A-485
Catalog No.: GC32677Purity:>98.50%
A-485 is a potent and selective p300/CBP (histone acetyltransferase paralog/CREB binding protein) catalytic inhibitor with IC50 of 60nM for p300 HAT. A-485 inhibits the activity of p300-BHC (bromodomain HAT-C/H3) and CBP-BHC domains with IC50 of 9.8nM and 2.6nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1889279-16-6
10mM (in 1mL DMSO)In Stock
$272.00
1
1mgIn Stock
$77.00
1
5mgIn Stock
$231.00
1
10mgIn Stock
$350.00
1
50mgIn Stock
$693.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $272.00 | In Stock | 1 | |
| 1mg | $77.00 | In Stock | 1 | |
| 5mg | $231.00 | In Stock | 1 | |
| 10mg | $350.00 | In Stock | 1 | |
| 50mg | $693.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
A-485 is a potent and selective p300/CBP (histone acetyltransferase paralog/CREB binding protein) catalytic inhibitor with IC50 of 60nM for p300 HAT. A-485 inhibits the activity of p300-BHC (bromodomain HAT-C/H3) and CBP-BHC domains with IC50 of 9.8nM and 2.6nM, respectively. A-485 selectively inhibits the proliferation of lineage-specific tumor types, including several hematological malignancies and androgen receptor-positive prostate cancer [1-2].
A-485 reduces the level of acetylated histone H3 lysine 27 (H3K27Ac) in PC3 cells in a concentration-dependent manner with an EC50 of 73nM, but has little effect on H3K9Ac (EC50 > 10mM) [1]. A-485 has an inhibitory effect on H3K27Ac in three melanoma cell lines (WM2664, SKMEL5 and A375 cells) with IC50 of 0.59, 0.93 and 0.96μM, respectively. A-485 significantly induces cell senescence in sensitive melanoma cell lines WM2664 and SKMEL5, but no similar effect was observed in resistant A375 cells [3].
A-485 reduced tumor volume (54%) in the LuCaP-77 CR mouse xenograft model of castration-resistant prostate cancer when administered at a dose of 100mg/kg for 21 days [1]. In the GH3 cell xenograft nude mouse model, A-485 can significantly inhibit tumor volume (50mg/kg group inhibited 32.37%, 100mg/kg group inhibited 54.15%) and tumor weight (50mg/kg group inhibited 43.83% , the 100mg/kg group inhibited 61.41%) [4].
References:
[1] Lasko LM, et al. Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature. 2017 Oct 5;550(7674):128-132.
[2] Tottone L, Zhdanovskaya N, Carmona Pestaña Á, Zampieri M, Simeoni F, Lazzari S, Ruocco V, Pelullo M, Caiafa P, Felli MP, Checquolo S, Bellavia D, Talora C, Screpanti I, Palermo R. Histone Modifications Drive Aberrant Notch3 Expression/Activity and Growth in T-ALL. Front Oncol. 2019 Apr 3;9:198.
[3] Wang R, He Y, Robinson V, Yang Z, Hessler P, Lasko LM, Lu X, Bhathena A, Lai A, Uziel T, Lam LT. Targeting Lineage-specific MITF Pathway in Human Melanoma Cell Lines by A-485, the Selective Small-molecule Inhibitor of p300/CBP. Mol Cancer Ther. 2018 Dec;17(12):2543-2550.
[4] Ji C, Xu W, Ding H, et al. The p300 inhibitor A-485 exerts antitumor activity in growth hormone pituitary adenoma[J]. The Journal of Clinical Endocrinology & Metabolism, 2022, 107(6): e2291-e2300.
Protocol
| Cell experiment [1]: | |
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Cell lines |
Human T-ALL cell lines |
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Preparation Method |
TALL-1 cell lines were treated with 5μM A-485 or an equal volume of vehicle (DMSO), and 48 hours later, live TALL-1 cells were transiently transfected with an expression vector encoding human c-Myc. Cell viability was measured by MTS assay. |
|
Reaction Conditions |
5μM, 48h |
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Applications |
A-485 inhibited the viability of TALL-1 cells, and the expression of exogenous c-Myc partially saved the viability of NotCH3-dependent TALL-1 cells exposed to A-485. |
| Animal experiment [2]: | |
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Animal models |
LuCaP-77 CR xenograft model |
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Preparation Method |
LuCap-77 CR xenograft tumors were established in SCID mice, and A-485 was administered intraperitoneally (ip) at a dose of 100mg/kg twice daily for 21 days. |
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Dosage form |
100mg/kg, twice daily for 21 days , i.p. |
|
Applications |
After 21 days of administration, A-485 inhibited tumor growth by 54% compared to vehicle control. |
|
References: |
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Product Documents
Purity:>98.50%Appearance:A solid
Chemical Properties
CAS No.
1889279-16-6
SMILES
O=C(N1CC(N([C@@H](C)C(F)(F)F)CC2=CC=C(F)C=C2)=O)[C@]3(OC1=O)C4=CC=C(NC(NC)=O)C=C4CC3
Molecular Formula
C25H24F4N4O5
Molecular Weight
536.48
Solubility
DMSO : 100 mg/mL (186.40 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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