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23

抑制剂 & 化合物

4

天然产物

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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。

化合物

PROTAC FKBP Degrader-3
Cat.No: T18610
Synonym:
Target: Others
Rimiducid
Cat.No: T14298
Synonym:
Target: Apoptosis, Others, Fatty Acid Synthase
Shield-1
Cat.No: T13884
Synonym:
Target: Others
AP20187
Cat.No: T14299
Synonym: B/B Homodimerizer
Target: Others
Everolimus
Cat.No: T1784
Synonym: 依维莫司,RAD001,SDZ-RAD
Target: Apoptosis, Others, mTOR, Autophagy
GPI-1046
Cat.No: T11451
Synonym: 1-(1,2-二氧代-3,3-二甲基戊基)-L脯氨酸-(3-吡啶基)-丙酯
Target: Others, HIV Protease
FKBP12 PROTAC RC32
Cat.No: T13694
Synonym: RC32
Target: Others
Etonogestrel
Cat.No: T2567
Synonym: 3-Oxodesogestrel,3-keto-Desogestrel,依托孕烯,Nexplanon,Implanon
Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Progesterone Receptor, Endogenous Metabolite
FKBP12-IN-Q2
Cat.No: T71840
Synonym:
Target:
FKBP12 PROTAC dTAG-13
Cat.No: T11291
Synonym: dTAG-13
Target: Epigenetic Reader Domain
FKBP12 PROTAC dTAG-7
Cat.No: T11292
Synonym: dTAG-7
Target: Epigenetic Reader Domain
FKBP51F67V-selective antagonist Ligand2
Cat.No: T79184
Synonym:
Target: FKBP
dFKBP-1
Cat.No: T18597
Synonym:
Target: Others
Zotarolimus
Cat.No: T6033
Synonym: ABT-578,佐他莫司,咗他莫司,A 179578
Target: mTOR
Pimecrolimus
Cat.No: T2648
Synonym: SDZ-ASM 981,ASM 981,吡美莫司
Target: Others
Shield-2
Cat.No: T24788
Synonym:
Target:
AP1867-3-(aminoethoxy)
Cat.No: T13549
Synonym:
Target: Others
SLF-amido-C2-COOH
Cat.No: T13914
Synonym: PROTAC FKBP12-binding moiety 1
Target: Others
SLF
Cat.No: T13888
Synonym:
Target: Others
SLF TFA
Cat.No: T73817
Synonym:
Target:
TSPO ligand-3
Cat.No: T80928
Synonym:
Target: AUTACs
AUTAC2
Cat.No: T74026
Synonym:
Target:
Suc-Ala-Leu-Pro-Phe-pNA
Cat.No: T76622
Synonym:
Target:
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。

天然产物

Tacrolimus
Cat.No: T2144
Synonym: 他克莫司,Fujimycin,FK506,FR900506
Target: Phosphatase, Others, Antibacterial, Antibiotic, mTOR, Autophagy
Rapamycin
Cat.No: T1537
Synonym: Sirolimus,AY 22989,雷帕霉素,NSC-2260804
Target: Others, Endogenous Metabolite, Antibiotic, mTOR, Autophagy, Antifungal
Ascomycin
Cat.No: T2481
Synonym: FK520,Immunomycin,子囊霉素,FR-900520
Target: Phosphatase, Others, Antibiotic, Parasite, Antifungal
Tacrolimus monohydrate
Cat.No: T20879
Synonym: FK-506,FR 900506,Prograf,FR900506,Tacrolimus hydrate,LCP-Tacro,他克莫司一水合物,FK 506
Target: Phosphatase, Others, Antibacterial, Antibiotic, Autophagy
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