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.
For research use only. We do not sell to patients.
- CAS No.: 3033288-68-2
- Formula: C20H22N2O4S
- Molecular Weight:386.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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BRPF1 1.16 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
0.82 μM
Compound: 20l
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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
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[PMID: 35385803] |
| LNCaP | IC50 |
1.07 μM
Compound: 20l
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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
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[PMID: 35385803] |
| LNCaP C4-2B | IC50 |
0.78 μM
Compound: 20l
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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] |
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.
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Cell Line:22Rv1 cell, LNCaP cells
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Concentration:0.4, 2, 5, and 10 μM
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Incubation Time:48 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:50 mg/kg
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Administration:IP, once daily for 21 days
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Result:Inhibited the progression of the tumors significantly (53% tumor growth inhibition) without body weight loss.
Chemical Information
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CAS No. 3033288-68-2
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Appearance Solid
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Molecular Weight 386.46
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Formula C20H22N2O4S
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Color White to off-white
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SMILES
COC1=CC=C(C=C1S(=O)(NC2=CC=C3C(CCN3C(C)=O)=C2)=O)C4CC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (273 KB)
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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)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)