[CAS NO. 1627929-55-8] PLX51107
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PRODUCTS SPECIFICATIONS [1627929-55-8]
Store
Catalog
SLK-S8739
Brand
Selleck
CAS
1627929-55-8
DESCRIPTION [1627929-55-8]
Overview
| MDL | MFCD31657388 |
|---|---|
| Molecular Weight | 438.48 |
| Molecular Formula | C26H22N4O3 |
| SMILES | O=C(O)C1=CC=C(C2=CN([C@H](C3=NC=CC=C3)C)C4=CC(C5=C(C)ON=C5C)=CN=C42)C=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2806 mL | 11.4030 mL | 22.8061 mL |
| 5 mM | 0.4561 mL | 2.2806 mL | 4.5612 mL |
| 10 mM | 0.2281 mL | 1.1403 mL | 2.2806 mL |
| 50 mM | 0.0456 mL | 0.2281 mL | 0.4561 mL |
Description
PLX51107 is as a novel inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).
Targets
In vitro
In a set of cell cultures, short-term (4h) treatment of PLX51107 result in robust change in PD markers but do not induce an immediate apoptotic response. Induction of apoptosis occurrs after prolonged treatment (16 hours or more of continuous exposure). PLX51107 induces accumulation of p21 and IκBα, reduced levels of cMYC, and modulation of pro- and anti-apoptotic proteins.
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