2. PROTAC Cell Cycle/DNA Damage Autophagy Apoptosis Immunology/Inflammation
  3. PROTACs FKBP
  4. dTAGV-1

dTAGV-1 is a potent and selective degrader of FKBP12F36V-tagged proteins PROTAC degrader. dTAGV-1 can induce degradation of FKBP12F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A)).

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

CAS No. : 2451573-86-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of dTAGV-1:

dTAGV-1 Related Antibodies

Top Publications Citing Use of Products

    dTAGV-1 purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8052):1095-1103.  [Abstract]

    dTAGV-1 hydrochloride (500 nM; 0-48 h) depleted FOCAD protein levels within four hours. Following FOCAD degradation, levels of SKIV2L, TTC37 and AVEN protein decreased by 8 h, reaching a maximum by 2 days in MIAPACA2 FOCAD-dTAG cells.

    dTAGV-1 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Nov 28;11(48):eadz2345.  [Abstract]

    Western blot analysis of total RNAPII, degraded RPB1 (tagged with GFP), and RNAPIImut (tagged with HA; WT, Y1F, S2A, T4V, S5A and S7A) levels before and after Doxycycline (Dox) or dTAGV-1 TFA (100 nM) treatment. α-Tubulin served as the loading control.

    dTAGV-1 purchased from MedChemExpress. Usage Cited in: Mayo Clinic. 2025.

    Representative Western blot analysis of KLF5 after 250 nM dTAGV-1 TFA treatment for 0, 1, 4 and 24 h. HSC70 was used as a loading control.

    View All PROTACs Isoform Specific Products:

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    von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    dTAGV-1 is a potent and selective degrader of FKBP12F36V-tagged proteins PROTAC degrader. dTAGV-1 can induce degradation of FKBP12F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A))[1].

    IC50 & Target

    FKBP12

     

    In Vitro

    dTAGV-1 (0.1 nM-10 μM; 24 h) induces potent degradation of FKBP12F36V-Nluc with no effects on FKBP12WT-Nluc in 293FT cells[1].

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

    dTAGV-1 Related Antibodies
    In Vivo

    dTAGV-1 (35 mg/kg; i.p; 3 days) TFA induces degradation of FKBP12F36V-Nluc in mice[1].
    Pharmacokinetic Analysis in Mice (non-salt form)[1]

    Route Dose (mg/kg) Tmax (hr) t1/2 (hr) Cmax (ng/mL) AUClast (hr·ng/mL) AUCinf (hr·ng/mL) CL (mL/min/kg) Vss (L/kg)
    i.v. 2 0.08 3.02 7780 3245 3329 10.1 0.56
    i.p. 10 2.00 4.43 2123 18088 18517 9.05 /
    i.p. 2 1.67 3.64 595 2245 3136 10.7 /

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

    Animal Model: 8-week-old immunocompromised female mice were transplanted with MV4;11 luc-FKBP12F36V cells[1]
    Dosage: 35 mg/kg
    Administration: Intraperitoneal injection (i.p.); once daily for 3 days
    Result: Significantly reduced the bioluminescent signal 4 h after the first administration. The signal continuously decreased 4 h after each of the three administrations, and degradation was still evident 28 h after the final administration.
    Molecular Weight

    1247.54

    Formula

    C68H90N6O14S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@H]1N(CCCC1)C([C@H](C2=CC(OC)=C(C(OC)=C2)OC)CC)=O)O[C@@H](C3=C(C=CC=C3)OCC(NCCCCCCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)=O)=O)=O)CCC7=CC(OC)=C(C=C7)OC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 75 mg/mL (60.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.8016 mL 4.0079 mL 8.0158 mL
    5 mM 0.1603 mL 0.8016 mL 1.6032 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    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 (2.00 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

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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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    +
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    %
    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
    References

    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
    DMSO 1 mM 0.8016 mL 4.0079 mL 8.0158 mL 20.0394 mL
    5 mM 0.1603 mL 0.8016 mL 1.6032 mL 4.0079 mL
    10 mM 0.0802 mL 0.4008 mL 0.8016 mL 2.0039 mL
    15 mM 0.0534 mL 0.2672 mL 0.5344 mL 1.3360 mL
    20 mM 0.0401 mL 0.2004 mL 0.4008 mL 1.0020 mL
    25 mM 0.0321 mL 0.1603 mL 0.3206 mL 0.8016 mL
    30 mM 0.0267 mL 0.1336 mL 0.2672 mL 0.6680 mL
    40 mM 0.0200 mL 0.1002 mL 0.2004 mL 0.5010 mL
    50 mM 0.0160 mL 0.0802 mL 0.1603 mL 0.4008 mL
    60 mM 0.0134 mL 0.0668 mL 0.1336 mL 0.3340 mL
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    dTAGV-1 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.

    Keywords:

    dTAGV-12451573-86-5dTAGV1dTAGV 1PROTACsFKBPFK506-binding proteinFKBP12F36VdegradationInhibitorinhibitorinhibit

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