2. Epigenetics Apoptosis PI3K/Akt/mTOR Cytoskeleton Cell Cycle/DNA Damage
  3. Epigenetic Reader Domain Apoptosis AMPK c-Myc PAK Bcl-2 Family
  4. XY221

XY221 (Compound 16o) 选择性抑制 BRD4 BD2，IC50 为 5.8 nM。XY221 展现出对 泛 pan-BD2 和 BRD4 BD2 域的高选择性，分别比 BRD4 BD1 高 667 倍，比 BRD2/3/T BD2高 9-32倍。XY221 可诱导 MV4-11 细胞凋亡，并具有抗癌活性。

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XY221 Chemical Structure

XY221 Chemical Structure

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Customer Review

XY221 相关抗体

Top Publications Citing Use of Products

查看 AMPK 亚型特异性产品:

查看所有亚型
NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

查看 PAK 亚型特异性产品:

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity [1].

IC50 & Target

BRD4 BD1

3869 nM (IC50)

BRD4 BD2

5.8 nM (IC50)

BRD3 BD2

70.98 nM (Ki)

体外研究
(In Vitro)

XY221 抑制 BRD4 BD2, BRD3 BD2, BRD2 BD2, BRDT BD2 and BRD4 BD1 的 IC50 值分别为 5.8, 70.98, 53.47, 183, 3869 nM[1]。
XY221 抑制 MV4−11, LNCaP, HL-7702 cells 增殖的 IC50 分别为 0.51, 0.68, 47.7 μM[1]。
XY221 (500-2000 nM，72 h) 能显著抑制 MV4-11 细胞的增殖和诱导 MV4-11 细胞凋亡[1]。
XY221 (1-10 μM，2 h) 在 RLM (鼠肝线粒体) 中半衰期长达 120 min 以上，在 HLM (人肝线粒体) 中半衰期也长达 120 min 以上[1]。
XY221 (500-2000 nM, 72h) 抑制 MV4−11 细胞中靶基因 p21 ,ODC1, BRD4 和 AKT 、AMPK 的磷酸化[1]。
XY221 (2 μM, 72h) 在 mRNA 水平上抑制 MV4−11 细胞原癌基因 MYC 及其靶基因 p21 和细胞周期相关基因 BCL-2[1]。

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

XY221 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4−11 cells
Concentration: 500, 2000 nM
Incubation Time: 24-72 h
Result: Inhibited target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK.

Real Time qPCR[1]

Cell Line: MV4−11 cells
Concentration: 2 μM
Incubation Time: 72 h
Result: Inhibited target genes p21 ,ODC1, BRD4 and the phosphorylation of AKT and AMPK.
Suppressed oncogene MYC and its target gene p21 and cell-cycle-related gene BCL-2 at mRNA level.
体内研究
(In Vivo)

XY221 在大鼠中静脉 (iv) 和口服给药(po) 时的药代动力学参数

route Cmax(μg/L) Tmax(h) AUC(0-t)(μg/L・h) AUC(0-∞)(μg/L・h) T1/2(h) CI(L/h/kg) F (%)
XY221 iv (5 mg/kg) 9790 0.03 4291 4294 1.35 1.21
XY221 po (25 mg/kg) 567 3.67 2811 2816 2.13 13.1

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

559.63

Formula

C32H34FN3O5
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

XY221 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:

XY221XY 221XY-221Epigenetic Reader DomainApoptosisAMPKc-MycPAKBcl-2 FamilyAMP-activated protein kinaseMycp21 activated kinasesantiproliferationantileukemiaacute myeloid leukemiaprostate cancer,Inhibitorinhibitorinhibit

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