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BP-1-102

CAS号

1334493-07-0

分子式

C29H27F5N2O6S

主要靶点

STAT

仅限科研使用

Cat No : CM06551

Print datasheet

Synonyms

BP 1 102|BP1102|BP-1-102|Inhibitor|inhibit|STAT3|STAT

验证数据展示

  • CAS No.: 1334493-07-0

    BP-1-102
    CAS#: 1334493-07-0

产品信息

CAS号 1334493-07-0
分子式 C29H27F5N2O6S
主要靶点 STAT
主要通路 JAK/STAT 信号通路|干细胞
分子量 626.59
纯度 99.81%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 BP 1 102|BP1102|BP-1-102|Inhibitor|inhibit|STAT3|STAT

靶点活性

STAT3:504 nM(Kd)

体内活性

静脉注射或口服灌胃给药BP-1-102可在肿瘤组织中达到微摩尔或微克水平，抑制人乳腺和肺肿瘤异种移植物的生长，并调节Stat3活性、Stat3靶基因和体内可溶性因子。BP-1-102选择性地抑制含有持续激活的stat3的恶性细胞的生长、存活、恶性转化、迁移和侵袭。在血浆中，BP-1-102的浓度可达到微摩尔水平，在肿瘤组织中以微克形式检测到[1]。

体外活性

BP-1-102通过504 nM的亲和力(KD)结合Stat3，阻断Stat3-磷酸化酪氨酸(pTyr)肽段相互作用，抑制Stat3依赖型肿瘤细胞的生长、存活、迁移和侵袭。BP-1-102对异常活跃的Stat3在肿瘤细胞中的抑制作用导致c-Myc、Cyclin D1、Bcl-xL、Survivin和VEGF表达下调。用BP-1-102处理乳腺癌细胞进一步阻断了Stat3–NF-κB的交流，颗粒细胞集落刺激因子、可溶性细胞间黏附分子1、巨噬细胞迁移抑制因子/糖基化抑制因子、白细胞介素1受体拮抗剂及丝氨酸蛋白酶抑制蛋白1的释放，以及焦点粘附激酶和paxillin的磷酸化。BP-1-102在体外抑制Stat3 DNA结合活性，IC50值为6.8±0.8 μM，优先抑制Stat3-Stat3、相较于Stat1-Stat3、Stat1-Stat1或Stat5-Stat5的DNA结合活性。BP-1-102对phospho-Shc、Src、Jak-1/2、Erk1/2或Akt水平几乎没有影响[1]。

溶解度

DMSO:93 mg/mL (148.5 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

细胞实验

Proliferating cells in 6- or 96-well plates are treated once with 0–30 μM BP-1-102 for 24 h or with 10 μM BP-1-102 for up to 96 h. Viable cells are counted by trypan blue exclusion/phase-contrast microscopy or assessed by a CyQUANT Cell Proliferation Kit.(Only for Reference)

参考文献

1.Zhang X, et al. Proc Natl Acad Sci U S A. 2012, 109(24):9623-8.
2.He Q R, Tang J J, Chen Z F, et al. Natural Product Trienomycin A is a STAT3 pathway inhibitor that exhibits potent in vitro and in vivo efficacy against pancreatic cancer[J]. Authorea Preprints. 2020
3.Yan J, Zhou B, Guo L, et al. GOLM1 upregulates expression of PD-L1 through EGFR/STAT3 pathway in hepatocellular carcinoma[J]. American journal of cancer research. 2020, 10(11): 3705.
4.Chen C, Lu M, Lin S, et al. The nuclear gene rpl18 regulates erythroid maturation via JAK2-STAT3 signaling in zebrafish model of Diamond–Blackfan anemia[J]. Cell Death & Disease. 2020, 11(2): 1-11.
5.Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma[J]. Theranostics. 2020, 10(14): 6530.

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