G9D-4 TFA
Based on 1 Customer Validation
G9D-4 TFA is a G9a PROTAC degrader. G9D-4 TFA induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 TFA exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 TFA can be used for research on pancreatic cancer.
(Pink: EHMT2/G9a/KMT1C ligand (HY-15273); Blue: Cereblon ligand (HY-10984); Black: linker).
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- Pureté: 99.44%
- Formule: C55H76F3N9O9
- Masse moléculaire:1064.24
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
G9D-4 (0.008-20 μM; 0-24 h) TFA induces G9a degradation in PANC-1 and ASPC-1 cells, with DC50 values of 0.1 μM and 0.2 μM, respectively. It accelerates the degradation of G9a protein in PANC-1 cells without altering GLP protein levels[1].
G9D-4 (0.04-10 μM; 24 h) TFA reduces the level of H3K9me2 in PANC-1 cells[1].
G9D-4 (1 μM; 8 h) TFA induces G9a degradation in PANC-1 cells. This process requires the formation of a G9a-G9D-4 TFA-CRBN ternary complex and is dependent on the neddylation-proteasome pathway[1].
G9D-4 (72 h) TFA inhibits the cell growth of a panel of pancreatic cancer cell lines (KP-4, PANC-1, ASPC-1, HPAF-II, Panc10.05, SW1990, Panc08.13, Panc04.03, Panc05.04, and Panc02.03 cells), with IC50 values ranging from 12 to 32 μM, also inhibits the growth of 22Rv1 cells, with an IC50 of 9.9 μM[1].
G9D-4 (0.1-12.5 μM; 24 h) TFA induces apoptosis in PANC-1 cells, downregulates G9a and H3K9me2, and upregulates γH2AX and cleaved PARP[1].
G9D-4 (0-15 μM; 72 h) TFA enhances the inhibitory effect of MRTX1133 (HY-134813) on cell proliferation of KRASG12D-mutant pancreatic cancer cell lines (ASPC-1 cells and KP-4 cells), and synergistically induces cell apoptosis[1].
G9D-4 (5-10 μM; 10−14 days) TFA significantly enhances the colony formation inhibitory activity of MRTX1133 in KP-4 cells, and exerts a synergistic inhibitory effect on long-term cell proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1 cells
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Concentration:0.008, 0.04, 0.2, 1, 5, 10 μM (dose-response); 1 μM (time-course)
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Incubation Time:8 h (dose-response); 0, 2, 4, 6, 8, 16, 24 h (time-course)
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Result:Induced dose-dependent G9a degradation with a DC50 of 0.1 μM. Did not alter GLP protein levels.
Triggered G9a degradation starting after 8 h and continuing through 24 h.
Selectively and dose-dependently reduced H3K9me2 levels.
Induced significant G9a degradation as early as 4 h.
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Cell Line:PANC-1 cells
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Concentration:5-12.5 μM (24 h); 10 μM (time-course)
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Incubation Time:24 h (dose-response); 12, 24, 48, 72 h (time-course)
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Result:Induced significant apoptosis in a dose-dependent manner at 24 h, with ~70% of cells apoptotic at 12.5 μM.
Caused time-dependent apoptosis at 10 μM, with ~60% of cells apoptotic at 72 h.
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Cell Line:ASPC-1 cells
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Concentration:0.008, 0.04, 0.2, 1, 5, 10, 15, 20 μM
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Incubation Time:8 h
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Result:Induced dose-dependent G9a degradation with a DC50 of 0.2 μM.
Did not alter GLP protein levels.
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Cell Line:PANC-1 cells
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Concentration:0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Dose-dependently reduced G9a and H3K9me2 levels.
Dose-dependently increased γH2AX and cleaved PARP levels, indicating induction of DNA damage and apoptosis.
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Cell Line:ASPC-1, KP-4, Panc02.03, Panc10.05, HPAFII, Panc08.13 KRASG12D mutant pancreatic cancer cell lines
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Concentration:30 μM starting concentration, 1.2-fold serial dilutions (ASPC-1); 20 μM starting concentration, 1.2-fold serial dilutions (KP-4); fixed concentrations (co-treated with MRTX1133)
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Incubation Time:72 h
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Result:Combined with MRTX1133 showed strong synergistic antiproliferative activity. Had all CI values below 0.8 (ED50, ED75, ED90), with ED90 CI values below 0.4 across all tested cell lines.
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Cell Line:KP-4, ASPC-1 cells
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Concentration:5-10 μM (alone); 5-10 μM (co-treated with 1-5 μM MRTX1133, respectively)
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Incubation Time:10-14 days
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Result:Alone reduced colony formation. Combined with MRTX1133 almost completely eliminated colony formation, with a significantly greater effect than either single agent.
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Cell Line:ASPC-1, KP-4 cells
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Concentration:10 μM (co-treated with 1 μM MRTX1133, ASPC-1); 10 μM (co-treated with 5 μM MRTX1133, KP-4)
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Incubation Time:24 h
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Result:Combined with MRTX1133 induced significantly higher levels of apoptosis than either single agent.
Triggered ~75% apoptosis in ASPC-1 cells. Triggered ~30% apoptosis in KP-4 cells.
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Cell Line:ASPC-1 cells
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Concentration:10 μM (co-treated with 1 μM MRTX1133)
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Incubation Time:24 h
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Result:Combined with MRTX1133 further reduced H3K9me2 levels and significantly increased γH2AX and cleaved PARP levels compared to either single agent.
Chemical Information
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Appearance Solid
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Masse moléculaire 1064.24
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Formule C55H76F3N9O9
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Color Light yellow to yellow
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SMILES
COC1=CC2=C(C=C1OCCCN3CCCC3)N=C(C4CCCCC4)N=C2NC5CCN(CC5)CCCC(NCCCCCCCCCNC6=C(C7=CC=C6)C(N(C7=O)C8C(NC(CC8)=O)=O)=O)=O.OC(C(F)(F)F)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 200 mg/mL (187.93 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (4.70 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (4.70 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture). 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 | 0.9396 mL | 4.6982 mL | 9.3964 mL | 23.4909 mL |
| 5 mM | 0.1879 mL | 0.9396 mL | 1.8793 mL | 4.6982 mL | |
| 10 mM | 0.0940 mL | 0.4698 mL | 0.9396 mL | 2.3491 mL | |
| 15 mM | 0.0626 mL | 0.3132 mL | 0.6264 mL | 1.5661 mL | |
| 20 mM | 0.0470 mL | 0.2349 mL | 0.4698 mL | 1.1745 mL | |
| 25 mM | 0.0376 mL | 0.1879 mL | 0.3759 mL | 0.9396 mL | |
| 30 mM | 0.0313 mL | 0.1566 mL | 0.3132 mL | 0.7830 mL | |
| 40 mM | 0.0235 mL | 0.1175 mL | 0.2349 mL | 0.5873 mL | |
| 50 mM | 0.0188 mL | 0.0940 mL | 0.1879 mL | 0.4698 mL | |
| 60 mM | 0.0157 mL | 0.0783 mL | 0.1566 mL | 0.3915 mL | |
| 80 mM | 0.0117 mL | 0.0587 mL | 0.1175 mL | 0.2936 mL | |
| 100 mM | 0.0094 mL | 0.0470 mL | 0.0940 mL | 0.2349 mL |
G9D-4 TFA Related Classifications
HY-162749A Related Classifications
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