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Referencia número: 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)).

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Pureza: 99.84%
No. CAS: 3057627-63-8
Fòrmula: C₃₂H₂₇N₇O₉
Peso molecular:653.60

Almacenamiento:

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

GT-653 Chemical Structure

No. CAS: 3057627-63-8

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Fluorescent Dye

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

Actividad biológica
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- IC₅₀ & Target
- In Vitro
Chemical Information
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Bioz

Actividad biológica

Descripciòn

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

Ver todos los productos específicos de isoformas Histone Demethylase :

Ver todos los productos específicos de isoformas PROTACs :

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

No. CAS 3057627-63-8
Appearance Solid
Peso molecular 653.60
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (269 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Instrucciones de manejo (2659 KB)

Referencias

[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

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

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100 mg

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GT-653

Ver todos los productos específicos de isoformas Histone Demethylase

Ver todos los productos específicos de isoformas PROTACs

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

GT-653 Related Classifications

HY-158432 Related Classifications