2. Epigenetics
  3. Epigenetic Reader Domain
  4. G-6599

G-6599 is a monovalent molecular glue-like degrader of SMARCA2/SMARCA4. G-6599 covalently binds to a specific cysteine residue of the E3 ligase FBXO22 in a biotransformation-independent manner, promotes the formation of a ternary complex with SMARCA2/A4, and achieves efficient and specific degradation of the two proteins via the ubiquitin-proteasome pathway. G-6599 is applicable to the research of androgen-dependent prostate cancer and mutant non-small cell lung cancer.

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

G-6599

G-6599 Chemical Structure

CAS No. : 2901806-51-5

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Based on 1 publication(s) in Google Scholar

G-6599 Related Antibodies

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Description

G-6599 is a monovalent molecular glue-like degrader of SMARCA2/SMARCA4. G-6599 covalently binds to a specific cysteine residue of the E3 ligase FBXO22 in a biotransformation-independent manner, promotes the formation of a ternary complex with SMARCA2/A4, and achieves efficient and specific degradation of the two proteins via the ubiquitin-proteasome pathway. G-6599 is applicable to the research of androgen-dependent prostate cancer and mutant non-small cell lung cancer[1].

In Vitro

G-6599 (20 h; 100 nM) potently and selectively degrades SMARCA2 and SMARCA4 in SW1573 cells via the ubiquitin-proteasome pathway, with no off-target degradation effects detected[1].
G-6599 (7 days) selectively inhibits the growth of LNCaP and NCI-H1944 cells with functional SMARCA2/A4, but shows no activity in NCI-H522 cells with defective SMARCA2/A4 function[1].

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

G-6599 Related Antibodies

Immunofluorescence[1]

Cell Line: SW1573 cells
Concentration: 100 nM
Incubation Time: 20 h
Result: Degraded SMARCA2 with a DC50 of 0.018 nM and Dmax of 97%.
Degraded SMARCA4 with a DC50 of 0.056 nM and Dmax of 95%.
Molecular Weight

523.67

Formula

C31H37N7O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

OC1=CC=CC=C1C2=CC(N3CC4N(C5=CC(C#CCCN6CCCCCC6)=NC=C5)C(CC4)C3)=C(N)N=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (190.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9096 mL 9.5480 mL 19.0960 mL
5 mM 0.3819 mL 1.9096 mL 3.8192 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 and light). 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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In Vivo Dissolution Calculator
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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 and light). 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 1.9096 mL 9.5480 mL 19.0960 mL 47.7400 mL
5 mM 0.3819 mL 1.9096 mL 3.8192 mL 9.5480 mL
10 mM 0.1910 mL 0.9548 mL 1.9096 mL 4.7740 mL
15 mM 0.1273 mL 0.6365 mL 1.2731 mL 3.1827 mL
20 mM 0.0955 mL 0.4774 mL 0.9548 mL 2.3870 mL
25 mM 0.0764 mL 0.3819 mL 0.7638 mL 1.9096 mL
30 mM 0.0637 mL 0.3183 mL 0.6365 mL 1.5913 mL
40 mM 0.0477 mL 0.2387 mL 0.4774 mL 1.1935 mL
50 mM 0.0382 mL 0.1910 mL 0.3819 mL 0.9548 mL
60 mM 0.0318 mL 0.1591 mL 0.3183 mL 0.7957 mL
80 mM 0.0239 mL 0.1193 mL 0.2387 mL 0.5967 mL
100 mM 0.0191 mL 0.0955 mL 0.1910 mL 0.4774 mL
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G-6599 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:

G-65992901806-51-5G6599G 6599Epigenetic Reader Domainubiquitin-proteasome pathwaySMARCA4FBXO22SMARCA4-mutant non-small cell lung cancerSW1573 cellsE3 ligaseandrogen-dependent prostate cancerSMARCA2cysteine residueInhibitorinhibitorinhibit

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