2. PROTAC Epigenetics Apoptosis
  3. PROTACs Histone Methyltransferase Apoptosis
  4. G9D-4 TFA

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).

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

G9D-4 TFA

G9D-4 TFA Chemical Structure

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of G9D-4 TFA:

G9D-4 TFA Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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[1]. (Pink: EHMT2/G9a/KMT1C ligand (HY-15273); Blue: Cereblon ligand (HY-10984); Black: linker).

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 (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.

G9D-4 TFA Related Antibodies

Western Blot Analysis[1]

Cell Line: PANC-1 cells
Concentration: 0.008, 0.04, 0.2, 1, 5, 10 μM (dose-response); 1 μM (time-course)
Incubation Time: 8 h (dose-response); 0, 2, 4, 6, 8, 16, 24 h (time-course)
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.

Apoptosis Analysis[1]

Cell Line: PANC-1 cells
Concentration: 5-12.5 μM (24 h); 10 μM (time-course)
Incubation Time: 24 h (dose-response); 12, 24, 48, 72 h (time-course)
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.

Western Blot Analysis[1]

Cell Line: ASPC-1 cells
Concentration: 0.008, 0.04, 0.2, 1, 5, 10, 15, 20 μM
Incubation Time: 8 h
Result: Induced dose-dependent G9a degradation with a DC50 of 0.2 μM.
Did not alter GLP protein levels.

Western Blot Analysis[1]

Cell Line: PANC-1 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Dose-dependently reduced G9a and H3K9me2 levels.
Dose-dependently increased γH2AX and cleaved PARP levels, indicating induction of DNA damage and apoptosis.

Cell Proliferation Assay[1]

Cell Line: ASPC-1, KP-4, Panc02.03, Panc10.05, HPAFII, Panc08.13 KRASG12D mutant pancreatic cancer cell lines
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)
Incubation Time: 72 h
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.

Cell Proliferation Assay[1]

Cell Line: KP-4, ASPC-1 cells
Concentration: 5-10 μM (alone); 5-10 μM (co-treated with 1-5 μM MRTX1133, respectively)
Incubation Time: 10-14 days
Result: Alone reduced colony formation. Combined with MRTX1133 almost completely eliminated colony formation, with a significantly greater effect than either single agent.

Apoptosis Analysis[1]

Cell Line: ASPC-1, KP-4 cells
Concentration: 10 μM (co-treated with 1 μM MRTX1133, ASPC-1); 10 μM (co-treated with 5 μM MRTX1133, KP-4)
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: ASPC-1 cells
Concentration: 10 μM (co-treated with 1 μM MRTX1133)
Incubation Time: 24 h
Result: Combined with MRTX1133 further reduced H3K9me2 levels and significantly increased γH2AX and cleaved PARP levels compared to either single agent.
Molecular Weight

1064.24

Formula

C55H76F3N9O9
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9396 mL 4.6982 mL 9.3964 mL
5 mM 0.1879 mL 0.9396 mL 1.8793 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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    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.
  • Protocol 2

    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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 (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
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G9D-4 TFA 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:

G9D-4PROTACsHistone MethyltransferaseApoptosisG9a PROTACs degraderASPC-1 cellsKP-4 cellsPANC-1 cellspancreatic cancer
Inhibitorinhibitorinhibit

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