G9D-4 TFA |
Catalog No.GC80876
One-Click Copy Product Info
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G9D-4 TFA is a G9a PROTAC degrader.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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In Vitro, 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 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].
References:
[1]. Yunkai Shi, et al. Discovery of Potent and Selective G9a Degraders for the Treatment of Pancreatic Cancer. J Med Chem. 2024 Jul 23.
| Cas No. | SDF | ||
| Formula | C55H76F3N9O9 | M.Wt | 1064.24 |
| Solubility | DMSO: 200 mg/mL (187.93 mM; Need ultrasonic) | Storage | Store at 4°C, away from moisture |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 939.6 μL | 4.6982 mL | 9.3964 mL |
| 5 mM | 187.9 μL | 939.6 μL | 1.8793 mL |
| 10 mM | 94 μL | 469.8 μL | 939.6 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)