2. PROTAC Epigenetics GPCR/G Protein
  3. PROTACs Histone Methyltransferase GLP Receptor
  4. PROTAC G9a/GLP degrader 1

PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468)).

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

PROTAC G9a/GLP degrader 1

PROTAC G9a/GLP degrader 1 Chemical Structure

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PROTAC G9a/GLP degrader 1 Related Antibodies

Top Publications Citing Use of Products

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

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Description

PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468))[1].

IC50 & Target[1]

G9a

336 nM (DC50)

GLP

988 nM (DC50)

VHL

 

In Vitro

PROTAC G9a/GLP degrader 1 (Compound 4) (0.03-10 μM, 0-72 h) exhibits potent and persistent G9a/GLP degrading ability and effectively reduces the level of the catalytic product H3K9me2 of G9a in breast cancer MCF-7 cells[1].
PROTAC G9a/GLP degrader 1 (01-10 μM, 24-72 h) significantly inhibits the migration ability of MCF-7 cells, but does not significantly affect the viability of MCF-7 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC G9a/GLP degrader 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.03, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 0, 3, 6, 12, 24, 48 and 72 h
Result: Initiated the degradation of G9a/GLP within 6 hours and persisted for at least 72 hour.
Effectively reduced the level of the catalytic product H3K9me2 of G9a.

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 72 h
Result: Did not reduce the MCF-7 cell viability.

Cell Migration Assay [1]

Cell Line: MCF-7 cells
Concentration: 3 μM
Incubation Time: 24 h
Result: Suppressed the migration of MCF-7 cells.
Molecular Weight

1081.33

Formula

C57H76N8O11S
SMILES

O=C(CCOCCOCCOCCNC(C1=CC=C(C=C1)NC([C@H](CCC2CC2)NC(C3=C(C4=C(N3)CC(C)(C)CC4=O)C)=O)=O)=O)N[C@H](C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C=C6)C7=C(N=CS7)C)=O)=O)C(C)(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC G9a/GLP degrader 1 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:

PROTAC G9a/GLP degrader 1PROTACsHistone MethyltransferaseGLP ReceptorPROTACRK-701H3K9me2MCF-7Chemical ProbeInhibitorinhibitorinhibit

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