dTAGV-1 hydrochloride
Based on 6 publication(s) in Google Scholar
dTAGV-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.
(Pink: FKBP12 ligand (HY-114420); Blue: VHL ligand (HY-112078); Black: linker (HY-W012001)).
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 2624313-16-0
- Formula: C68H91ClN6O14S
- Molecular Weight:1284.00
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Publications Citing Use of MedChemExpress (MCE) dTAGV-1 hydrochloride
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Biological Activity
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FKBP12 |
VHL |
dTAGV-1 (500 nM; 1-24 h) hydrochloride rapidly degrades FKBP12F36V-KRASG12V and blocks downstream signaling in PATU-8902 FKBP12F36V-KRASG12V; KRAS-/- cells, with its activity dependent on the VHL and proteasome pathways[1].
dTAGV-1 (50-5000 nM; 24 h) hydrochloride potently degrades FKBP12F36V-EWS/FLI and reverses aberrant EWS/FLI-mediated signaling pathways in EWS502 FKBP12F36V-EWS/FLI; EWS/FLI-/- cells, with a hook effect observed at the concentration of 5000 nM[1].
dTAGV-1 (0.1-10 μM; 120 h) hydrochloride reduces the 3D sphere proliferation capacity of PATU-8902 FKBP12F36V-KRASG12V; KRAS-/- cells[1].
dTAGV-1 (1 μM; 0-6 days) hydrochloride inhibits the proliferation of EWS502 FKBP12F36V-EWS/FLI and EWS/FLI-/- cells[1].
Treatment of A549 RPB1dTAG cells with dTAGV-1 (100 nM; 4-12 h) hydrochloride effectively degrades GFP-tagged wild-type RNAPII, enabling acute replacement with Doxycycline (HY-N0565) hydrochloride-induced HA-tagged RNAPII phosphorylation site mutants under conditions where their expression levels match those of wild-type RNAPII[2].
dTAGV-1 (500 nM; 0-48 h) hydrochloride induces rapid degradation of FOCAD protein in MIAPACA2 cells, which in turn causes post-translational depletion of SKIV2L, TTC37 and AVEN proteins without affecting their RNA levels[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PATU-8902 LACZ-FKBP12F36V
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Concentration:500 nM (in combination with 125-2000 nM THAL-SNS-032 (HY-123937))
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Incubation Time:24 h
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Result:Alone, did not alter CDK9 protein levels.
In combination with THAL-SNS-032, led to pronounced degradation of both LACZ-FKBP12F36V and CDK9 at levels comparable to treatment with each degrader alone, avoiding substrate competition effects.
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Cell Line:PATU-8902 FKBP12F36V-KRASG12V; KRAS-/- (3D-spheroid suspensions)
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Concentration:0.1, 1, 10, 100 nM, 1, 10 μM
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Incubation Time:120 h
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Result:Diminished 3D-spheroid cell proliferation to levels comparable to CRBN-recruiting dTAG molecules.
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Cell Line:A549 cells expressing GFP-FKBP12F36V-tagged wild-type RNAPII (RPB1dTAG) with inducible HA-tagged RNAPII mutants (WT, Y1F, S2A, T4V, S5A, S7A)
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Concentration:100 nM
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Incubation Time:4 h; 12 h
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Result:Rapidly degraded GFP-tagged wild-type RPB1 after 4 hours of treatment.
Confirmed HA-tagged RNAPII mutants were expressed at levels comparable to wild-type RNAPII.
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) (8-week-old female, immunocompromised, leukemia model via tail vein injection of MV4;11 luc-FKBP12F36V cells)[1]
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Dosage:35 mg/kg
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Administration:i.p.; daily; 3 consecutive days
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Result:Induced striking loss of bioluminescent signal 4 hours after the first administration.
Maintained consistent loss of bioluminescent signal 4 hours after each of the three administrations.
Showed evident degradation of bioluminescent signal 28 hours after the final administration.
Chemical Information
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CAS No. 2624313-16-0
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Appearance Solid
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Molecular Weight 1284.00
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Formula C68H91ClN6O14S
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Color White to off-white
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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.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Nature
2025 Feb;638(8052):1095-1103. PMID: 39910291
dTAGV-1 hydrochloride 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.
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Sci Adv
FeaSion decodes the regulatory landscape and functional diversity of RNA polymerase II CTD phosphorylation. [Abstract]2025 Nov 28;11(48):eadz2345. PMID: 41313762
dTAGV-1 hydrochloride 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.
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dTAGV-1 hydrochloride 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.
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Solvent & Solubility
DMSO : 100 mg/mL (77.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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)
Purity & Documentation
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Data Sheet (281 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]. Nabet B, et al. Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nature communications. 2020 Sep 18;11(1):4687. [Content Brief]
[2]. Zhu J, et al. FeaSion decodes the regulatory landscape and functional diversity of RNA polymerase II CTD phosphorylation. Science advances. 2025 Nov 28;11(48):eadz2345. [Content Brief]
[3]. Prindle V, et al. Synthetic lethality of mRNA quality control complexes in cancer. Nature. 2025 Feb;638(8052):1095-1103. [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 | 0.7788 mL | 3.8941 mL | 7.7882 mL | 19.4704 mL |
| 5 mM | 0.1558 mL | 0.7788 mL | 1.5576 mL | 3.8941 mL | |
| 10 mM | 0.0779 mL | 0.3894 mL | 0.7788 mL | 1.9470 mL | |
| 15 mM | 0.0519 mL | 0.2596 mL | 0.5192 mL | 1.2980 mL | |
| 20 mM | 0.0389 mL | 0.1947 mL | 0.3894 mL | 0.9735 mL | |
| 25 mM | 0.0312 mL | 0.1558 mL | 0.3115 mL | 0.7788 mL | |
| 30 mM | 0.0260 mL | 0.1298 mL | 0.2596 mL | 0.6490 mL | |
| 40 mM | 0.0195 mL | 0.0974 mL | 0.1947 mL | 0.4868 mL | |
| 50 mM | 0.0156 mL | 0.0779 mL | 0.1558 mL | 0.3894 mL | |
| 60 mM | 0.0130 mL | 0.0649 mL | 0.1298 mL | 0.3245 mL |
dTAGV-1 hydrochloride Related Classifications
HY-145514C Related Classifications
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