PROTAC商业化元年,一站式砌块库助你跑赢降解剂研发赛道
2026-09-03 · 推荐产品 · 百灵威授权转载
2026年,全球首款PROTAC药物韦德格司群正式上市,靶向蛋白降解从概念验证迈入商业化时代。
但PROTAC的"哑铃型"结构决定了它的研发痛点:分子量大、Linker设计难、三类砌块(靶头+连接链+E3配体)采购散乱。药物化学家花在找齐合适砌块上的时间,往往比设计分子还长。
百灵威提供覆盖PROTAC核心链路的分子砌块解决方案,助您加速降解剂研发,抢占靶向蛋白降解赛道先机。
Linker核心骨架——哌啶 & 哌嗪
PROTAC连接链的长度、刚柔性、水溶性直接决定降解效率。哌啶和哌嗪是Linker设计中出场率最高的脂肪环骨架。
靶头配体首选——嘧啶 & 吲哚
嘧啶环凭借与靶蛋白铰链区的强氢键作用,成为PROTAC靶头设计的核心杂环;吲哚则在激酶类降解剂中持续走强。
哌啶 & 哌嗪
| 品名 | CAS | 货号 |
|---|---|---|
| Methyl 1-methyl-4-oxopiperidine-3-carboxylate hydrochloride, 97% 1-甲基-4-氧代哌啶-3-甲酸甲酯盐酸盐 | 13049-77-9 | 296101 |
| 1-Boc-4-(5-formyl-4-methylthiazol-2-yl)piperidine, 95% 1-Boc-4-(5-甲酰基-4-甲基噻唑-2-基)哌啶 | 850374-97-9 | 605733 |
| Ethyl 1-(2-Chloroacetyl)-4-piperidinecarboxylate, 97% 1-(2-氯乙酰基)-4-哌啶甲酸乙酯 | 318280-71-6 | 102181 |
| 1-(1-Boc-piperidin-4-yl)-piperazine hydrochloride, 98% 1-(1-Boc-哌啶-4-基)-哌嗪盐酸盐 | 205059-39-8 | 908074 |
| tert-Butyl 4-(5-formylpyrid-2-yl)piperazine-1-carboxylate, 97% 4-(5-甲酰基吡啶-2-基)哌嗪-1-甲酸叔丁基酯 | 479226-10-3 | 113874 |
| 4-(5-Carboxy-pyridin-2-yl)-piperazine-1-carboxylic acid tert-butyl ester, 97% 4-(5-羧基-吡啶-2-基)-哌嗪-1-羧酸叔丁酯 | 201809-22-5 | 559672 |
| 1-(3-Methyl-pyridin-2-yl)-piperazine, 98% 1-(3-甲基吡啶-2-基)哌嗪 | 111960-11-3 | 409477 |
嘧啶 & 吲哚
| 品名 | CAS | 货号 |
|---|---|---|
| 2,4-Diaminopyrimidine-5-carboxylic acid, 97% 2,4-二氨基-5-羧基嘧啶 | 18588-61-9 | 295336 |
| 2,4-Dichloro-6-ethyl-5-fluoropyrimidine, 97% 2,4-二氯-6-乙基-5-氟嘧啶 | 137234-85-6 | 355635 |
| 6-Ethylthieno[2,3-d]pyrimidin-4(3H)-one, 98% 6-乙基噻吩并[2,3-d]嘧啶-4(3H)-酮 | 18593-51-6 | 127119 |
| N-(4-Aminopyrimidin-2-yl)-N-methylamine, 97% N-(4-氨基嘧啶-2-基)甲胺 | 22404-42-8 | 150756 |
| 4-Aminopyrimidine-5-carboxamide, 97% 4-氨基嘧啶-5-甲酰胺 | 4786-51-0 | 252992 |
| 6-Chloro-1H-indole-2-carboxylic acid, 97% 6-氯-1H-吲哚-2-羧酸 | 16732-75-5 | 100116 |
| 2-Methyl-7-azaindole, 99% 2-甲基-7-氮杂吲哚 | 23612-48-8 | 971474 |
| 4-Methoxy-7-azaindole-2-carbaldehyde, 97% 4-甲氧基-2-醛基7-氮杂吲哚 | 290333-01-6 | 136130 |
超干溶剂
| 品名 | CAS | 货号 |
|---|---|---|
| 1-Methyl-2-pyrrolidinone, 99.5%, SuperDry, with molecular sieves, water≤50 ppm, J&Kseal 1-甲基-2-吡咯烷酮 | 872-50-4 | 942009 |
| Tetrahydrofuran, 99.9%, SuperDry, stabilized with 250 ppm BHT, Water≤50 ppm, J&KSeal 四氢呋喃 | 109-99-9 | 315353促 危化品 |
| Acetonitrile, 99.9%, SuperDry, with molecular sieves, water≤50 ppm, J&KSeal 乙腈 | 75-05-8 | 939631促 危化品 |
| 1,4-Dioxane, 99.5%, SuperDry, with molecular sieves, stabilized with BHT, J&Kseal, water≤50 ppm 1,4-二氧六环 | 123-91-1 | 972869促 危化品 |
| Dimethyl sulfoxide, 99.7%, SuperDry, with molecular sieves, water≤50 ppm, J&KSeal 二甲基亚砜 | 67-68-5 | 292271促 |
核磁检测试剂
| 品名 | CAS | 货号 |
|---|---|---|
| Dimethyl sulfoxide-d6, 99.8 atom%D, contains 0.03% v/v TMS 氘代二甲基亚砜-d6 | 2206-27-1 | 182473促 |
| Chloroform-d, 99.8 atom%D, contains 0.03% v/v TMS, packed in 10*0.6 ml ampoules 氘代氯仿 | 865-49-6 | 240987促 |
| Tetrahydrofuran-d8, 99.5 atom%D 氘代四氢呋喃-d8 | 1693-74-9 | 247731 |
| Acetonitrile-d3, 99.8 atom%D 氘代乙腈-d3 | 2206-26-0 | 236920促 |
| Dichloromethane-d2, 99.8 atom%D 氘代二氯甲烷 | 1665-00-5 | 334919促 |
| Methanol-d4, 99.8 atom%D 氘代甲醇-d4 | 811-98-3 | 114655促 |
耗材
| 品名 | CAS | 货号 |
|---|---|---|
| TLC silica gel plate (fluorescent indicator), GF254, layer thickness 0.2-0.25 mm, 100*100 mm, 80 pcs/pack 薄层色谱硅胶板(含荧光) | / | 983347 |
| Silica, powder, 200 mesh 硅胶 | 112945-52-5 | 227600 |
| Spotting capillary tube, I.D.:0.3mm, Length:100mm, 1000pcs/pack 玻璃点样毛细管 | / | 2734477 |
| 5 mm NMR Economy Sample Tube w/ Cap, 7″, High-Throughput 5毫米,高通量经济型核磁管,7英寸 | / | 1001281 |
| Digital stainless steel hotplate magnetic stirrer, with heating, heating temperature range: RT 340℃, power 550 W 数显不锈钢加热磁力搅拌器 | / | 1122416 |
| Magnetic stir bar, PTFE-coated, egg-shaped, A100 (6*10mm), 5 pcs/pack 聚四氟乙烯磁力搅拌子,椭圆型 | / | 1482821 |
相关阅读
表观遗传学与PROTAC蛋白质降解技术——新型药物发现工具小分子大作为:PROTAC 药物的独特作用机制深度解析
技术桥梁,靶向链接——PROTAC Linker助力新药研发