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BAZ2-ICR 

Cat. No.: HY-19336 Purity: >99.0%
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BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.

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BAZ2-ICR Chemical Structure

BAZ2-ICR Chemical Structure

CAS No. : 1665195-94-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 362 In-stock
Estimated Time of Arrival: December 31
5 mg USD 460 In-stock
Estimated Time of Arrival: December 31
10 mg USD 770 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe[1].

IC50 & Target

IC50: 130 nM (BAZ2A) and 180 nM (BAZ2B); Kd: 109 nM (BAZ2A) and 170 nM (BAZ2A)[1]

In Vitro

To investigate whether BAZ2-ICR (Compound 13) can displace BAZ2 bromodomains from chromatin in living cells, a fluorescence recovery after photobleaching (FRAP) assay utilizing GFP-tagged BAZ2A full length protein transfected into human osteosarcoma cells (U2OS) are tested. 1 μM BAZ2-ICR reduces the recovery time of the wild-type (wt) construct to a level similar to the dominant negative mutant, confirming that BAZ2-ICR inhibits BAZ2A in cells[1].

In Vivo

BAZ2-ICR (Compound 13) shows very high solubility (25 mM in D2O), a measured log D of 1.05, high stability in mouse microsomes, and permeation in the CaCo-2 model and thus a suitable profile for oral and intravenous gavage. BAZ2-ICR (5 mg/kg) shows 70% bioavailability and moderate clearance (∼50% of mouse liver blood flow) and volume of distribution[1].

Molecular Weight

357.41

Formula

C₂₀H₁₉N₇

CAS No.

1665195-94-7

SMILES

N#CC1=CC=C(C2=C(C3=CN(C)N=C3)N=CN2CCC4=CN(C)N=C4)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

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

Purity: >99.0%

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Keywords:

BAZ2-ICREpigenetic Reader DomainBAZ2ABAZ2BbromodomainsoralintravenousbioavailabilityepigeneticchemicalprobeInhibitorinhibitorinhibit

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BAZ2-ICR
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HY-19336
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