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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T18610 | PROTAC FKBP Degrader-3 | Others | Others |
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an VHL binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader[1]. | |||
T14298 |
Rimiducid
|
Apoptosis; Others; Fatty Acid Synthase | Apoptosis; Metabolism; Others |
Rimiducid 是一种可渗透脂质的他克莫司类似物,是一种二聚剂,通过交联 FKBP 结构域起作用。它将 Caspase 9 自杀开关二聚化并迅速诱导细胞凋亡。 | |||
T13884 |
Shield-1
|
Others | Others |
Shield-1 是 FK506 结合蛋白 12 (FKBP) 的特异性、高亲和力和细胞渗透性配体,通过与突变的 FKBP (mtFKBP) 结合来逆转不稳定性,允许 mtFKBP 融合蛋白的条件表达。它可以稳定整个融合蛋白。 | |||
T14299 |
AP20187
B/B Homodimerizer |
Others | Others |
AP20187 (B/B Homodimerizer) 是一种细胞渗透性配体,用于二聚化 FK506 结合蛋白 (FKBP) 融合蛋白。它启动生物信号级联和基因表达或破坏蛋白质-蛋白质相互作用。 | |||
T1784 |
Everolimus
依维莫司,RAD001,SDZ-RAD |
Apoptosis; Others; mTOR; Autophagy | Apoptosis; Autophagy; Others; PI3K/Akt/mTOR signaling |
Everolimus (SDZ-RAD) 是 Rapamycin 的衍生物,也是一种口服活性的mTOR1选择性抑制剂。它与FKBP-12结合可产生免疫抑制复合物,还抑制肿瘤细胞增殖并诱导细胞凋亡和自噬,有免疫抑制和抗癌活性。 | |||
T11451 |
GPI-1046
1-(1,2-二氧代-3,3-二甲基戊基)-L脯氨酸-(3-吡啶基)-丙酯 |
Others; HIV Protease | Microbiology/Virology; Others; Proteases/Proteasome |
GPI-1046 是一种无抗生素作用的亲免素配体,部分通过上调 PFC 和 NAc 核心中的谷氨酸转运蛋白 1 来减少乙醇摄入。 | |||
T13694 |
FKBP12 PROTAC RC32
RC32 |
Others | Others |
FKBP12 PROTAC RC32 contains conjugation of Rapamycin and a ligand for an E3 ubiquitin ligase.FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. | |||
T2567 |
Etonogestrel
3-Oxodesogestrel,3-keto-Desogestrel,依托孕烯,Nexplanon,Implanon |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Progesterone Receptor; Endogenous Metabolite | Endocrinology/Hormones; Metabolism; Others |
Etonogestrel (Implanon) 是孕激素去氧孕烯的生物活性代谢物,与靶器官中的孕酮受体和雌激素受体高亲和力地结合,可诱导FKBP51mRNA 和蛋白表达。它是一种甾体孕激素,用作激素避孕药。 | |||
T71840 |
FKBP12-IN-Q2
|
||
FKBP12-IN-Q2 is an inhibitor of FKBP12. | |||
T11291 |
FKBP12 PROTAC dTAG-13
dTAG-13 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN. FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader. | |||
T11292 |
FKBP12 PROTAC dTAG-7
dTAG-7 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by connecting BET bromodomains to the E3 ubiquitin ligase CRBN. Additionally, it serves as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein. | |||
T79184 | FKBP51F67V-selective antagonist Ligand2 | FKBP | Apoptosis; Autophagy; Immunology/Inflammation |
FKBP51F67V-selective antagonist Ligand2(示例3-3)是针对杏仁核中由FKBP51 F67V过表达引起的焦虑表型的有效逆转剂。本物质特异性地结合到FKBP51 F67V,与野生型FKBP51及FKBP52无亲和力。 | |||
T18597 |
dFKBP-1
|
Others | Others |
dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF of FKBP12, the Thalidomide based cereblon ligand and a linker[1]. | |||
T6033 |
Zotarolimus
ABT-578,佐他莫司,咗他莫司,A 179578 |
mTOR | PI3K/Akt/mTOR signaling |
Zotarolimus (ABT-578) 是一种免疫抑制剂,是雷帕霉素的衍生物,具有抗增殖活性。它被专门开发作为局部输送支架用于预防冠状动脉再狭窄。 | |||
T2648 |
Pimecrolimus
SDZ-ASM 981,ASM 981,吡美莫司 |
Others | Others |
Pimecrolimus (SDZ-ASM 981) 是一种免疫亲和素配体,能与胞质受体特异性的结合。 | |||
T24788 |
Shield-2
|
||
Shield-2 is a potent FKBP-derived destabilizing domain stabilizing ligand. | |||
T13549 | AP1867-3-(aminoethoxy) | Others | Others |
AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader. | |||
T13914 |
SLF-amido-C2-COOH
PROTAC FKBP12-binding moiety 1 |
Others | Others |
SLF-amido-C2-COOH is a synthetic ligand for FKBP (SLF), and can be used in the synthesis of PROTACs. | |||
T13888 |
SLF
|
Others | Others |
SLF is a synthetic ligand for FK506-binding protein (FKBP)( with an affinity of 3.1 μM for FKBP51 and an IC50 of 0.22 μM for FKBP12). SLF can be used in the synthesis of PROTAC. | |||
T73817 | SLF TFA | ||
SLF TFA 是 FK506 结合蛋白 (FKBP) 的合成配体,对FKBP51的亲和力为 3.1 μM,对FKBP12的IC50为 2.6 μM,可用于合成PROTAC 分子。 | |||
T80928 |
TSPO ligand-3
|
AUTACs | PROTAC |
TSPO ligand-3为AUTAC2的配体,其中AUTAC2包含p-氟苄基鸟嘌呤(FBnG)及FKBP合成配体(SLF)两部分,能在HeLa细胞中显著沉默FKBP12蛋白。 | |||
T74026 |
AUTAC2
|
||
AUTAC2 是一种 FKBP12靶向自噬介导降解体 (AUTAC)。AUTAC2 包含一个 FBnG 和 SLF 部分,其中 SLF 与 FKBP12 非共价结合。 | |||
T76622 |
Suc-Ala-Leu-Pro-Phe-pNA
|
||
Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA) 是一种 FK-506 结合蛋白 (FKBP) 的底物。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2144 |
Tacrolimus
他克莫司,Fujimycin,FK506,FR900506 |
Phosphatase; Others; Antibacterial; Antibiotic; mTOR; Autophagy | Autophagy; Metabolism; Microbiology/Virology; Others; PI3K/Akt/mTOR signaling |
Tacrolimus (Fujimycin) 可与 FKBP12 结合形成高亲和力复合物 (Ki: 0.2 nM),抑制钙/钙调蛋白依赖性蛋白磷酸酶的活性。 | |||
T1537 |
Rapamycin
Sirolimus,AY 22989,雷帕霉素,NSC-2260804 |
Others; Endogenous Metabolite; Antibiotic; mTOR; Autophagy; Antifungal | Autophagy; Metabolism; Microbiology/Virology; Others; PI3K/Akt/mTOR signaling |
Rapamycin (AY 22989) 属于大环内酯类天然产物,是一种 mTOR 抑制剂,具有特异性(HEK293 细胞:IC50=0.1 nM)。Rapamycin 具有免疫抑制活性,并能诱导自噬。 | |||
T2481 |
Ascomycin
FK520,Immunomycin,子囊霉素,FR-900520 |
Phosphatase; Others; Antibiotic; Parasite; Antifungal | Metabolism; Microbiology/Virology; Others |
Ascomycin (Immunomycin) 是 Tacrolimus 的乙基类似物,具有免疫抑制特性。它也是一种大环聚酮类抗生素,具有抗疟疾、抗真菌和抗痉挛等多种生物活性。它可防止移植排斥,并具有用于各种皮肤病研究的潜力。 | |||
T20879 |
Tacrolimus monohydrate
FK-506,FR 900506,Prograf,FR900506,Tacrolimus hydrate,LCP-Tacro,他克莫司一水合物,FK 506 |
Phosphatase; Others; Antibacterial; Antibiotic; Autophagy | Autophagy; Metabolism; Microbiology/Virology; Others |
Tacrolimus monohydrate (LCP-Tacro) 是大环内酯类化合物,它与 FK506 结合蛋白 (FKBP) 结合形成复合物并抑制钙调神经磷酸酶,从而抑制 T 淋巴细胞信号转导和 IL-2 转录。具有强免疫抑制特性。 |