增殖具有抑制作用，对 Chp-134 和 Kelly 细胞系的IC50 分别为 7 和 12 nM。Tubulin polymerization-IN-47 是治疗肝癌、结肠癌、肺癌和乳腺癌的候选化合物。
T41180	JQAD1	Epigenetic Reader Domain	Chromatin/Epigenetic
	JQAD1是一种有效的、选择性的组蛋白乙酰转移酶 EP300降解剂（PROTAC；DC50≤31.6nM）；其包含 EP300抑制剂A485，通过连接体连接至脑啡肽E3连接酶配体。JQAD1以蛋白酶体依赖的方式导致神经母细胞瘤细胞系中EP300的降解。JQAD1抑制H3K27ac 和EP300的表达水平并诱导细胞凋亡。JQAD1抑制Kelly 细胞异种移植的NSG 小鼠的肿瘤生长。CRC 和MYCN 基因表达水平在JQAD1治疗的肿瘤中下调。JQAD1在诱导EP300降解的浓度下对共活化剂CBP 没有显著影响。
T79645	Tubulin polymerization-IN-48
	Tubulin polymerization-IN-48 (Compound 4k) 是一种中等强度破坏微管网络的微管蛋白聚合抑制剂。其对神经母细胞瘤癌细胞增殖的抑制效果显著，Chp-134 细胞系和 Kelly 细胞系的IC50值分别为79 nM和165 nM。
T50110	CD532	Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	CD532 是一种高效的 Aurora A 激酶抑制剂，IC50 值为 45 nM。CD532 可阻断 Aurora A 激酶活性，驱动 MYCN 降解，可以直接与 AURKA 相互作用并诱导整体构象转变。CD532 可用于研究癌症。
T36176	AMK (hydrochloride)
	AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7...

化合物

BSJ-4-116

Cat.No: T9117

Synonym:

Target: CDK, Ligand for E3 Ligase

Tubulin polymerization-IN-47

Cat.No: T77651

Synonym:

Target: Microtubule Associated

JQAD1

Cat.No: T41180

Synonym:

Target: Epigenetic Reader Domain

Tubulin polymerization-IN-48

Target: Aurora Kinase

Cat. No.	Product Name	Target	Signaling Pathways
T36954	Nemorosone
	Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem...