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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T14593 | Biotin-PEG3-Mal | Others | Others |
Biotin-PEG3-Mal is a biotinylated polyethylene glycol (PEG) derivative used as a linker in the synthesis of proteolysis targeting chimeras (PROTACs). By introducing the biotin moiety, it enables specific recognition and binding to target proteins. Additionally, the PEG spacer contributes to improved solubility and flexibility of the linker. This compound offers a valuable tool for constructing PROTACs, which hold great potential in targeted protein degradation strategies[1]. | |||
T82870 |
Biotin-PEG-Alk (MW 3400)
|
||
Biotin-PEG-Alk (MW 3400)是一种具有生物素标记的PEG化合物,用于酶辅因子的生物素(Biotin)标记蛋白质,同时含有亲水性低毒的聚乙二醇(PEG)基团和可进行叠氮反应的无环(不论是否含有支链)脂肪烃Alk基(Alkyne)。此化合物作为点击化学试剂,其Alkyne基团能够通过铜催化的叠氮-炔环加成反应(CuAAc)与含Azide基团的分子高效结合。 |