FKBP Degrader
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FKBP12 PROTAC dTAG-13
0 ImagesSynonyms: dTAG-13FKBP12 PROTAC dTAG-13 (dTAG-13) is a FKBP12F36V PROTAC degrader and a PXR partial agonist. FKBP12 PROTAC dTAG-13 induces ubiquitination and proteasomal degradation of proteins tagged with FKBP12F36V, without degrading wild-type FKBP12 or un-fused PXR. It weakly promotes the recruitment of SRC-1, strongly inhibits the interaction between NCoR and PXR, and upregulates the expression of CYP3A4 and other drug metabolism-related genes. FKBP12 PROTAC dTAG-13 is applicable to research related to breast cancer and leukemia[1].
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PROTAC FKBP Degrader-3
0 ImagesPROTAC FKBP Degrader-3 is a selective FKBP PROTAC degrader with an IC50 of 1.8 nM. PROTAC FKBP Degrader-3 targets and degrades the FKBP protein by recruiting the VHL E3 ligase, and this degradation process is primarily mediated by K11 and K48 ubiquitin chain linkages. PROTAC FKBP Degrader-3 can be applied in cancer research.
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SP3N hydrochloride
0 ImagesCat. No.: HY-161794APurity: 99.84%SP3N hydrochloride is a specific degrader of the prolyl isomerase FKBP12. As a prodrug, SP3N hydrochloride is metabolized by Diamine oxidase into the active aldehyde metabolite SP3CHO (HY-161795). SP3N hydrochloride induces the proximity of FKBP12 to the SCFFBXO22 E3 ligase complex, thereby triggering the polyubiquitination and proteasomal degradation of FKBP12. SP3N hydrochloride can be used in cancer research.
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dTAGV-1 TFA
0 ImagesdTAGV-1 TFA is a selective FKBP12F36V PORTAC degrader. dTAGV-1 TFA induces rapid degradation of FKBP12F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 TFA is applicable to functional validation studies of cancer and undegradable oncoproteins.
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dTAGV-1 hydrochloride
0 ImagesdTAGV-1 hydrochloride is a selective FKBP12F36V PORTAC degrader. dTAGV-1 hydrochloride induces rapid degradation of FKBP12F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 hydrochloride is applicable to functional validation studies of cancer and undegradable oncoproteins.
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dTAG-47
0 ImagesdTAG-47 is a heterobifunctional PROTAC degrader that specifically binds to the FKBP12F36V domain and Cereblon (CRBN). By recruiting the CRBN E3 ubiquitin ligase, dTAG-47 induces ubiquitination and proteasomal degradation of FKBP12F36V-fused Cas9 and tagged KDM5A. dTAG-47 can induce upregulated expression of some endogenous retrovirus (ERV) genes and is suitable for cancer research.
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dTAGV-1
0 ImagesdTAGV-1 is a selective FKBP12F36V PORTAC degrader. dTAGV-1 induces rapid degradation of FKBP12F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 is applicable to functional validation studies of cancer and undegradable oncoproteins.
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22-SLF
0 ImagesCat. No.: HY-163807CAS No.: 3079209-82-522-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC50 of 0.5 µM. 22-SLF interacts with C227 and C228 in FBXO22 to induce a ternary complex between FKBP12 and FBXO22, and degrades FKBP12 in a FBXO22-dependent manner. 22-SLF can be used for fundamental cancer research as a probe to study the FBXO22 degradation pathway.
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SP3N
0 ImagesCat. No.: HY-161794SP3N is a specific degrader of the prolyl isomerase FKBP12. As a prodrug, SP3N is metabolized by Diamine oxidase into the active aldehyde metabolite SP3CHO (HY-161795). SP3N induces the proximity of FKBP12 to the SCFFBXO22 E3 ligase complex, thereby triggering the polyubiquitination and proteasomal degradation of FKBP12. SP3N can be used in cancer research.
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10-SLF
0 ImagesCat. No.: HY-173082CAS No.: 2765058-89-510-SLF is an FKBP12 PROTAC degrader. 10-SLF covalently interacts with the cysteine residue of FBXW7R465C, forms a ternary complex with FKBP12, and promotes FBXW7-R465C-dependent proteasomal degradation of FKBP12. 10-SLF can be used for the research of pancreatic cancer.
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SelDeg51
0 ImagesCat. No.: HY-181289CAS No.: 3036372-80-9SelDeg51 is a selective FKBP51 PROTAC degrader with a Kd value of 18 nM and a Dmax of 90%. SelDeg51 induces proteasomal degradation of FKBP51 via the FKBP51:SelDeg51:VCB ternary complex and reactivates the glucocorticoid receptor signaling pathway. SelDeg51 can be used for research on stress-related mental disorders, chronic pain, and obesity.
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FKBP12 PROTAC FM4
0 ImagesFKBP12 PROTAC FM4 is a PROTAC degrader of FKBP12, with a DC50 value of 0.09-0.22 nM. FKBP12 PROTAC FM4 inhibits global protein synthesis, induces apoptosis, and selectively reduces the viability of cervical cancer cells expressing MTH1-E6 and FKBP12F36V-tagged SARS1. FKBP12 PROTAC FM4 is applicable to research related to HPV-positive cervical cancer.
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MC-25B
0 ImagesCat. No.: HY-170983MC-25B is a DCAF16-recruiting FKBP12 PROTAC degrader with a DC50 of 0.35 μM. MC-25B promotes the formation of a ternary complex with DCAF16 and nuclear-localized FKBP12_NLS, thereby mediating DCAF16-dependent degradation of FKBP12_NLS via the proteasome and Cullin-RING ligase pathway.
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RAFKBP12
0 ImagesCat. No.: HY-181498CAS No.: 2375455-59-5RAFKBP12 is a FKBP12 CAP-TAC (proteinase complex cap-targeted chimera) degrader. RAFKBP12 demonstrates the feasibility of the CAP-TAC strategy, which enables proteasome-dependent degradation of FKBP12 that is independent of E3 ubiquitin ligases and protein ubiquitination.
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dTAGV-1 TFA (Standard)
0 ImagesCat. No.: HY-145514RCAS No.: 2624313-15-9dTAGV-1 TFA (Standard) is the analytical standard of dTAGV-1 TFA (HY-145514). This product is intended for research and analytical applications. dTAGV-1 TFA is a selective FKBP12F36V PORTAC degrader. dTAGV-1 TFA induces rapid degradation of FKBP12F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 TFA is applicable to functional validation studies of cancer and undegradable oncoproteins.
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FKBP12 PROTAC dTAG-13 (Standard)
0 ImagesCat. No.: HY-114421RCAS No.: 2064175-41-1Synonyms: dTAG-13 (Standard)FKBP12 PROTAC dTAG-13 (Standard) is the analytical standard of FKBP12 PROTAC dTAG-13 (HY-114421). This product is intended for research and analytical applications. FKBP12 PROTAC dTAG-13 (dTAG-13) is a FKBP12F36V PROTAC degrader and a PXR partial agonist. FKBP12 PROTAC dTAG-13 induces ubiquitination and proteasomal degradation of proteins tagged with FKBP12F36V, without degrading wild-type FKBP12 or un-fused PXR. It weakly promotes the recruitment of SRC-1, strongly inhibits the interaction between NCoR and PXR, and upregulates the expression of CYP3A4 and other drug metabolism-related genes. FKBP12 PROTAC dTAG-13 is applicable to research related to breast cancer and leukemia.
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dTAG-Fluorescein
0 ImagesCat. No.: HY-183439CAS No.: 2365116-48-7dTAG-Fluorescein is a dTAG-class PROTAC conjugated with fluorescein. dTAG-Fluorescein is applicable to homogeneous time-resolved fluorescence (HTRF) competitive displacement binding assays to detect binding affinity with His-FKBP12F36V. dTAG-Fluorescein can recruit VHL or CRBN E3 ligase complexes, thereby specifically driving the selective degradation of FKBP12F36V-tagged proteins, with very limited activity against FKBP12WT and IKZF1.
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