FKBP12 PROTAC dTAG-13
Based on 11 publication(s) in Google Scholar
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[1].
(Pink: FKBP12F36V ligand (HY-114420); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 2064175-41-1
- Formula: C57H68N4O15
- Molecular Weight:1049.17
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) FKBP12 PROTAC dTAG-13
More- Nat Commun. 2025 Jul 18;16(1):6631. [Abstract]
- Acta Pharm Sin B. 2023 Nov;13(11):4523-4534. [Abstract]
- Nat Struct Mol Biol. 2025 Jul 11. [Abstract]
- Proc Natl Acad Sci U S A. 2024 Jun 25;121(26):e2405905121. [Abstract]
- Stem Cell Res Ther. 2024 Sep 18;15(1):310. [Abstract]
- EMBO Rep. 2025 Mar;26(6):1528-1565. [Abstract]
- ACS Pharmacol Transl Sci. 2025 Nov 11;8(12):4410-4422. [Abstract]
- Drug Metab Dispos. 2025 May;53(5):100066. [Abstract]
- bioRxiv. 2026 May 21:2026.05.19.726384. [Abstract]
- bioRxiv. 2026 May 12.
- bioRxiv. 2025 Jun 19.
Customer Validation & Images
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IF
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RT-PCR
All PROTACs Isoforms
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Biological Activity
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FKBP12 |
Cereblon |
FKBP12 PROTAC dTAG-13 (0.00001-100 μM; 24 h) marginally modulates basal PXR-coregulator interactions but potently disrupts SPA70-induced PXR-NCoR complex formation in transfected HepG2 cells[1].
FKBP12 PROTAC dTAG-13 (10 μM, 0.3-30 μM; 24 h) acts as a partial PXR agonist to induce endogenous CYP3A4 expression in SNU-C4 and SNU719 cells, and partially inhibits Rifampicin (HY-B0272)-mediated CYP3A4 induction in SNU719 cells, without altering PXR or GAPDH RNA levels[1].
FKBP12 PROTAC dTAG-13 (0.1-10 μM; 30 min) potently induces CRBN-FKBP12F36V-PXR complex formation but does not induce CRBN-unfused PXR complex formation in transfected HepG2 cells[1].
FKBP12 PROTAC dTAG-13 (0.00001-100 μM; 24 h) retains partial agonist/antagonist activity for unfused PXR in transfected HepG2 cells regardless of CRBN co-expression, but its agonist activity is abolished and antagonistic activity is enhanced for FKBP12F36V-PXR when CRBN is co-overexpressed[1].
FKBP12 PROTAC dTAG-13 (1 µM; 1 h, 24 h, 48 h, 72 h) induces rapid, proteasome- and CRBN-dependent degradation of FKBP12F36V-KRASG12V in NIH/3T3 cells, rapidly reversing KRASG12V-driven signaling, morphology, cell cycle, and proliferation to basal cellular states[3].
FKBP12 PROTAC dTAG-13 (16 h) potently induces degradation of luciferase-FKBP12F36V in MV4;11 cells, as measured by reduced bioluminescence[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SNU-C4 cells, SNU719 cells
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Concentration:10 μM; 0.3-30 μM plus 5 μM rifampicin
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Incubation Time:24 h
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Result:Induced CYP3A4 RNA expression to ~1.5-2-fold of DMSO control levels in SNU-C4 cells.
Induced CYP3A4 RNA expression to ~3-5-fold of DMSO control levels in SNU719 cells.
Did not affect PXR or GAPDH RNA levels.
Incompletely blocked rifampicin-mediated CYP3A4 induction in a concentration-dependent manner in SNU719 cells.
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Cell Line:NIH/3T3 cells stably expressing FKBP12F36V-KRASG12V fusion constructs
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Concentration:1 µM
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Incubation Time:1 h, 24 h, 48 h, 72 h
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Result:Led to rapid degradation of FKBP12F36V-KRASG12V, with pMEK and pAKT levels reduced to baseline within 1 hour.
Pre-treatment with carfilzomib, MLN4924, or lenalidomide prevented degradation.
Treated cells reverted to control NIH/3T3 morphology within 24 hours, showed a reduction in S-phase cells to control levels within 48 hours, and exhibited significant anti-proliferative activity within 72 hours.
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUC0-t | AUC0-∞ | MRT0-∞ |
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| Mice[2] | 20 mg/kg | i.p. | 0.5 h | 1413.9 nM | 3.1 h | 6517.1 nM·h | 6655.0 nM·h | 4.1 h |
dTAG-13 (25 mg/kg; i.p.; single dose) induces significant, rapid, and reversible degradation of luciferase-FKBP12F36V in a mouse disseminated leukemia model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) (female, 8 weeks old, disseminated leukemia model via tail-vein injection of MV4;11 cells stably expressing luciferase-FKBP12F36V)[3]
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Dosage:25 mg/kg
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Administration:i.p.; single dose
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Result:Induced significant, rapid, and durable reduction in bioluminescent signal 4 hours after administration.
Recovered cellular bioluminescence to levels comparable to the vehicle treatment group 28 hours following the final treatment.
Chemical Information
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CAS No. 2064175-41-1
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Appearance Solid
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Molecular Weight 1049.17
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Formula C57H68N4O15
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Color White to light yellow
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SMILES
COC1=CC=C(CC[C@H](C2=C(OCC(NCCCCCCOC3=CC=CC4=C3C(N(C5CCC(NC5=O)=O)C4=O)=O)=O)C=CC=C2)OC([C@@H]6CCCCN6C([C@@H](CC)C7=CC(OC)=C(OC)C(OC)=C7)=O)=O)C=C1OC
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Synonyms
dTAG-13
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (11)
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Journal Impact Factor
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Most Recent
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Nat Commun
Systematic comparison and base-editing-mediated directed protein evolution and functional screening yield superior auxin-inducible degron technology. [Abstract]2025 Jul 18;16(1):6631. PMID: 40681502 -
Acta Pharm Sin B
The F-box-only protein 44 regulates pregnane X receptor protein level by ubiquitination and degradation. [Abstract]2023 Nov;13(11):4523-4534. PMID: 37969738
FKBP12 PROTAC dTAG-13 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Nov;13(11):4523-4534. [Abstract]
293T FBXO44 KO cells were transfected with FLAG-PXR and MYC-FKBPF36V-FBXO44 for 48 h, treated with the indicated doses (0-1 μM) of dTAG-13 for 24 h, and analyzed by Western blot
FKBP12 PROTAC dTAG-13 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Nov;13(11):4523-4534. [Abstract]
293T FBXO44 KO cells were transfected with FLAG-PXR and MYC-FKBPF36V-FBXO44 for 48 h, treated with the indicated doses (0-1 μM) of dTAG-13 for 24 h, and analyzed by RT-qPCR.
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Nat Struct Mol Biol
A heterotrimeric protein complex assembles the metazoan V-ATPase upon dissipation of proton gradients. [Abstract]2025 Jul 11. PMID: 40646309
FKBP12 PROTAC dTAG-13 purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2025 Jul 11. [Abstract]
HEK-293T cells expressing WDR7-dTAG-3xHA were pretreated with or without dTAG13 (1 μM, 0-60 min). Cell lysates were analyzed by SDS–PAGE and immunoblotting with the indicated antibodies.
FKBP12 PROTAC dTAG-13 purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2025 Jul 11. [Abstract]
HEK-293T cells expressing endogenous WDR7-dTAG-3xHA and stably expressing the antiporter VMAT2 were pretreated with or without dTAG13 (1 µM, 4 h).
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Proc Natl Acad Sci U S A
A MOZ-TIF2 leukemia mouse model displays KAT6-dependent H3K23 propionylation and overexpression of a set of active developmental genes. [Abstract]2024 Jun 25;121(26):e2405905121. PMID: 38889153 -
Stem Cell Res Ther
PROTAC-mediated vimentin degradation promotes terminal erythroid differentiation of pluripotent stem cells. [Abstract]2024 Sep 18;15(1):310. PMID: 39294765
FKBP12 PROTAC dTAG-13 purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2024 Sep 18;15(1):310. [Abstract]
dTAG-13 (1 μM, 24 h). Expression, re-localization, and degradation of HA-dTAG Vimentin were monitored by immunofluorescence and quantified by automated image analysis. Scale bar = 500 μm.
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EMBO Rep
A CRISPR-Cas9 screen reveals genetic determinants of the cellular response to decitabine. [Abstract]2025 Mar;26(6):1528-1565. PMID: 39930152 -
ACS Pharmacol Transl Sci
Metabolism, Pharmacokinetics, and Tissue Distribution of a Selective FK506-Binding Protein 12 F36V Mutant Degrader in Mice. [Abstract]2025 Nov 11;8(12):4410-4422. PMID: 41409176 -
Drug Metab Dispos
Applications of contemporary tools to measure plasma protein binding of targeted protein degraders. [Abstract]2025 May;53(5):100066. PMID: 40286535 -
bioRxiv
2026 May 21:2026.05.19.726384. PMID: 42239119 -
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Solvent & Solubility
DMSO : ≥ 100 mg/mL (95.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Huber AD, et al. PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. Structure. 2024;32(12):2352-2363.e8. [Content Brief]
[2]. Zhou S, et al. Metabolism, Pharmacokinetics, and Tissue Distribution of a Selective FK506-Binding Protein 12 F36V Mutant Degrader in Mice. ACS Pharmacol Transl Sci. 2025;8(12):4410-4422. Published 2025 Nov 11. [Content Brief]
[3]. Nabet B, et al. The dTAG system for immediate and target-specific protein degradation. Nat Chem Biol. 2018;14(5):431-441. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.9531 mL | 4.7657 mL | 9.5313 mL | 23.8284 mL |
| 5 mM | 0.1906 mL | 0.9531 mL | 1.9063 mL | 4.7657 mL | |
| 10 mM | 0.0953 mL | 0.4766 mL | 0.9531 mL | 2.3828 mL | |
| 15 mM | 0.0635 mL | 0.3177 mL | 0.6354 mL | 1.5886 mL | |
| 20 mM | 0.0477 mL | 0.2383 mL | 0.4766 mL | 1.1914 mL | |
| 25 mM | 0.0381 mL | 0.1906 mL | 0.3813 mL | 0.9531 mL | |
| 30 mM | 0.0318 mL | 0.1589 mL | 0.3177 mL | 0.7943 mL | |
| 40 mM | 0.0238 mL | 0.1191 mL | 0.2383 mL | 0.5957 mL | |
| 50 mM | 0.0191 mL | 0.0953 mL | 0.1906 mL | 0.4766 mL | |
| 60 mM | 0.0159 mL | 0.0794 mL | 0.1589 mL | 0.3971 mL | |
| 80 mM | 0.0119 mL | 0.0596 mL | 0.1191 mL | 0.2979 mL |
FKBP12 PROTAC dTAG-13 Related Classifications
HY-114421 Related Classifications
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