Art. -Nr.: HY-162749A

G9D-4 TFA

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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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.44%
Formel: C₅₅H₇₆F₃N₉O₉
Molecular Weight:1064.24

Speicherung:

4°C, sealed storage, away from moisture

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

G9D-4 TFA Chemical Structure

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Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

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 KRAS^G12D-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.

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.

Chemical Information

Appearance Solid
Molecular Weight 1064.24
Formel C₅₅H₇₆F₃N₉O₉
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9396 mL

4.6982 mL

9.3964 mL

5 mM

0.1879 mL

0.9396 mL

1.8793 mL

10 mM

0.0940 mL

0.4698 mL

0.9396 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yunkai Shi, et al. Discovery of Potent and Selective G9a Degraders for the Treatment of Pancreatic Cancer. J Med Chem. 2024 Jul 23. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

PROTAC Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

G9D-4 TFA Related Classifications

HY-162749A Related Classifications