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PROTAC抑制剂 Cocktails
Ligand for Target Protein for PROTAC
Targeted protein degradation (TPD) is attracting substantial interest owing to its potential to therapeutically modulate proteins that have proved difficult to target with conventional small molecules. A major class of molecules that may enable such proteins to be modulated through TPD are known as proteolysis-targeting chimera (PROTAC) protein degraders. These are heterobifunctional small molecules consisting of two ligands joined by a linker: one ligand recruits and binds a protein of interest (POI) while the other recruits and binds an E3 ubiquitin ligase.
- PROTAC BRD4 ligand-1T125512313230-51-0In housePROTAC BRD4 ligand-1 是 PROTAC GNE-987 靶向 BRD4 蛋白的配体，也是一种 BET 的抑制剂。
- ¥ 1390
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- IbrutinibT1835936563-96-1Ibrutinib (PCI-32765) 是一种布鲁顿酪氨酸激酶 (BTK) 抑制剂 (IC50=0.5 nM)，具有不可逆性和选择性。Ibrutinib 可以阻断 BTK 抑制 B 细胞的增殖和存活，具有抗肿瘤活性，可以用于治疗慢性淋巴细胞白血病等。
- ¥ 488
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客户已引用 - (+)-JQ-1T21101268524-70-4(+)-JQ-1 (JQ1) 是一种 BET 溴结构域抑制剂，抑制 BRD4(1 2) (IC50=77 33 nM)，具有特异性和可逆性。(+)-JQ-1 可以诱导细胞自噬，抑制细胞增殖。
- ¥ 253
规格数量 客户已引用 - QuizartinibT2066950769-58-1Quizartinib (AC220) 是一种第二代 Ⅱ 型 FLT3 酪氨酸激酶抑制剂，具有口服活性和高选择性，抑制 FLT3-WT 和 FLT3-ITD 自磷酸化 (IC50=4.1 1.1 nM)。Quizartinib 可以诱导肿瘤细胞凋亡。
- ¥ 297
规格数量 客户已引用 - Navitoclax-piperazineT121862143096-93-7Navitoclax-piperazine (ABT-263-piperazine) 是一种特大型 B 细胞淋巴瘤(BCL-XL)抑制剂。它和 E3 泛素连接酶的 VHL 配体可用来合成 PROTAC DT2216。
- ¥ 868
规格数量 - SMARCA-BD ligand 1 for ProtacT138481997319-92-2In houseSMARCA-BD ligand 1 for Protac 能够与 BAF ATPase 亚基 SMARCA2 结合，可用于 PROTAC 技术，用于降解 SMARCA2。
- ¥ 593
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- DUPAT19301302941-52-2DUPA (N,N''-Carbonylbis[L-glutamic acid]) 是谷氨酸脲，在药物偶联中作为靶向部分，可选择靶向性地将细胞毒性药物递送到前列腺癌细胞。
- ¥ 396
规格数量 - SLF-amido-C2-COOHT139141092369-24-8SLF-amido-C2-COOH (ZZY01-083) 是一种 FKBP 配体，具有潜在的抗菌活性，可用于合成 PROTAC。
- ¥ 445
规格数量 - BI-4464T54801227948-02-8BI-4464 是一种高选择性的 ATP 竞争性 PTK2 FAK 抑制剂，IC50=17 nM。它可用于PROTAC 降解剂的 PTK2 配体。
- ¥ 497
规格数量 - Dasatinib carbaldehydeT185952112837-79-1Dasatinib carbaldehyde (PROTAC ABL binding moiety 4) 基于 ABL 抑制剂达沙替尼，通过接头与 IAP 配体结合，形成 SNIPER [1]。
- ¥ 119
规格数量 - AP1867-3-(aminoethoxy)T135492127390-15-0In houseAP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.
- ¥ 2890
规格数量 - Androgen receptor antagonist 1T103201338812-36-4In houseAndrogen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
- ¥ 4280
规格数量 - Imatinib carbaldehydeT185921436868-85-7Imatinib carbaldehyde (also known as CGP-57148B carbaldehyde) is a compound derived from Imatinib, an inhibitor of the ABL protein. Imatinib carbaldehyde binds to the IAP ligand with the assistance of a linker, resulting in the formation of SNIPER[1].
- 待询
规格数量 - PROTAC BRD9-binding moiety 1 hydrochlorideT13915LPROTAC BRD9-binding moiety 1 hydrochloride inhibits BRD9 activity by binding to BRD9, utilizing the PROTAC (Proteolysis Targeting Chimera) mechanism.
- ¥ 3740
规格数量 - GNF5-amido-MeT18593778277-37-5GNF5-amido-Me, the moiety based on GNF5 (ABL inhibitor),binds through a linker to the IAP ligand forming SNIPER[1].
- 待询
规格数量 - PAG 4'-piperazine-4-methylpiperidineT203766PAG 4'-piperazine-4-methylpiperidine 是一种用于 PROTAC 研究和开发的功能化 cereblon 配体。包含一个 E3 ligase ligand 和一个末端哌啶，以进一步化学合成生成具有刚性连接子的 Protein Degraders。它是 PROTAC R&D 的一系列功能化工具分子的一部分。
- 待询
规格数量 - H117T203027H117 是一种 PROTAC 靶蛋白配体，可用于合成 PROTAC HP211206，与 SARS-CoV-2 主蛋白酶 (Mpro) 具有竞争性结合和抑制效果，IC50 为 151.3 nM。
- 待询
规格数量 - SMARCA2 ligand-11T2036153033592-44-5SMARCA2 ligand-11 是一种SMARCA2的配体，用于合成靶向蛋白的PROTAC SMARCA2 degrader-32。
- 待询
规格数量 - CCW16-PEG2-butyl-BocNHT203751CCW16-C9-BocNH，由RING finger protein 4 (RNF4) 招募配体、含有亲水和疏水基团的连接体以及与目标配体羧酸反应的悬挂胺组成，在靶向蛋白降解和PROTAC研究中的蛋白降解剂开发和合成中起重要作用。
- 待询
规格数量 - BRD9 ligand-7T203041BRD9 ligand-7 是 PROTAC 的靶蛋白配体 (Ligand for Target Protein for PROTAC)，并可用于合成 BRD9 Degrader-1。
- 待询
规格数量 - SMARCA2 ligand-12T2033272755762-94-6SMARCA2 ligand-12 是一种PROTAC靶蛋白配体 (Ligand for Target Protein for PROTAC)，用于合成PROTAC SMARCA2 degrader-25。
- 待询
规格数量 - ITK ligand 1T203599ITK ligand 1 是PROTAC靶蛋白配体 (Ligands for Target Protein for PROTACS) ，用于合成PROTACs。
- 待询
规格数量 - Apcin-AT103451683617-62-0Apcin-A is an anaphase-promoting complex (APC) inhibitor. It interacts strongly with Cdc20 and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V.
- ¥ 1710
规格数量 - FN-1501-propionic acidT136962408642-48-6FN-1501-propionic acid, a CDK2 9 ligand, in conjunction with a CRBN ligand, has been utilized in the design of a PROTAC CDK2 9 degrader.
- ¥ 10600
规格数量 - CDK9-IN-11T107432748368-15-0CDK9-IN-11 是一种有效的CDK9抑制剂，可作为 PROTAC CDK9 Degrader-1 的配体。
- ¥ 10600
规格数量 - BET-IN-6T105222570470-39-0BET-IN-6 是一种有效且高亲和力的BRD2 BRD4抑制剂。BET-IN-6 是靶蛋白 BRD2 4 的配体，可用于合成 PROTAC BRD2 BRD4 degrader-1 。
- ¥ 10600
规格数量 - Estrone-N-O-C1-amidoT17940138219-84-8Estrone-N-O-C1-amido (ERα ligand 1) is an estrogen ligand derived from Estrone that specifically binds to estrogen receptor α (ERα). Through a linker, Estrone-N-O-C1-amido (ERα ligand 1) forms a complex with the cIAP1 ligand Bestatin, leading to the creation of SNIPER[1].
- 待询
规格数量 - Ch55-O-C3-NH2T18650144298-98-6Ch55-O-C3-NH2, also known as RAR ligand 1, is a ligand derived from the Ch55 compound that specifically targets RAR. Through a linker, Ch55-O-C3-NH2 interacts with cIAP1 ligand Bestatin to form SNIPER[1].
- 待询
规格数量 - SirReal1-O-propargylT186411862237-99-7SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2[1].
- 待询
规格数量 - Ipatasertib-NH2T180531001382-14-4Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for the target protein AKT used in PROTAC, binding to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 for AKT degradation[1].
- 待询
规格数量 - Pomalidomide-PEG5-AlkyneT203769Pomalidomide-PEG5-Alkyne是合成靶向蛋白质降解剂和PROTACs的构建模块。该结合物含有(CRBN)-募集配体和带有悬挂炔的PEG化交联剂。该炔用于与靶配体上的叠氮化物进行点击化学反应。
- 待询
规格数量 - c-Myc ligand 1T2036201942834-87-8c-Mycligand 1 是c-Myc抑制剂，作为PROTAC靶蛋白配体 (Ligand for Target Protein for PROTAC)，可用于合成PROTAC c-Myc inhibitor 7。
- 待询
规格数量 - CDK ligand for PROTAC hydrochlorideT10734LCDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.
- ¥ 3010
规格数量 - PD0325901-O-C2-dioxolaneT402172581116-22-3PD0325901-O-C2-dioxolane的主体为PD0325901，PD0325901是一种典型的非ATP竞争性MEK1 2（丝裂原活化蛋白激酶）抑制剂，占据ATP结合位点附近的变构结合袋，具有减少ERK的磷酸化和抑制细胞增殖的抗癌作用。
- ¥ 1080
规格数量 - A-1210477-piperazinylT191722351218-72-7A-1210477-piperazinyl is a compound that specifically targets and binds to the protein myeloid cell leukemia 1 (MCL1). This compound is utilized in PROTAC technology, which harnesses the ability to selectively degrade target proteins.
- 待询
规格数量 - HG-7-85-01-DecyclopropaneT18594Decyclopropane, also known as HG-7-85-01, is a chemical compound with ABL inhibitor properties. It binds to the IAP ligand through a linker, resulting in the formation of SNIPER [1].
- 待询
规格数量 - Palbociclib-propargylT185152366269-23-8Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1].
- ¥ 1050
规格数量 - AP1867-2-(carboxymethoxy)T186112230613-03-1AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG molecules[1].
- ¥ 1620
规格数量 - I-BET762 carboxylic acidT130861300019-38-8I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).
- ¥ 399
规格数量 - CCR7 Ligand 1T10716681514-83-0CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM
- ¥ 15400
规格数量 - Pomalidomide-pyridine-PEG1-piperazine hydrochlorideT203767Pomalidomide-pyridine-PEG1-piperazine hydrochloride 是用于合成靶向蛋白降解剂和PROTACs的构件，包含Cereblon (CRBN) 招募配体、具有增强刚性的连接子，并带有与目标配体上的羧酸反应的悬挂胺。
- 待询
规格数量 - Thalidomide-Photoswitch3-NH2 hydrochlorideT203799Thalidomide-Photoswitch3-NH2 hydrochloride是合成PHOTACs的重要成分，这些PHOTACs是通过不同光波长调节可逆性激活的PROTACs，其在黑暗中会失去活性，而在390 nm波长的照射下被激活为顺式异构体。在450 nm以上的波长范围内，这些PHOTACs会被可逆失活。该共轭物由Cereblon (CRBN) 招募配体、偶氮苯光开关交联剂以及一个与目标弹头酸基反应的悬浮胺基组成，被用于PHOTAC-I-10和PHOTAC-II-6的制备。
- 待询
规格数量 - IRAK4 ligand-12T2030242573304-97-7IRAK4 ligand-12 是一种PROTAC靶蛋白配体 (Ligand for Target Protein for PROTAC)，可用于合成KTX-951。
- 待询
规格数量 - MTH1 degrader-1T2032262412987-06-3MTH1 degrader-1 是MTH1 aTAG抑制剂，也是PROTAC靶蛋白配体 (Ligand for Target Protein for PROTAC)，可用于合成PROTAC aTAG 4531。
- 待询
规格数量 - SI-109T129052429877-30-3SI-109 is a potent inhibitor of STAT3 SH2 domain (Ki=9 nM),and with antitumor activity.
- ¥ 11520
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