B026
B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.
For research use only. We do not sell to patients.
- CAS No.: 2379416-48-3
- Formula: C27H23F4N5O4
- Molecular Weight:557.50
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
p300 8.1 nM (IC50) |
CBP 9.5 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
4.4 nM
Compound: B026
|
Antiproliferative activity against human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay
Antiproliferative activity against human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay
|
[PMID: 31910017] |
| HT | IC50 |
>10 μM
Compound: B026
|
Antiproliferative activity against human HT cells measured after 3 days by celltiter-glo luminescence assay
Antiproliferative activity against human HT cells measured after 3 days by celltiter-glo luminescence assay
|
[PMID: 31910017] |
| K562 | IC50 |
104.4 nM
Compound: B026
|
Antiproliferative activity against human K562 cells measured after 3 days by celltiter-glo luminescence assay
Antiproliferative activity against human K562 cells measured after 3 days by celltiter-glo luminescence assay
|
[PMID: 31910017] |
| Kasumi 1 | IC50 |
40.5 nM
Compound: B026
|
Antiproliferative activity against human Kasumi-1 cells measured after 3 days by celltiter-glo luminescence assay
Antiproliferative activity against human Kasumi-1 cells measured after 3 days by celltiter-glo luminescence assay
|
[PMID: 31910017] |
| LNCaP-Clone-FGC | IC50 |
9.8 nM
Compound: B026
|
Antiproliferative activity against human LNCaP-FGC cells measured after 5 days by celltiter-glo luminescence assay
Antiproliferative activity against human LNCaP-FGC cells measured after 5 days by celltiter-glo luminescence assay
|
[PMID: 31910017] |
| Maver1 | IC50 |
2.6 nM
Compound: B026
|
Antiproliferative activity against human Maver1 cells measured after 3 days by celltiter-glo luminescence assay
Antiproliferative activity against human Maver1 cells measured after 3 days by celltiter-glo luminescence assay
|
[PMID: 31910017] |
| MV4-11 | IC50 |
4.2 nM
Compound: B026
|
Antiproliferative activity against human MV4-11 cells measured after 3 days by celltiter-glo luminescence assay
Antiproliferative activity against human MV4-11 cells measured after 3 days by celltiter-glo luminescence assay
|
[PMID: 31910017] |
In Vitro
B026 (0-5 μM; 12 h; cancer cell lines) has antiproliferative activity[1].
B026 (0-5 μM; 6 h; MV-4-11 cells) exhibits inhibitory effects on H3K27Ac expression[1].
B026 (0-5 μM; 12 h; MV-4-11 cells) targets the cellular p300 protein and increases the thermal stability of p300 protein in a dose-dependent manner[1].
B026 (0-1 μM; 24 h; MV-4-11 cells) decreases the expression of MYC, which a key oncogenictranscription factor that is regulated by superenhancer regions containing p300/CBP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:Maver-1, MV-4-11, K562, Kasumi-1, LnCaP-FGC and 22Rv1 cells
-
Concentration:0-5 μM
-
Incubation Time:12 hours
-
Result:Inhibited cell growth with IC50 values of 2.6, 4.2, 4.4, 9.8, 40.5 and 104.4 nM for Maver-1, MV-4-11, 22Rv1, LnCaP-FGC, Kasumi-1 and K562 cells, respectively.
-
Cell Line:MV-4-11 cells
-
Concentration:0, 0.313, 0.625, 1.25, 2.5 and 5 μM
-
Incubation Time:6 hours
-
Result:Decreased the expression of H3K27Ac in a dose-dependent manner.
In Vivo
B026 (50-100 mg/kg; p.o.; daily, for 28 days; balb/c female mice) inhibits tumor growth in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Balb/c female mice with MV-4-11 xenograft[1]
-
Dosage:50 and 100 mg/kg
-
Administration:Oral administration; daily, for 28 days
-
Result:Inhibited tumor growth with TGI of 75.0% at 50 mg/kg and 85.7% at 100 mg/kg, respectively.
-
Animal Model:Male SD rats[1]
-
Dosage:1 and 3 mg/kg
-
Administration:Intravenous injection and oral administration; 0.25, 0.5 , 1 , 2 , 4 , 8 and 24 hours
-
Result:
1.19 Administration i.v. (1 mg/kg) p.o. (3 mg/kg) T1/2 (h) 1.5 1.02 Tmax (h) 0.83 Cmax (μM) 1.12 AUClast (μM·h) 2.22 3.71 Vdss (L/kg) 1.5 CL_obs (mL/min/kg) 13.4 PPB % 98.2 F % 56
Chemical Information
-
CAS No. 2379416-48-3
-
Molecular Weight 557.50
-
Formula C27H23F4N5O4
-
SMILES
O=C1[C@@]2(NC(N1CC(N3[C@@H](COC4=CC=C(F)C=C4C3)C(F)(F)F)=O)=O)C5=CC=C(C6=CN(N=C6)C)C=C5CC2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)