PP121
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PP121是酪氨酸激酶和磷酸肌醇激酶的双重抑制剂[1].
PP121可抑制酪氨酸激酶和PI3-Ks,但不能抑制丝氨酸-苏氨酸激酶.该物质可有效抑制p110α\p110β\p110γ\p110δ\DNA-PK和mTOR,IC50值分别为52 nM\1.4 μM\1.1 μM\150 nM\60 nM和10 nM[1].对于酪氨酸激酶,PP121可抑制Ab1\Hck\Src\VEGFR2\EGFR\EphB4和PDGFR,IC50值分别为21 nM\4 nM\10 nM\55 nM\550 nM\220 nM 和<1 nM.
在细胞中,PP121可逆转v-Src介导的细胞转化和还原肌动蛋白应力纤维染色.PP121也可在甲状腺瘤中有效抑制突变Ret激酶,IC50值小于1 nM.此外,PP121还可通过靶向Bcr-Abl介导的细胞存活和PI3-K/mTOR介导的细胞增殖,逃避抗药性[1].
参考文献：
[1] Apsel B, Blair J A, Gonzalez B, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nature chemical biology, 2008, 4(11): 691-699.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 319.37 |
| Cas No. | 1092788-83-4 |
| Formula | C17H17N7 |
| Solubility | insoluble in H2O; ≥1.65 mg/mL in EtOH with gentle warming and ultrasonic; ≥15.95 mg/mL in DMSO |
| Chemical Name | 1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazolo[3,4-d]pyrimidin-4-amine |
| SDF | Download SDF |
| Canonical SMILES | C1CCC(C1)N2C3=C(C(=N2)C4=CN=C5C(=C4)C=CN5)C(=NC=N3)N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | PP-121是PDGFR\Hck\mTOR\VEGFR2\Src和Abl的多靶点抑制剂,IC50值分别为2 nM\8 nM\10 nM\12 nM\14 nM和18 nM. | |||||
| 靶点 | PDGFR | Hck | VEGFR | mTOR | Src | Abl |
| IC50 | 2 nM | 8 nM | 12 nM | 13 nM | 14 nM | 18 nM |
化学结构
