A-485

Catalog No.S8740

A-485 Chemical Structure

Molecular Weight(MW): 536.48

A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets.

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Biological Activity

Description A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets.
Targets
p300 HAT [1]
()
0.06 μM
In vitro

A-485 is acetyl-CoA competitive p300/CBP catalytic inhibitor. A-485 selectively inhibited proliferation across lineage-specific tumor types, including several hematological malignancies and androgen receptor-positive prostate cancer. A-485 inhibited the androgen receptor transcriptional program in both androgen sensitive and castrate resistant prostate cancer. A-485 inhibited the activity of the p300-BHC (bromodomain-HAT-C/H3) domain (IC50 = 9.8 nM) as well as CBP-BHC (IC50 = 2.6 nM). A-485 is assayed against other HAT family members and does not inhibit the activity of PCAF, HAT1, MYST3, MYST4, TIP60 and GCN5L2 at 10 µM and is selective over BET bromodomain proteins and >150 non-epigenetic targets. The compound only displayed substantial binding (>90%) to dopamine and serotonin transporters at 10 µM along with modest inhibition of Plk3 (IC50=2.7 µM). As A-485 does not achieve significant brain exposure, it is unlikely to modulate these transporters in vivo. A-485 is selective for p300/CBP over other HATs and histone methyltransferases (HMTs) in cells. It only inhibits H3K27Ac and H3K18Ac. A-485 selectively inhibits hematological and prostate cancer cell proliferation and that inhibition of p300/CBP-mediated global histone acetylation does not necessarily translate to an anti-proliferative phenotype. A-485 is primarily metabolized by CYP3A4 in vitro. A-485 also exhibits modest inhibition of CYP2C8 (IC50=0.99 μM) and CYP2C9 (IC50=1.65 μM). There was no activity toward hERG (>30 μM)[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLT3 MVrGeY5kfGmxbjDhd5NigQ>? NGPOUWU2KM7:TR?= NUXRTG9TPDhiaB?= MYXk[YNz\WG|ZXSgUm9VS0h|IHX4dJJme3Orb36gcIV3\Wy| NILoWIU{OTByMUS3NC=>
WM2664 NFfqOIZHfW6ldHnvckBie3OjeR?= NHPwUmVJO0t{N3HjJGlEPTB;MD62JO69VQ>? M3;BbVMxOjZ4OECx
SKMEL5 NXvVV3RFTnWwY4Tpc44h[XO|YYm= NIDpTlZJO0t{N3HjJGlEPTB;MD65JO69VQ>? NVzodIhmOzB{Nk[4NFE>
A375 MV7GeY5kfGmxbjDhd5NigQ>? NYDjUYJ7UDONMkfhZ{BKSzVyPUGuNEDPxE1? MX2zNFI3PjhyMR?=

... Click to View More Cell Line Experimental Data

In vivo

A-485 displays favorable ADME properties and PK profile. A-485 inhibits tumor growth in a castration resistant xenograft model. Treatment of A-485 in LuCaP-77 CR tumor bearing mice tumor induces a decrease in tumor c-Myc protein levels and moderate body weight loss[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: HeLa cells
  • Concentrations: 10 μM
  • Incubation Time: 16 h
  • Method:

    HeLa cells were SILAC labeled with heavy isotopes of arginine and lysine. The cells were treated with A-485 (10 μM) or vehicle control for 16 hours. Cell were lysed in ice-cold lysis buffer [50 mM Hepes, pH7.5, 150 mM NaCl, 1 mM EDTA, 1% NP-40, 0.1% sodium deoxycholate, 1x complete protease inhibitor cocktail]. Proteins were proteolyzed with trypsin, and acetylated peptides were analyzed.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: LuCap-77 CR xenograft tumors (established in SCID mice)
  • Formulation: --
  • Dosages: 100 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (186.4 mM)
Ethanol 100 mg/mL (186.4 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 536.48
Formula

C25H24F4N4O5

CAS No. 1889279-16-6
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Histone Acetyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID