Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10359 |
AR antagonist 1
|
Androgen Receptor; Ligand for E3 Ligase; Ligands for Target Protein for PROTAC | Endocrinology/Hormones; PROTAC |
AR antagonist 1 是 AR 拮抗剂,能够与 E3 连接酶配体结合,与 VHL 蛋白结合亲和力较弱,用于 PROTACARD-266 合成。 | |||
T5480 |
BI-4464
|
FAK; Ligands for Target Protein for PROTAC | Angiogenesis; Cytoskeletal Signaling; PROTAC; Tyrosine Kinase/Adaptors |
BI-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。 | |||
T2110 |
(+)-JQ-1
JQ1 |
Epigenetic Reader Domain; Autophagy; Ligands for Target Protein for PROTAC | Autophagy; Chromatin/Epigenetic; PROTAC |
(+)-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。 | |||
T12186 |
Navitoclax-piperazine
ABT-263-piperazine |
BCL; Ligands for Target Protein for PROTAC | Apoptosis; PROTAC |
Navitoclax-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。 | |||
T1835 |
Ibrutinib
伊布替尼,依鲁替尼,PCI-32765 |
Tyrosine Kinases; Src; BTK; Ligands for Target Protein for PROTAC | Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors |
Ibrutinib (PCI-32765) 是一种不可逆的、选择性的 Btk 抑制剂,IC50=0.5 nM,它是一种 Btk 配体,用于合成一系列 PROTAC 分子,如 P13I。P13I 作用于人 Burkitt’s 淋巴瘤 RAMOS 细胞,浓度为 10 和 100 nM 时,分别降解 73% 和 89% Btk。 | |||
T39910 |
Desmorpholinyl Navitoclax-NH-Me
Desmorpholinyl ABT-263-NH-Me,Desmorpholinyl Navitoclax-NH-Me |
BCL | Apoptosis |
Desmorpholinyl Navitoclax-NH-Me (Desmorpholinyl ABT-263-NH-Me) is a Bcl-xL inhibitor, which can be employed alongside a CRBN ligand to synthesize XZ739, a PROTAC BCL-XL degrader [1] [2]. | |||
T19301 |
DUPA
N,N''-Carbonylbis[L-glutamic acid],(2S,2'S)-2,2'-Carbonylbis(Azanediyl)Dipentanedioic Acid |
Others; Ligands for Target Protein for PROTAC | Others; PROTAC |
DUPA (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。 | |||
T2066 |
Quizartinib
AC220,奎扎替尼 |
Apoptosis; FLT; Autophagy; Ligands for Target Protein for PROTAC | Angiogenesis; Apoptosis; Autophagy; PROTAC; Tyrosine Kinase/Adaptors |
Quizartinib (AC220) 是一种具有口服活性的高选择性Ⅱ 型 FLT3酪氨酸激酶抑制剂,可诱导细胞凋亡。它抑制 Wt FLT3 和 突变型 FLT3-ITD 自磷酸化,IC50分别为 4.1 nM 和 1.1 nM。它可通过优化的 linker 与 VHL 配体连接,从而形成 PROTAC Flt3 降解剂。 | |||
T15125 | Diethylene Glycol Monobenzyl Ether | Others | Others |
Diethylene Glycol Monobenzyl Ether is a PEG-based linker, specifically designed for the synthesis of PROTACs[1]. It serves as a versatile chemical compound, enabling the formation of PROTAC molecules by connecting target protein ligands with E3 ligase ligands, ultimately leading to targeted protein degradation. | |||
T17345 | 7-Octynoic acid | Others | Others |
7-Octynoic acid (compound 42) serves as a PROTAC linker for synthesizing various PROTACs, which are composed of two distinct ligands joined by this linker. One ligand interacts with an E3 ubiquitin ligase, while the other binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs selectively degrade target proteins[1]. | |||
T18542 |
Phthalimide-PEG3-C2-OTs
|
Others | Others |
Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker composed of PEGs. It is utilized in the synthesis of various PROTACs, which involve the connection of two distinct ligands through a linker. One ligand is specific for an E3 ubiquitin ligase, while the other ligand is designed for targeting the specific protein of interest. Through leveraging the intracellular ubiquitin-proteasome system, PROTACs are capable of selectively degrading target proteins [1]. | |||
T83953 |
Pomalidomide 4'-PEG5-amine
|
||
Pomalidomide 4'-PEG5-amine是一种功能化的cereblon配体,用于PROTAC研究与开发;它结合了一个E3连接酶配体和一个末端带有氨基的PEG5连接体,以便与目标蛋白配体进行共轭。它是专为PROTAC研发设计的一系列功能化工具分子之一。 | |||
T83954 |
VH 032 amide-alkylC7-acid
(S,R,S)-AHPC-amido-C7-acid |
||
VH 032 amide-alkylC7-acid 是一种用于PROTAC研究与开发的功能化Von-Hippel-Lindau蛋白配体(VHL),结合了E3连接酶配体和具有末端羧酸的alkylC7连接物,便于与目标蛋白配体偶联。该化合物是为PROTAC研发设计的一系列功能化工具分子之一。 |