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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Based on 1 publication(s) in Google Scholar

PROTAC G9a/GLP degrader 1 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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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 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

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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 (0.1-10 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
Appearance

Solid

Color

White to light yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (92.48 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 0.9248 mL 4.6239 mL 9.2479 mL
5 mM 0.1850 mL 0.9248 mL 1.8496 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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. 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 0.9248 mL 4.6239 mL 9.2479 mL 23.1197 mL
5 mM 0.1850 mL 0.9248 mL 1.8496 mL 4.6239 mL
10 mM 0.0925 mL 0.4624 mL 0.9248 mL 2.3120 mL
15 mM 0.0617 mL 0.3083 mL 0.6165 mL 1.5413 mL
20 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1560 mL
25 mM 0.0370 mL 0.1850 mL 0.3699 mL 0.9248 mL
30 mM 0.0308 mL 0.1541 mL 0.3083 mL 0.7707 mL
40 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5780 mL
50 mM 0.0185 mL 0.0925 mL 0.1850 mL 0.4624 mL
60 mM 0.0154 mL 0.0771 mL 0.1541 mL 0.3853 mL
80 mM 0.0116 mL 0.0578 mL 0.1156 mL 0.2890 mL
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PROTAC G9a/GLP degrader 1 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:

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

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