1. Epigenetics
  2. Epigenetic Reader Domain

BAY-299 

Cat. No.: HY-107424 Purity: 99.24%
Handling Instructions

BAY-299 is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.

For research use only. We do not sell to patients.

BAY-299 Chemical Structure

BAY-299 Chemical Structure

CAS No. : 2080306-23-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
25 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 280 In-stock
Estimated Time of Arrival: December 31
100 mg USD 490 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BAY-299 is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.

IC50 & Target[1]

BRPF2 BD

67 nM (IC50)

BRPF1 BD

3150 nM (IC50)

BRPF3 BD

5550 nM (IC50)

TAF1 BD2

8 nM (IC50)

TAF1L BD2

106 nM (IC50)

In Vitro

BAY-299 is a dual inhibitor of the bromodomain and PHD finger (BRPF) family member BRPF2 and the TATA box binding protein-associated factors TAF1 and TAF1L. TR-FRET assays showed that BAY-299 is a potent inhibitor of BRPF2 BD with an IC50 of 67 nM, and a selectivity of 47- and 83-fold over BRPF1 and BRPF3 BDs. The profile of BAY-299 is further confirmed by AlphaScreen assay, where an IC50 of 97 nM and a selectivity of 23- and 25-fold over BRPF1 and BRPF3 BDs are measured. NanoBRET experiments show that the interaction of BRPF2 BD with histones H4 and H3.3 is blocked by BAY-299 with IC50 values of 575 and 825 nM, respectively. For TAF1 BD2, the IC50 values are 970 and 1400 nM, respectively. No inhibitory effect is observed for the interaction between BRPF1 or BRD4 and histone H4 up to 10 μM for BAY-299. BAY-299 inhibits MOLM-13, MV4-11, 769-P, Jurkat, NCI-H526, CHL-1, and 5637 cells proliferation with GI50s of 1060, 2630, 3210, 3900, 6860, 7400, and 7980 nM, respectively[1].

In Vivo

Studies of the in vivo pharmacokinetic properties of BAY-299 in rat reveal that blood clearance is low (ca. 17% of hepatic blood flow), volume of distribution in steady-state high, terminal half-life long to very long (t1/2=10 h), and bioavailability high (F=73%). In vivo blood clearance is as anticipated based on rat liver microsome values but lower than expected based on hepatocyte data[1].

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (58.21 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3285 mL 11.6423 mL 23.2845 mL
5 mM 0.4657 mL 2.3285 mL 4.6569 mL
10 mM 0.2328 mL 1.1642 mL 2.3285 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

MOLM-13, MV4-11, 769-P, Jurkat, NCI-H526, CHL-1, and 5637 cell lines are treated with BAY-299 while in the logarithmic growth phase, and their viability is determined by AlamarBlue staining[1].

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

Animal Administration
[1]

Rats[1]
BAY-299 is administered to three male Wistar rats per arm, either intravenously or intragastrally formulated as solutions. BAY-299 is given as i.v. bolus, and blood samples are taken at 2 min, 8 min, 15 min, 30 min, 45 min, 1 h, 2 h, 4 h, 6 h, 8 h, and 24 h after dosing. For pharmacokinetics after intragastral administration, BAY-299 is given intragastrally to fasted rats and blood samples are taken at 5 min, 15 min, 30 min, 45 min, 1 h, 2 h, 4 h, 6 h, 8 h, and 24 h after dosing. Blood is collected into lithium-heparin tubes and centrifuged for 15 min at 3000 rpm[1].

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

References
Molecular Weight

429.47

Formula

C₂₅H₂₃N₃O₄

CAS No.

2080306-23-4

SMILES

O=C(N1C2=C(C)C=C(N(C)C3=O)C(N3C)=C2)C4=CC=C(CCCO)C5=C4C(C1=O)=CC=C5

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

Room temperature in continental US; may vary elsewhere

Purity: 99.24%

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Product Name:
BAY-299
Cat. No.:
HY-107424
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BAY-299

Cat. No.: HY-107424