2. Epigenetics
  3. Epigenetic Reader Domain
  4. XY153

XY153 (compound 8l) 是 BD2 选择性的 BET 抑制剂，选择性地与 BRD4 BD2 结合。XY153 与 BRD4 BD2，BRD3 BD2 和 BRD2 BD2 结合 IC50 值分别为 0.79，5.31 和 5.09 nM。XY153 对多种肿瘤细胞系显示出有效的抗增殖活性。XY153 可用于急性髓性白血病和癌症的研究。

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XY153

XY153 Chemical Structure

CAS No. : 2933176-32-8

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XY153 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer[1].

IC50 & Target

IC50: 0.79 nM (BRD4 BD2), 5.31 nM (BRD3 BD2), 5.09 nM (BRD2 BD2)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
1 μM
Compound: 8l; XY153
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
BXPC-3 IC50
1 μM
Compound: 8l; XY153
Antiproliferative activity against human BxPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human BxPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
CWR22R IC50
232 nM
Compound: 8l; XY153
Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
DU-145 IC50
1 μM
Compound: 8l; XY153
Antiproliferative activity against AR-negative human DU-145 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against AR-negative human DU-145 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
HFL1 IC50
4.6 μM
Compound: 8l; XY153
Cytotoxicity against human HFL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Cytotoxicity against human HFL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
HT-29 IC50
300 nM
Compound: 8l; XY153
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
HepG2 IC50
1 μM
Compound: 8l; XY153
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
Kasumi 1 IC50
471 nM
Compound: 8l; XY153
Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
MCF7 IC50
1 μM
Compound: 8l; XY153
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
MDA-MB-231 IC50
1 μM
Compound: 8l; XY153
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
MOLM-13 IC50
260 nM
Compound: 8l; XY153
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
MV4-11 IC50
0.00054 μM
Compound: 8l; XY153
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
MV4-11 IC50
0.55 nM
Compound: 8l; XY153
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 120 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
THP-1 IC50
1.3 μM
Compound: 8l; XY153
Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
U-937 IC50
1 μM
Compound: 8l; XY153
Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
U2OS IC50
1 μM
Compound: 8l; XY153
Antiproliferative activity against human U2OS cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
Antiproliferative activity against human U2OS cells assessed as cell growth inhibition incubated for 72 hrs by Cell titre Glo-luminiscence cell viability assay
[PMID: 35333526]
体外研究
(In Vitro)

XY153 shows strong antiproliferative activities for specific cancer cell lines but with a better safety profile against a normal lung fibroblast cell line[1].

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

XY153 相关抗体:

Cell Viability Assay[1]

Cell Line: MV4-11, MOLM-13, Kasumi-1, THP-1, HT-29, 22Rv1, Du145, MCF-7, MDA-MB-231, A549, U2OS, U937, HepG2, BxPC-3 and HFL-1 cell lines
Concentration: 0.001 nM-10 μM
Incubation Time: 96 hours
Result: Inhibited acute myeloid leukemia (AML) cell lines with IC50s of 0.55 nM, 260 nM, 471 nM and 1.3 μM for MV4-11, MOLM-13, Kasumi-1 and THP-1 cell lines, respectively. Showed potent cytotoxicity to AR-positive prostate cancer cell line 22Rv1 and colorectal cancer cell line HT-29 with IC50s of 232 and 300 nM, respectively. Exhibited weak cytotoxicity to normal lung fibroblast cell line HFL-1 with an IC50 value of 4.6 μM.
分子量

555.64

Formula

C33H34FN3O4
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

XY153 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:

XY1532933176-32-8XY 153XY-153Epigenetic Reader Domainanti-proliferationanticancerAMLBD222Rv1HT-29MV4-11MOLM-13Kasumi-1THP-1Inhibitorinhibitorinhibit

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目录号：
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