2. Epigenetics
  3. Histone Acetyltransferase
  4. B026

B026 是一种具有选择性且口服有效的 p300/CBP 组蛋白乙酰转移酶 (p300/CBP HAT) 抑制剂，对于 p300 和 CBP 的 IC50 值为 1.8 nM 和 9.5 nM。B026 对雄激素受体阳性 (AR+) 前列腺癌细胞具有抗癌活性。

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B026 Chemical Structure

B026 Chemical Structure

CAS No. : 2379416-48-3

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B026 相关抗体

Top Publications Citing Use of Products

查看 Histone Acetyltransferase 亚型特异性产品:

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

细胞效力
(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]
体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

B026 相关抗体:

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.
体内研究
(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].

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
分子量

557.50

Formula

C27H23F4N5O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

B026 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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目录号：
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