1. Epigenetics
  2. Epigenetic Reader Domain
  3. 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.

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TRIM24/BRPF1-IN-2

TRIM24/BRPF1-IN-2 Chemische Struktur

CAS. Nr. : 3033288-68-2

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Beschreibung

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[1].

IC50 & Target

BRPF1

1.16 μM (IC50)

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.

RT-PCR[1]

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.
Molekulargewicht

386.46

Formel

C20H22N2O4S

CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

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

Versand

Room temperature in continental US; may vary elsewhere.

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

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Art. -Nr.:
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