2. Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Apoptosis HDAC
  4. JNJ-16241199

JNJ-16241199  (Synonyms: R306465)

目录号: HY-10226
产品使用指南

摩尔计算器

JNJ-16241199 是一种具有口服活性的选择性 hydroxamate-based histone deacetylase (HDAC) 抑制剂，对 HDAC 1 和 HDAC8 的IC50 分别为 3.3 nM 和 23 nM。JNJ-16241199 诱导组蛋白 3 乙酰化，并显著上调 A2780 卵巢癌细胞中 p21waf1, cip1 的表达。JNJ-16241199 诱导细胞凋亡 (cell apoptosis)，并在多种人类恶性肿瘤中显示抗癌活性。JNJ-16241199 可用于癌症研究。

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JNJ-16241199 Chemical Structure

JNJ-16241199 Chemical Structure

CAS No. : 604769-01-9

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JNJ-16241199 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JNJ-16241199 is an orally active, selective hydroxamate-based histone deacetylase (HDAC) inhibitor, with the IC50 of 3.3 nM and 23 nM for HDAC1 and HDAC8, respectively. JNJ-16241199 induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells. JNJ-16241199 induces cell apoptosis and shows anticancer activity in a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study[1].

IC50 & Target

HDAC1

3.3 nM (IC50)

HDAC8

23 nM (IC50)

体外研究
(In Vitro)

JNJ-16241199 对性淋巴细胞白血病 (ALL)、急性髓性白血病 (AML)、慢性淋巴细胞白血病 (CLL)、慢性髓性白血病 (CML)、淋巴瘤和骨髓瘤细胞具有抑制增殖作用 (IC50 = 15-486 nM) [1]。
JNJ-16241199 抑制原代人乳腺上皮细胞 (HMEC) 增殖，IC50 值为 32 nM，对静止的非增殖 HMEC 细胞不敏感 (IC50 值为 7815 nM) [1]。
JNJ-16241199 (0.1, 0.3, 1 μM, 24-48 h) 可以诱导 A2780 细胞发生细胞凋亡，并抑制其血管生成[1]。

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

JNJ-16241199 相关抗体:

Cell Cycle Analysis[1]

Cell Line: Human A2780 ovarian carcinoma cells
Concentration: 0, 0.1, 0.3, 1 μM
Incubation Time: 24 h or 48 h
Result: Decreased in S phase at 300 nM, with a parallel increase in G1 phase, but increased in the sub-G1 fraction of cells at the 1 μM after 24 h.
Increased in sub-G1 phase at all active concentrations starting from 100 nM after 48 h.
体内研究
(In Vivo)

JNJ-16241199 (每天 10-40 mpk，连续 28 天，p.o) 抑制 A2780 卵巢癌、H460 肺癌和 HCT116 结肠癌原位异种移植肿瘤模型小鼠中肿瘤的生长[1]。

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

Animal Model: Human A2780, H460 and HCT116 orthotopic xenograft tumor models[1]
Dosage: 10-40 mpk/day for 28 days
Administration: Oral gavage (p.o.)
Result: Induced H3 acetylation and p21waf1, cip1 promoter activity in A2780 ovarian tumour tissue.
Decreased tumour volume in three orthotopic xenograft tumor models.
Reached maximal decrease in final tumour volume to 76–87% in human A2780 orthotopic xenograft tumor models.
分子量

413.45

Formula

C19H19N5O4S
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

JNJ-16241199 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

JNJ-16241199604769-01-9R306465JNJ16241199JNJ 16241199R 306465R-306465ApoptosisHDACHistone deacetylasesA2780H460T116Acute lymphoblastic leukaemiaChronic lymphoblastic leukaemiaChronic myeloid leukaemiaLymphomaMyelomaInhibitorinhibitorinhibit

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