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Search Results for " fkbp12 "

25

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T71840	FKBP12-IN-Q2
	FKBP12-IN-Q2 is an inhibitor of FKBP12.
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.
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.
T18611	AP1867-2-(carboxymethoxy) PROTAC FKBP12-binding moiety 2	Others	Others
	AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG molecules[1].
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.
T40031	Thalidomide-O-C6-NH2 hydrochloride 4-((6-aminohexyl)oxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride,萨力多胺-O-C6-氨基盐酸盐	E3 Ligase Ligand-Linker Conjugate	PROTAC
	Thalidomide-O-C6-NH2 hydrochloride (4-((6-aminohexyl)oxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride) 是一种合成的E3 连接酶配体 -linker 偶联物，用于 PROTAC dTAG-13 的合成。其中 dTAG-13 是一种 FKBP12F36V 和 BET 的降解剂。
T74025	AUTAC1	AUTACs	PROTAC
	AUTAC1是一种 MetAP2 靶向自噬介导降解体 (AUTAC)，具有潜在的抗癌活性，可降解 MetAP2 和 FKBP12 蛋白，可用于合成 PROTAC。
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。
T9950	ElteN378	mTOR	PI3K/Akt/mTOR signaling
	Elte N378 是一种高效的合成 FKBP12 抑制剂，Ki 为 0.5 nM，是一种低原子量配体，其亲和力与大环内酯类雷帕霉素相当。
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。
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].
T40251	dTAGV-1 TFA
	dTAGV-1 TFA is a highly effective and specific compound that targets mutant FKBP12 F36V fusion proteins for degradation. It possesses potent activity in inducing the degradation of the FKBP12 F36V -Nluc protein in living organisms.
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。
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。
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。
T74556	dTAG-47
	dTAG-47，异双功能 dTAG 分子，靶向突变型 FKBP12 (FKBP12F36V)。FKBP12F36V 可用作降解标签 (dTAG) 并与靶蛋白融合。dTAG-47可用于基底样乳腺癌（BBC）的研究。
T18061	KB02-SLF	Others	Others
	KB02-SLF is a PROTAC-based nuclear FKBP12 degrader, known as a molecular glue. It facilitates the degradation of nuclear FKBP12 by covalently modifying DCAF16, an E3 ligase. Moreover, KB02-SLF enhances the longevity of protein degradation in biological systems. The compound SLF acts as a linker, binding to the ubiquitin E3 ligase ligand KB02, resulting in the formation of KB02-SLF[1].
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.
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.
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。
T81743	mTORC1-IN-1	mTOR	PI3K/Akt/mTOR signaling
	mTORC1-IN-1（compound T1）为一种rapalog及选择性mTORC1抑制剂，调节细胞生长和代谢，与多种疾病如癌症相关。该化合物通过与FKBP12-FRB复合物结合（对接分数−11.6 kcal/mol）来靶向mTORC1。
T13734	ILS-920	Others	Others
	ILS-920 is a Rapamycin analog characterized by diminished immunosuppressive effects but remarkable neuroprotective properties. It exhibits selective binding affinity towards the immunophilin FKBP52 as well as the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 displays a notable 200-fold preference for FKBP52 over FKBP12.
T74412	dTAGV-1-NEG TFA
	dTAGV-1-NEG TFA 是一种非对映异构体，是 dTAGV-1 的异双功能阴性对照。dTAGV-1-NEG TFA 是一种 FKBP12F36V 选择性降解剂。
T36253	dTAGV-1
	Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells. Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use. Negative control...

化合物

Cat.No: T71840

FKBP12 PROTAC RC32

Cat.No: T13694

Synonym: RC32

Target: Others

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

AP1867-2-(carboxymethoxy)

Cat.No: T18611

Synonym: PROTAC FKBP12-binding moiety 2

Target: Others

SLF-amido-C2-COOH

Cat.No: T13914

Synonym: PROTAC FKBP12-binding moiety 1

Target: Others

Thalidomide-O-C6-NH2 hydrochloride

Cat.No: T40031

Synonym: 4-((6-aminohexyl)oxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride,萨力多胺-O-C6-氨基盐酸盐

Target: E3 Ligase Ligand-Linker Conjugate

Cat.No: T74025

Target: AUTACs

Cat.No: T14298

Target: Apoptosis, Others, Fatty Acid Synthase

Cat.No: T9950

Target: mTOR

Cat.No: T6033

Synonym: ABT-578,佐他莫司,咗他莫司,A 179578

Target: mTOR

Cat.No: T18597

Target: Others

Cat.No: T40251

Cat.No: T73817

Cat.No: T1784

Synonym: 依维莫司,RAD001,SDZ-RAD

Target: Apoptosis, Others, mTOR, Autophagy

Cat.No: T74026

Cat.No: T74556

Cat.No: T18061

Target: Others

Cat.No: T13888

Target: Others

AP1867-3-(aminoethoxy)

Cat.No: T13549

Target: Others

Cat.No: T80928

Target: AUTACs

Cat.No: T81743

Target: mTOR

Cat.No: T13734

Target: Others

dTAGV-1-NEG TFA

Cat.No: T74412

Cat.No: T36253

Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
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。

天然产物

Cat.No: T2481

Synonym: FK520,Immunomycin,子囊霉素,FR-900520

Target: Phosphatase, Others, Antibiotic, Parasite, Antifungal

Cat.No: T1537

Synonym: Sirolimus,AY 22989,雷帕霉素,NSC-2260804

Target: Others, Endogenous Metabolite, Antibiotic, mTOR, Autophagy, Antifungal

Cat.No: T2144

Synonym: 他克莫司,Fujimycin,FK506,FR900506

Target: Phosphatase, Others, Antibacterial, Antibiotic, mTOR, Autophagy

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