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Cat. No.: HY-143332

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TRIM24/BRPF1-IN-2

TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC₅₀ values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 3033288-68-2
Formule: C₂₀H₂₂N₂O₄S
Masse moléculaire:386.46

Stockage:

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

TRIM24/BRPF1-IN-2 Chemical Structure

CAS No.: 3033288-68-2

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Quantité

Amount: USD 0.00

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Protocole (1)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

BRPF1

1.16 μM (IC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	0.82 μM Compound: 20l	Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by Cell Titer-Glo assay Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by Cell Titer-Glo assay	[PMID: 35385803]
LNCaP	IC₅₀	1.07 μM Compound: 20l	Antiproliferative activity against human LNCaP cells measured after 96 hrs by Cell Titer-Glo assay Antiproliferative activity against human LNCaP cells measured after 96 hrs by Cell Titer-Glo assay	[PMID: 35385803]
LNCaP C4-2B	IC₅₀	0.78 μM Compound: 20l	Antiproliferative activity against human LNCaP C4-2B cells measured after 96 hrs by Cell Titer-Glo assay Antiproliferative activity against human LNCaP C4-2B cells measured after 96 hrs by Cell Titer-Glo assay	[PMID: 35385803]

In Vitro

TRIM24/BRPF1-IN-2 (compound 20l) (0-10 μM, 48 h) suppresses the growth of the prostate cell lines (C4-2B, LNCaP, and 22Rv1), with IC₅₀ values of 0.78±0.15, 1.07±0.47, and 0.82±0.26 μM, respectively^[1].
TRIM24/BRPF1-IN-2 inhibits gene and protein expression in prostate cancer cells^[1].
TRIM24/BRPF1-IN-2 displays reasonable Caco-2 permeability^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

RT-PCR^[1]

View Protocol

Cell Line:

22Rv1 cell, LNCaP cells
Concentration:

0.4, 2, 5, and 10 μM
Incubation Time:

48 h
Result:

Decreased the mRNA expression of full-length AR, AR-V7 and AR-regulated genes PSA, KLK2 and TMPRSS2. inhibited the mRNA level of C-MYC.

In Vivo

TRIM24/BRPF1-IN-2 (compound 20l) (50 mg/kg, IP, once daily for 21 days) suppresses tumor growth (TGI = 53%) without exhibiting noticeable toxicity^[1].

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

Animal Model:

Mice (n = 5-7 per dose group, Four-week-old, male, non-obese diabetic server combined immune-deficiency (NOD SCID), 22Rv1 xenograft model)^[1]
Dosage:

50 mg/kg
Administration:

IP, once daily for 21 days
Result:

Inhibited the progression of the tumors significantly (53% tumor growth inhibition) without body weight loss.

Chemical Information

CAS No. 3033288-68-2
Appearance Solid
Masse moléculaire 386.46
Formule C₂₀H₂₂N₂O₄S
Color White to off-white
SMILES

COC1=CC=C(C=C1S(=O)(NC2=CC=C3C(CCN3C(C)=O)=C2)=O)C4CC4
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Protocole

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 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)
Instruction de manipulation (2659 KB)

Références

[1]. Xiang Q, et al. Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors. Eur J Med Chem. 2022 Jun 5;236:114311. [Content Brief]

Calculators

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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.

Bioz

Keywords

MOQ

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100 mg

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