B026

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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.

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B026 Chemical Structure

CAS No. : 2379416-48-3

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Biological Activity
Purity & Documentation
References
Customer Review

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.

Cell Viability Assay^[1]

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.

Western Blot Analysis^[1]

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 (1-3 mg/kg; i.v. and p.o.; 0-24 h; male SD rats) has a low clearance (13.4 mL/min/kg) and good oral exposure (AUC=3.71 μM·h) with good oral bioavailability (F=56%) in rat^[1].
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)
T_1/2 (h)	1.5	1.02
T_max (h)		0.83
C_max (μM)		1.12
AUC_last (μM·h)	2.22	3.71
Vd_ss (L/kg)	1.5
CL_{_obs} (mL/min/kg)	13.4
PPB %		98.2
F %		56

Molecular Weight

557.50

Formula

C₂₇H₂₃F₄N₅O₄

CAS No.

2379416-48-3

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.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Yang Y, et, al. Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors. J Med Chem. 2020 Feb 13;63(3):1337-1360. [Content Brief]

B026 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

B0262379416-48-3B 026B-026Histone AcetyltransferaseHATsHATp300CBPhistone acetyltransferaseanticancerH3K27AcMYCInhibitorinhibitorinhibit

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