技术桥梁，靶向链接——PROTAC Linker助力新药研发-百灵威

当前临床治疗中普遍采用的药物多是基于小分子设计的，它们通过“占据驱动”的机制来抑制蛋白质的功能，从而达到治疗疾病的目的。

然而，与传统的小分子抑制剂和拮抗剂不同，PROTAC（蛋白降解靶向联合体）技术（图1）通过诱导致病靶蛋白的降解，开辟了药物研发的新路径。近年来，这一技术发展迅猛，已成为新药开发领域的重要工具。

图1 The mechanism of PROTAC-mediated protein degradation

PROTAC Linker（PROTAC 连接子）的最佳长度12个碳到20 个碳不等，在 PROTAC 构建中起着重要作用，用来连接 PROTAC 的两个功能基团，靶蛋白配体和E3 连接酶配体。较常用的接头是PEG、烷基链和烷基醚。

百灵威提供百余种PROTAC Linker，助力PROTAC 分子构建。

产品列表

品名	CAS	货号
N-Boc-2-(2-amino-ethoxy)-ethylamine, 98% BocNH-PEG1-CH2CH2NH2	127828-22-2	1033177
tert-Butyl (2-(2-(2-(2-aminoethoxy)ethoxy)ethoxy)ethyl)carbamate, 95% (2-(2-(2-(2-氨基乙氧基)乙氧基)乙氧基)乙基)氨基甲酸叔丁酯	101187-40-0	1033209
4-Maleimidobutyric acid, 98% 4-马来酰亚胺丁酸	57078-98-5	107212
3-(Benzyloxy)propanoic acid, 97% 3-(苄氧基)丙酸	27912-85-2	1188273
Methyl 4-bromobutyrate, 98% 4-溴丁酸甲酯	4897-84-1	136064
Biotin pentafluorophenyl ester, 90% 生物素五氟苯酯	120550-35-8	1420381
Toluene-4-sulfonic acid 4-bocamino-butyl ester, 97% 甲苯-4-磺酸4-Boc-氨基丁酯	180851-50-7	1426290
Boc-γ-OH, 98% N-Boc-γ-氨基丁酸	57294-38-9	143259
tert-Butyl (10-aminodecyl)carbamate, 97% (10-氨基十二烷基)氨基甲酸叔丁酯	216961-61-4	152818
Biotin-PEG3-Azide, 95% 生物素-PEG3-叠氮化物	875770-34-6	1528348
Fmoc-N-amido-PEG12-acid, 95% Fmoc-N-氨基-PEG12-酸	756526-01-9	1529587
15-Azido-4,7,10,13-tetraoxapentadecanoic acid, 95% 15-叠氮基-4,7,10,13-四氧杂十五烷酸	1257063-35-6	1530273
2-(2-(2-Methoxyethoxy)ethoxy)ethanamine, 98% 2-(2-(2-甲氧基乙氧基)乙氧基)乙胺	74654-07-2	1550054
4-((tert-Butoxycarbonyl)(methyl)amino)butanoic acid, 97% 4-(叔丁羰基(甲基)氨基)丁酸	94994-39-5	1606580
7-Methoxy-7-oxoheptanoic acid, 97% 7-甲氧基-7-氧代庚酸	20291-40-1	1751011
N-Boc-4,7,10-trioxa-1,13-tridecanediamine, 95% N-Boc-4,7,10-三氧杂-1,13-十三烷二胺	194920-62-2	177362
Boc-ε-Acp-OH/Boc-6-Ahx-OH, 98% Boc-6-氨基己酸	6404-29-1	177964
Pentaethylene glycol, 98% 五甘醇	4792-15-8	177978
Biotin-PEG2-NHS, 95% 生物素-PEG2-NHS	596820-83-6	1880522
Link-EZ NHS-PEG4-Biotin N/A	459426-22-3	1880523
tert-Butyl 1-amino-3,6,9,12-tetraoxapentadecan-15-oate 1-氨基-3,6,9,12-四氧杂十五烷-15-酸叔丁酯	581065-95-4	1880536
Amino-PEG6-t-butyl ester 氨基-PEG6-叔丁酯	1286281-32-0	1880537
Hydroxy-PEG5-t-butyl ester, 95% 羟基-PEG5-叔丁酯	850090-09-4	1880540
2,5,8,11,14-Pentaoxaheptadecan-17-oic acid, 97% 2,5,8,11,14-五氧杂十七烷-17-酸	81836-43-3	1880549
PEGylated, long-chain SMCC crosslinker 马来酰亚胺-PEG6-琥珀酰亚胺酯	1137109-21-7	1880577
Maleimide-PEG8-succinimidyl ester, 95% 马来酰亚胺-PEG8-琥珀酰亚胺酯	756525-93-6	1880578
Mal-PEG2-COOH, 98% MIPA-PEG2-丙酸	756525-98-1	1880583
[2-[[2-(Fmoc-amino)ethoxy]ethoxy]acetic acid, 98.5% [2-[[2-(Fmoc-氨基)乙氧基]乙氧基]乙酸	166108-71-0	190014
PEG5-Carboxylic acid tert-butyl ester, 95% PEG5-羧酸叔丁酯	518044-32-1	1908613
11-Azido-3,6,9-trioxaundecan-1-amine, 95% 11-叠氮-3,6,9-三氧杂十一烷-1-胺	134179-38-7	194036
7-Octynoic acid, 98% 7-辛炔酸	10297-09-3	1967004
Potassium 6-hydroxyhexanoate, 98% 6-羟基己酸钾	21810-34-4	2082137
S-Acetyl-PEG3-alcohol, 95% S-乙酰基-三聚乙二醇	153870-20-3	2096397
11-Aminoundecanoic acid, 97% 11-氨基十一酸	2432-99-7	212542
11-Maleimidoundecanoic acid, 97% 11-马来酰亚胺十一烷酸	57079-01-3	214339
4,7,10-Trioxa-1,13-tridecanediamine, 96% 4,7,10-三氧-1,13-十三烷二胺	4246-51-9	229690
N-(2-(2-(2-(2-(2-(2-Azidoethoxy)ethoxy)ethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-hexahydro-2-oxo-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, 95% N-(2-(2-(2-(2-(2-(2-叠氮基乙氧基)乙氧基)乙氧基)乙氧基)乙氧基)乙基)-5 -((3aS,4S,6aR)-六氢-2-氧代1H-噻吩并[3,4-d]咪唑-4-基)戊酰胺	1163732-89-5	2323667
Hydroxy-PEG6-t-butly ester, 95% 丙酸叔丁酯-六聚乙二醇	361189-64-2	2326485
Alkyne-PEG5-acid 乙炔-PEG5-酸	1245823-51-1	2326506
2-(2-(2-Bromoethoxy)ethoxy)ethanol, 97% 2-(2-(2-溴乙氧基)乙氧基)乙醇	57641-67-5	2326521^新
1,2-Dithiolane-3-pentanoic acid succinimidyl ester, 95% 1,2-二噻戊环-3-戊酸琥珀酰亚胺酯	40846-94-4	2327062
Biotin-PEG4-Azide, 95% 生物素-PEG4-叠氮化物	1309649-57-7	2451134
5-Amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione, 98% 5-氨基-2-(2,6-二氧代哌啶-3-基)异二氢吲哚-1,3-二酮	191732-76-0	2453058
Decaethylene glycol, 96% 十甘醇	5579-66-8	248777
1-Bromo-2-(2-methoxyethoxy)ethane, 93% 1-溴-2-(2-甲氧基乙氧基)乙烷	54149-17-6	249587
Biotin-PEG4-propionic acid, 96% 生物素-PEG4-丙酸生物素-PEG4-丙酸	721431-18-1	251844
N-BOC-cadaverine, 98% N-BOC-尸胺	51644-96-3	258199
Triethylene glycol di(p-toluenesulfonate), 97% 三乙二醇二(对甲苯磺酸酯)	19249-03-7	264125
Poly(ethylene glycol methyl ether), 99.5%, average M.W.: 4500 - 5500 甲氧基聚乙二醇	9004-74-4	264748
Fmoc-12-amino-4,7,10-trioxadodecanoic acid, 98% Fmoc-12-氨基-4,7,10-三氧杂十二烷酸	867062-95-1	268487
5-Ethynyl-2'-deoxyuridine, 98% 5-乙炔基-2'-去氧尿苷	61135-33-9	285211
Heptaethylene glycol, 95% 七聚乙二醇	5617-32-3	346320
Bis(2-bromoethyl) ether, 96% 双(2-溴乙基)醚	5414-19-7	350172
Boc-15-amino-4,7,10,13-tetraoxapentadecanoic acid, 97% Boc-15-氨基-4,7,10,13-四氧杂十五酸	756525-91-4	353454
Ethylene glycol-bis(succinic acid N-hydroxysuccinimide ester), 95% 乙二醇 -双(琥珀酸 N-羟基琥珀酰亚胺酯)	70539-42-3	359030
6-Maleimidohexanoic acid, 98% 6-马来酰亚胺基己酸	55750-53-3	360723
2-[2-(Benzyloxy)ethoxy]ethanol, 98% 2-[2-(苄氧基)乙氧基]乙醇	2050-25-1	361865
3-Cyanopropanoic acid, 97% 3-氰基丙酸	16051-87-9	362097^新
5-(Z-Amino)-1-pentanol, 98% 5-(Z-氨基)-1-戊醇	87905-98-4	367305
N-Succinimidyl 6-biotinamidohexanoate, 98% N-琥珀酰亚氨基6-生物素氨己酸	72040-63-2	416884
N-Biotinylcaproylaminocaproic acid, 98% N-生物素基己酰氨基己酸	89889-51-0	420548
Tetraethylene glycol dimethyl ether, 98% 四乙二醇二甲醚	143-24-8	425149
Octaethylene glycol, 97% 八乙二醇	5117-19-1	426085
Boc-21-amino-4,7,10,13,16,19-hexaoxaheneicosanoic acid, 97%, purum Boc-21-氨基-4,7,10,13,16,19-六氧杂二十一烷酸	882847-13-4	437801
3-Maleimidopropionic acid, 98% 3-马来酰亚胺丙酸	7423-55-4	453319
1,11-Diazido-3,6,9-trioxaundecane, 98%, colorless to light yellow 1,11-二叠氮基-3,6,9-三氧杂十一烷	101187-39-7	454559
Boc-5-aminovaleric acid, 97% Boc-5-氨基戊酸	27219-07-4	464666
5-Azido-2-nitrobenzoic acid N-hydroxysuccinimide ester, 97% 5-叠氮基-2-硝基苯甲酸-N-琥珀酰亚胺酯	60117-35-3	466475
1,2-Bis(2-aminoethoxy)ethane, 98% 1,2-双(2-氨基乙氧基)乙烷	929-59-9	502798
Biotin-C5-amine, 95% 生物素-C5-胺	115416-38-1	511704
2-[2-(Boc-amino)-ethoxy]-ethanol, 98% 2-[2-(Boc-氨基)乙氧基]乙醇	139115-91-6	536629
Diethyleneglycol diacetate, 98% 二乙酸二甘酵脂	628-68-2	540044
1-Bromo-6-chlorohexane, 99% 1-溴-6-氯己烷	6294-17-3	554942
N-Boc-2-[2-(2-amino-ethoxy)-ethoxy]-ethylamine, 98% N-Boc-2-[2-(2-氨基-乙氧基)乙氧基]-乙胺	153086-78-3	565606
8-Hydroxyoctanoic acid, 97% 8-羟基辛酸	764-89-6	567583
1,3-Dibromo-5,5-dimethylhydantoin, 98% 1,3-二溴-5,5-二甲基乙内酰脲	77-48-5	569341
4-(Boc-amino)butyl bromide, 90% 4-(Boc-氨基)丁基溴	164365-88-2	595644
Fmoc-18-amino-4,7,10,13,16-pentaoxaoctadecanoic acid, 97% Fmoc-18-氨基-4,7,10,13,16-五氧杂十八烷酸	882847-32-7	601830
Hexaethylene glycol, 97% 六甘醇	2615-15-8	607058
4-Ethynylphenylacetonitrile, 98% 4-乙炔基苯乙腈	351002-90-9	625830
N-Boc-2-Maleimidoethylamine, 98% N-Boc-2-马来酰亚胺乙胺	134272-63-2	640093
1,11-Diamino-3,6,9-trioxaundecane, 98% 1,11-二氨基-3,6,9-三氧杂十一烷	929-75-9	785361
1,3,4,6-Tetra-O-acetyl-2-[(azidoacetyl)amino]-2-deoxy-β-D-galactopyranos, 98% 1,3,4,6-四-氧-乙酰基-2-[(叠氮乙酰基)氨基]-2-脱氧-β-D-吡喃半乳糖	653600-56-7	9075844
THAL-SNS-032, 98% THAL-SNS-032	2139287-33-3	9088405
3-(2-(2-(2-Azidoethoxy)ethoxy)ethoxy)prop-1-yne, 95% 3-(2-(2-(2-叠氮基乙氧基)乙氧基)乙氧基)丙-1-炔	932741-18-9	9103733
Propargyl-peg3-amine, 97% 丙炔基-三聚乙二醇-氨基	932741-19-0	9110656
14-(Boc-amino)-3,6,9,12-tetraoxatetradecan-1-oic acid 14-(Boc-氨基)-3,6,9,12-四氧杂十四烷-1-甲酸	876345-13-0	9116827
1-(2-Bromoethoxy)-2-(2-methoxyethoxy)ethane, 95% 二乙二醇-2-溴乙基甲醚	72593-77-2	913922
ARV-825, 98% ARV-825	1818885-28-7	9173846
Azido-PEG5-acid, 95% Azido-PEG5-acid	217180-81-9	9230084
BocNH-PEG6-acid BocNH-PEG6-acid	391684-36-9	9230085
1-Azido-2-(2-methoxyethoxy)ethane, 98% 1-叠氮基-2-(2-甲氧基乙氧基)乙烷	215181-61-6	923589
Biotin-PEG12-NHS ester, 95% 生物素-PEG12-NHS酯	1934296-88-4	9280538
MT-802 MT-802	2231744-29-7	9336867
N-Biotinyl-N'-(3-maleimidopropionyl)-3,6-dioxaoctane-1,8-diamine, 90% N-生物素基-N'-(3-马来酰亚胺基丙酰基)-3,6-二氧杂辛烷-1,8-二胺	305372-39-8	934373
UNC6852, 98% UNC6852	2688842-08-0	9349633
tert-Butyl (4-(methylamino)butyl)carbamate, 97% (4-(甲基氨基)丁基)氨基甲酸叔丁酯	874831-66-0	951398
Pentaethylene glycol di(p-toluenesulfonate), 95% 二对甲苯磺酸戊乙二醇	41024-91-3	980089
N-Boc-1,4-diaminobutane, 98%, for synthesis N-Boc-1,4-二氨基丁烷	68076-36-8	185579
Triethylene glycol, 99%, for synthesis 三乙二醇	112-27-6	259885
1-Boc-piperazine, 98%, for synthesis 1-Boc-哌嗪	57260-71-6	318266
Tetraethylene glycol, 99%, for synthesis 四缩乙二醇	112-60-7	427284
tert-Butyl N-(2-hydroxyethyl)carbamate, 98%, for synthesis N-(2-羟乙基)氨基甲酸叔丁酯	26690-80-2	508294

参考文献

He, M., Cao, C., Ni, Z. et al. PROTACs: great opportunities for academia and industry (an update from 2020 to 2021). Sig Transduct Target Ther 7, 181 (2022).

技术桥梁，靶向链接——PROTAC Linker助力新药研发

产品列表

参考文献

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