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

G9D-4 is a G9a PROTAC degrader. G9D-4 induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 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

G9D-4 Chemical Structure

CAS No. : 3097803-96-5

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G9D-4 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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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

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Description

G9D-4 is a G9a PROTAC degrader. G9D-4 induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 can be used for research on pancreatic cancer[1]. (Pink: EHMT2/G9a/KMT1C ligand (HY-15273); Blue: Cereblon ligand (HY-10984); Black: linker).

IC50 & Target

Cereblon

 

In Vitro

G9D-4 (0.008-20 μM; 0-24 h) 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) reduces the level of H3K9me2 in PANC-1 cells[1].
G9D-4 (1 μM; 8 h) induces G9a degradation in PANC-1 cells. This process requires the formation of a G9a-G9D-4-CRBN ternary complex and is dependent on the neddylation-proteasome pathway[1].
G9D-4 (72 h) 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. It also inhibits the growth of 22Rv1 cells, with an IC50 of 9.9 μM[1].
G9D-4 (0.1-12.5 μM; 24 h) induces apoptosis in PANC-1 cells, downregulates G9a and H3K9me2, and upregulates γH2AX and cleaved PARP[1].
G9D-4 (0-15 μM; 72 h) 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) 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 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

950.22

Formula

C53H75N9O7
CAS No.
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
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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G9D-4 Related Classifications

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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-43097803-96-5PROTACsHistone MethyltransferaseApoptosisG9a PROTACs degraderASPC-1 cellsKP-4 cellsPANC-1 cellspancreatic cancer
Inhibitorinhibitorinhibit

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