Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T26252 |
PI3Kδ-IN-3
TC KHNS 11 |
PI3K | PI3K/Akt/mTOR signaling |
PI3Kδ-IN-3 (TC KHNS 11) 是一种 PI3Kδ 抑制剂,IC50 值为 9 nM。PI3Kδ-IN-3 具有良好的药代动力学特性且对 B 细胞功能有抑制作用。 | |||
T6330 |
Linperlisib
PI3Kδ-IN-2 |
PI3K | PI3K/Akt/mTOR signaling |
Linperlisib (PI3Kδ-IN-2) 是一种有效的,效选择性的,具有口服活性的 PI3Kδ的抑制剂,其 IC50=6.4 nM。 | |||
T63078 |
PI3Kδ/γ-IN-3
|
||
PI3Kδ/γ-IN-3 (Compound 58) 是一种口服具有活力的 PI3Kδ (IC50: 1 nM) 和 PI3Kγ (IC50: 16 nM) 双重抑制剂。 PI3Kδ/γ-IN-3 可诱导肿瘤细胞凋亡,能够于研究 B 细胞恶性肿瘤。 | |||
T2365 |
Pilaralisib
SAR245408,XL-147 |
PI3K | PI3K/Akt/mTOR signaling |
Pilaralisib (XL-147) 是一种有效的、选择性的 I 类PI3Ks 抑制剂,能够抑制 PI3Kα (IC50:39 nM),PI3Kβ (IC50:383 nM),PI3Kγ (IC50:23 nM) 和 PI3Kδ (IC50:36 nM)。 | |||
T36083 |
DS-7423
|
PI3K; mTOR | PI3K/Akt/mTOR signaling |
DS-7423 是PI3K 和mTOR 的有效抑制剂,抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。 | |||
T2078 |
Fimepinostat
CUDC-907,PI3K/HDAC Inhibitor,CUDC 907 |
Apoptosis; PI3K; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Fimepinostat (CUDC 907) 是一种 I 型PI3K 及 I 和 II 型HDAC 酶抑制剂,作用于 PI3Kα/PI3Kβ/PI3Kδ 和 HDAC1/HDAC2/HDAC3/HDAC10 ,IC50分别为 19/54/39 nM 和 1.7/5.0/1.8/2.8 nM。 | |||
T6322 |
Copanlisib
BAY 80-6946,可泮利塞,库潘尼西 |
Apoptosis; PI3K | Apoptosis; PI3K/Akt/mTOR signaling |
Copanlisib (BAY 80-6946) 是一种选择性的和 ATP 竞争性的泛 I 类PI3K 抑制剂,具有抗肿瘤活性,对PI3Kα,PI3Kδ,PI3Kβ和PI3Kγ的IC50分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。 | |||
T62997 | PI3K/AKT-IN-1 | ||
PI3K/AKT-IN-1 是一种有效的、双重的 PI3K/AKT 抑制剂,能够作用于 PI3Kγ (IC50: 6.99 μM)、PI3Kδ (IC50: 4.01 μM) 和 AKT (IC50: 3.36 μM)。PI3K/AKT-IN-1 通过抑制 PI3K/AKT 通路,诱导 caspase 3 依赖性凋亡,表现出抗癌作用。 | |||
T35531 |
FD223
|
||
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML[1]. | |||
T35488 |
(S)-PI3Kα-IN-4
(S)-PI3Kα-IN-4 |
||
(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitor... | |||
T78853 |
PI3K-IN-47
|
PI3K | PI3K/Akt/mTOR signaling |
PI3K-IN-47 (Compound 27) 是一款高度选择性的二价PI3K抑制剂,对PI3Kα具有极低的半抑制浓度(IC50: 0.44 nM), 同时对PI3Kβ、PI3Kγ、PI3Kδ也表现出良好的抑制活性(IC50分别为7.18 nM、13.92 nM、22.83 nM)。此化合物能够有效诱导细胞周期在G1期发生暂停,并且在体外抑制集落形成和细胞迁移。对于HGC-27异种移植的小鼠模型,PI3K-IN-47能够显著抑制肿瘤生长。 |