Referencia número: HY-114421

FKBP12 PROTAC dTAG-13

Name: FKBP12 PROTAC dTAG-13
Brand: MedChemExpress
SKU: HY-114421
Price: 261.00 USD
Availability: InStock
Rating: 5 (12 reviews)

(Synonyms: dTAG-13)

12 Cited Publications

Revisión del cliente

Based on 12 publication(s) in Google Scholar

FKBP12 PROTAC dTAG-13 (dTAG-13) is a FKBP12^F36V PROTAC degrader and a PXR partial agonist. FKBP12 PROTAC dTAG-13 induces ubiquitination and proteasomal degradation of proteins tagged with FKBP12^F36V, 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).

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 99.89%
No. CAS: 2064175-41-1
Fòrmula: C₅₇H₆₈N₄O₁₅
Peso molecular:1049.17

Almacenamiento:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

FKBP12 PROTAC dTAG-13 Chemical Structure

No. CAS: 2064175-41-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (12)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo (2)
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

FKBP12 PROTAC dTAG-13 (dTAG-13) is a FKBP12^F36V PROTAC degrader and a PXR partial agonist. FKBP12 PROTAC dTAG-13 induces ubiquitination and proteasomal degradation of proteins tagged with FKBP12^F36V, 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]^[2]^[3]. (Pink: FKBP12F36V ligand (HY-114420); Blue: Cereblon ligand (HY-103596); Black: linker).

IC₅₀ & Target

^[1]

FKBP12

Cereblon

Ver todos los productos específicos de isoformas PROTACs :

In Vitro

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-FKBP12^F36V-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 FKBP12^F36V-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 FKBP12^F36V-KRAS^G12V in NIH/3T3 cells, rapidly reversing KRAS^G12V-driven signaling, morphology, cell cycle, and proliferation to basal cellular states^[3].
FKBP12 PROTAC dTAG-13 (16 h) potently induces degradation of luciferase-FKBP12^F36V 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. Further protocols information, click here.

Real Time qPCR^[1]

View Protocol

Cell Line:

SNU-C4 cells, SNU719 cells
Concentration:

10 μM; 0.3-30 μM plus 5 μM rifampicin
Incubation Time:

24 h
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.

Western Blot Analysis^[3]

View Protocol

Cell Line:

NIH/3T3 cells stably expressing FKBP12F36V-KRASG12V fusion constructs
Concentration:

1 µM
Incubation Time:

1 h, 24 h, 48 h, 72 h
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.

Parmacokinetics

Species	Dose	Route	T_max	C_max	T_1/2	AUC_0-t	AUC_0-∞	MRT_0-∞
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

In Vivo

FKBP12 PROTAC dTAG-13 (20 mg/kg; i.p.; single dose) exhibits rapid absorption, sustained systemic exposure for 4 hours, broad tissue distribution (excluding the brain), extensive phase I metabolism, and efficient clearance in male C57BL/6NJ mice, supporting its use for short-term, peripheral targeted protein degradation studies^[2].
dTAG-13 (25 mg/kg; i.p.; single dose) induces significant, rapid, and reversible degradation of luciferase-FKBP12^F36V in a mouse disseminated leukemia model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD.Cg-Prkdc^scid Il2rg^tm1Wjl/SzJ (NSG) (female, 8 weeks old, disseminated leukemia model via tail-vein injection of MV4;11 cells stably expressing luciferase-FKBP12^F36V)^[3]
Dosage:

25 mg/kg
Administration:

i.p.; single dose
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

No. CAS 2064175-41-1
Appearance Solid
Peso molecular 1049.17
Fòrmula C₅₇H₆₈N₄O₁₅
Color White to light yellow
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
Synonyms

dTAG-13
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (12)

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Journal Impact Factor

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.
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).
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.
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
SSRN

2026 Aug 19.
bioRxiv

2026 May 12.
bioRxiv

A bulk cell heterozygous knock-in strategy for targeted protein degradation. [Abstract]

2026 May 21:2026.05.19.726384. PMID: 42239119
bioRxiv

2025 Jun 19.

Solvente y solubilidad

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9531 mL

4.7657 mL

9.5313 mL

5 mM

0.1906 mL

0.9531 mL

1.9063 mL

10 mM

0.0953 mL

0.4766 mL

0.9531 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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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

Protocolo

All Molecular Biology Animals and Diseases

RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

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FKBP12 PROTAC dTAG-13

12 Cited Publications

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FKBP12 PROTAC dTAG-13

Publications Citing Use of MedChemExpress (MCE) FKBP12 PROTAC dTAG-13

Ver todos los productos específicos de isoformas PROTACs