1. Epigenetics Apoptosis Immunology/Inflammation
  2. Epigenetic Reader Domain Histone Acetyltransferase Apoptosis IKZF Family
  3. KB528

KB528 是一种 p300/CBP 组蛋白乙酰转移酶 (KAT) 抑制剂,针对人源 p300CBPIC50 值处于低 nM 水平,且对其他 KAT 家族成员具有选择性。KB528 可调控 IRF4 转录网络,下调 IRF4MYCCAV2IGLL5 的表达,并降低 IKZF3 蛋白水平。KB528 强效诱导多发性骨髓瘤细胞凋亡 (apoptosis)。KB528 可用于多发性骨髓瘤的相关研究。

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KB528

KB528 Chemical Structure

CAS No. : 3082090-83-0

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生物活性

KB528 is a p300/CBP histone acetyltransferase (KAT) inhibitor with low nM IC50 values against human p300 and CBP, and exhibits selectivity over other KAT family members. KB528 modulates the IRF4 transcriptional network, downregulates the expression of IRF4, MYC, CAV2 and IGLL5, and reduces the protein level of IKZF3. KB528 potently induces apoptosis in multiple myeloma cells. KB528 is applicable to research related to multiple myeloma[1].

体外研究
(In Vitro)

KB528 (0-1 μM; 24-72 h) 可在处理 48 小时后选择性地以浓度依赖方式诱导 MM1.S 细胞凋亡[1]
KB528 (100 nM; 6-24 h) 在 MM1.S 细胞导致 IKZF3 蛋白乙酰化快速丢失,随后出现短暂的 mRNA 下降、蛋白丢失,最后 mRNA 水平反弹。

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

Apoptosis Analysis[1]

Cell Line: MM1.S cells
Concentration: 0.1, 1 and 10 μM
Incubation Time: 24, 48 and 72 h
Result: First induced cell cycle arrest in the treatment for 24 hours, followed by apoptosis.

RT-PCR[1]

Cell Line: MM1.S cells
Concentration: 100 nM
Incubation Time: 24 h
Result: Potently and almost completely downregulated the mRNA of IRF4 and its target genes and the inhibition of IKZF1 and IKZF3 is relatively mild.

Western Blot Analysis[1]

Cell Line: MM1.S cells
Concentration: 100 nM
Incubation Time: 6 and 14 h
Result: Significantly reduced the levels of MYC, IRF4, and IKZF3 proteins, and notably, the protein loss of IKZF3 was more significant than the decrease in its mRNA.
分子量

464.56

Formula

C28H28N6O

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
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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.

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产品名称:
KB528
目录号:
HY-181957
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