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Cat. No.: HY-158432

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GT-653

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GT-653 is a selective KDM5B PROTAC degrader. GT-653 induces ubiquitination and degradation of KDM5B without altering the transcriptional level of KDM5B. GT-653 upregulates the level of H3K4me3. GT-653 activates the type I Interferon signaling pathway. GT-653 can be used for the research of prostate cancer.
(Pink: KDM5B ligand (HY-158433); Blue: Cereblon ligand (HY-103596); Black: linker (HY-W004896)).

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

Purity: 99.84%
CAS No.: 3057627-63-8
Formula: C₃₂H₂₇N₇O₉
Molecular Weight:653.60

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GT-653 Chemical Structure

CAS No.: 3057627-63-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

GT-653 is a selective KDM5B PROTAC degrader. GT-653 induces ubiquitination and degradation of KDM5B without altering the transcriptional level of KDM5B. GT-653 upregulates the level of H3K4me3. GT-653 activates the type I Interferon signaling pathway. GT-653 can be used for the research of prostate cancer^[1]. (Pink: KDM5B ligand (HY-158433); Blue: Cereblon ligand (HY-103596); Black: linker (HY-W004896)).

IC₅₀ & Target^[1]

Cereblon

All Histone Demethylase Isoforms :

All PROTACs Isoforms :

In Vitro

GT-653 potently degrades the KDM5B protein in 22RV1 prostate cancer cells, with a degradation rate of 68.35%^[1].
GT-653 (0.1-20.0 μM; 24 h) dose-dependently decreases KDM5B protein levels and increases H3K4me3 levels in 22RV1 prostate cancer cells without altering KDM5B transcription^[1].
Co-incubation with GT-653 (20 μM; 12 h) and MG132 (HY-13259) induces the formation of the KDM5B-CRBN complex in 22RV1 prostate cancer cells^[1].
GT-653 (0.1-20.0 μM; 24 h, 48 h) does not significantly reduce the viability of 22RV1 prostate cancer cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

22RV1 prostate cancer cells
Concentration:

0.1-20.0 μM
Incubation Time:

24 h, 48 h
Result:

Showed no significant effect on cell viability at any tested concentration compared to control.

Chemical Information

CAS No. 3057627-63-8
Appearance Solid
Molecular Weight 653.60
Formula C₃₂H₂₇N₇O₉
Color White to off-white
SMILES

N#CC1=C2NC(C3=CC=C(C=C3)OCC(NCCOCCOC4=CC=CC5=C4C(N(C5=O)C6CCC(NC6=O)=O)=O)=O)=CC(N2N=C1)=O
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

References

[1]. Guan T, et al. Discovery of an efficacious KDM5B PROTAC degrader GT-653 up-regulating IFN response genes in prostate cancer. European journal of medicinal chemistry. 2024 Jun 05;272:116494. [Content Brief]

Calculators

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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.

MOQ

Minimum order quantity

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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GT-653

PROTAC Library

MCE Bioactive Compound Library

All Histone Demethylase Isoforms

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

GT-653

PROTAC Library

MCE Bioactive Compound Library

All Histone Demethylase Isoforms

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

GT-653 Related Classifications

HY-158432 Related Classifications