FKBP12 PROTAC dTAG-13 (Synonyms: dTAG-13)

Name: FKBP12 PROTAC dTAG-13
Brand: MedChemExpress
SKU: HY-114421
Rating: 5.0 (11 reviews)

Cat. No.: HY-114421 Purity: 99.89%: Data Sheet
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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].

For research use only. We do not sell to patients.

CAS No. : 2064175-41-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Customer Review

Based on 11 publication(s) in Google Scholar

11 Publications Citing Use of MCE FKBP12 PROTAC dTAG-13

RT-PCR

Flow Cytometry

: 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).

: 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.

: 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

FKBP12

Cereblon

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.

Real Time qPCR^[1]

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]

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.

Molecular Weight

1049.17

Formula

C₅₇H₆₈N₄O₁₅

CAS No.

2064175-41-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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:

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Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.89%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (248 KB) HNMR (148 KB) RP-HPLC (169 KB) LCMS (233 KB)

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

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

FKBP12 PROTAC dTAG-13 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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FKBP12 PROTAC dTAG-13 (Synonyms: dTAG-13)

Customer Review

FKBP12 PROTAC dTAG-13 Related Antibodies

11 Publications Citing Use of MCE FKBP12 PROTAC dTAG-13

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References

Customer Review

FKBP12 PROTAC dTAG-13 Related Antibodies

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Complete Stock Solution Preparation Table

FKBP12 PROTAC dTAG-13 Related Classifications

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