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Merck
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SML1175

Sigma-Aldrich

罗咪酯肽

≥98% (HPLC), powder, histone deacetylase inhibitor

别名:

FK228, FR901228, L-缬氨酸, N-((3S,4E)-3-羟基-7-巯基-1-氧代-4-庚基)-D-戊基-D-半胱氨酸-(2Z)-2-氨基-2-丁烯氧基-, (4-1)-内酯,环状(1-2)-二硫化物, 环[(2Z)-2-氨基-2-丁烯酰基-L-戊基-(3S,4E)-3-羟基-7-巯基-4-庚烯酰基-D-戊基-D-半胱氨酰]环状(35)-二硫化物, 缩酚酸肽

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About This Item

经验公式（希尔记法）:
C24H36N4O6S2
CAS号:
128517-07-7
分子量:
540.70
MDL编号:
MFCD18433404
UNSPSC代码:
12352200
PubChem化学物质编号:
329825701
NACRES:
NA.77

product name

罗咪酯肽, ≥98% (HPLC)

质量水平

100

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 25 mg/mL, clear

储存温度

−20°C

SMILES字符串

O=C(N/C(C(N[C@@H](C(C)C)C(O[C@@]1([H])CC2=O)=O)=O)=C\C)[C@@H](CSSCC/C=C/1)NC([C@H](N2)C(C)C)=O

InChI

1S/C24H36N4O6S2/c1-6-16-21(30)28-20(14(4)5)24(33)34-15-9-7-8-10-35-36-12-17(22(31)25-16)26-23(32)19(13(2)3)27-18(29)11-15/h6-7,9,13-15,17,19-20H,8,10-12H2,1-5H3,(H,25,31)(H,26,32)(H,27,29)(H,28,30)/b9-7+,16-6-/t15-,17-,19-,20+/m1/s1

InChI key

OHRURASPPZQGQM-GCCNXGTGSA-N

基因信息

human ... HDAC1(3065) , HDAC10(83933) , HDAC11(79885) , HDAC2(3066) , HDAC3(8841) , HDAC4(9759) , HDAC5(10014) , HDAC6(10013) , HDAC7(51564) , HDAC8(55869) , HDAC9(9734)

生化/生理作用

罗米地辛可促进细胞凋亡，同时阻碍神经胶质瘤模型中肿瘤的生长。
罗米地辛是HDAC1和HDAC2的一种非常有效的天然前药抑制剂，可被谷胱甘肽转化为活性形式。罗米地辛对HDAC1和HDAC2的IC50 值分别为36 nM和47 nM。它可杀死过表达Bcl-2和Bcl-XL的淋巴瘤细胞系，并已被批准用于治疗皮肤T细胞淋巴瘤（CTCL）和外周T细胞淋巴瘤，以及多种其他癌症。

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

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Anna Otte et al.
International journal of oncology, 49(6), 2453-2463 (2016-10-18)
Chemotherapeutic drug testing of SCCOHT-1 and BIN-67 tumor cells revealed synergistic growth-inhibition of >95% in vitro with a combination of foretinib and FK228. Application of this drug combination in vivo in NODscid mice-induced SCCOHT-1GFP tumors was associated with ~6-fold reduction in
Cai-Ping Chen et al.
Acta pharmaceutica Sinica. B, 9(5), 937-951 (2019-10-28)
Artemisinin and its derivatives (ARTs) were reported to display heme-dependent antitumor activity. On the other hand, histone deacetylase inhibitors (HDACi) were known to be able to promote heme synthesis in erythroid cells. Nevertheless, the effect of HDACi on heme homeostasis
Minsun Jung et al.
The oncologist, 24(8), e740-e748 (2019-01-31)
NUT carcinoma is a rare aggressive disease caused by BRD4/3-NUT fusion, and C-MYC upregulation plays a key role in the pathogenesis. Here, we report on the clinicopathological characteristics of Korean patients with NUT carcinoma and the in vitro efficacy of
YiHan Wu et al.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 84, 462-469 (2016-09-30)
Temozolomide is a novel cytotoxic agent currently used as first-line chemotherapy for glioblastoma multiforme (GBM). Romidepsin (FK228), a histone deacetylase inhibitor, is a promising new class of antineoplastic agent with the capacity to induce growth arrest and/or apoptosis of cancer
Florencia Cayrol et al.
Nature communications, 8, 14290-14290 (2017-01-31)
Peripheral T-cell lymphomas (PTCL) are aggressive diseases with poor response to chemotherapy and dismal survival. Identification of effective strategies to target PTCL biology represents an urgent need. Here we report that PTCL are sensitive to transcription-targeting drugs, and, in particular
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