PI3K/Akt/mTOR Signaling(PI3K/Akt/mTOR 信号传导)

Cat.No. 产品名称 Information

GC32891 PQR620 PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. PQR620 has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure.

GC32847 PI4KIIIbeta-IN-9 PI4KIIIbeta-IN-9是一种有效的PI4KIIIβ抑制剂，IC50为7nM。PI4KIIIbeta-IN-9也抑制PI3Kδ和PI3Kγ，IC50分别为152nM和1046nM。

GC32828 Tenalisib (RP6530)

RP6530

Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.

GC32794 Ipatasertib dihydrochloride (GDC-0068 (dihydrochloride))

(2S)-2-(4-氯苯基)-1-[4-[(5R,7R)-6,7-二氢-7-羟基-5-甲基-5H-环戊并嘧啶-4-基]-1-哌嗪基]-3-[(1-甲基乙基)氨基]-1-丙酮二盐酸盐,GDC-0068 dihydrochloride; RG-7440 dihydrochloride

A pan-Akt inhibitor

GC32767 3BDO

3BDO,MTOR激酶激活剂,自噬抑制剂

A butyrolactone derivative and autophagy inhibitor

GC32736 MELK-8a hydrochloride

NVS-MELK8a hydrochloride

A MELK inhibitor

GC32718 M3814 (nedisertib)

M3814

Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM.

GC32710 GDC-0077 (RG6114)

GDC-0077; RG6114

Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3.

GC32510 Loureirin A

龙血素 A

Loureirin A is a flavonoid extracted from the red resin of the herbs of Dracaena cochinchinensis, which is known as Dragon's Blood. Loureirin A inhibits platelet activation by an impairment of PI3K/Akt signaling. Loureirin A inhibits Akt phosphorylation.

GC32381 BF738735 BF738735是一种磷脂酰肌醇4-激酶IIIβ(PI4KIIIβ)抑制剂，IC50为5.7nM。

GC32254 Deltonin

三角叶薯蓣皂苷

Deltonin是从盾叶薯蓣中得到的甾体皂苷，能够抑制ERK1/2和AKT的活化，具有抗肿瘤的活性。

GC32199 T-00127_HEV1 T-00127_HEV1是一个phosphatidylinositol4-kinaseIIIbeta(PI4KB)抑制剂，其IC50值为60nM。

GC32163 BQR-695 (NVP-BQR695)

NVP-BQR695

An antimalarial compound

GC32118 KDU691 An antimalarial compound

GC31756 IPI-3063 IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5?±?1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.

GC31751 PI3Kδ-IN-2

YY-20394

PI3Kδ-IN-2 (YY-20394) 是 PI3K&#948 的强效、口服生物利用度和选择性抑制剂；提取自专利WO 2015055071 A1，化合物10； IC50 为 6.4 nM。

GC31666 Seletalisib (UCB5857)

UCB5857

Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold).

GC31661 APY0201 An inhibitor of PIKFYVE

GC31536 N-Oleoyl glycine

A putative substrate for peptidyl glycine α-amidating enzyme

GC31470 MK8722

(3S,3AS,6S,6AS)-6-((5-([1,1'-联苯]-4-基)-6-氯-1H-咪唑并[4,5-B]吡啶-2-基)氧基)六氢呋喃[3,2-B]呋喃-3-醇

MK-8722 is a potent, direct, allosteric activator of all 12 mammalian pan-AMPK complexes.

GC31411 EX229

AMPK Activator 991

An AMPK activator

GC31383 Chitosan oligosaccharide COS

壳聚糖低聚乳酸酯,COS

Chitosan oligosaccharide (COS) is an oligomer of β-(1?4)-linked d-glucosamine, of which actions involve the modulation of several important pathways including the suppression of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK) and the activation of AMP-activated protein kinase (AMPK).

GC31361 MK-3903 An AMPK activator

GC31348 7-Methoxyisoflavone

7-甲氧基异黄酮

A synthetic isoflavone

GC30884 LX2343 An inhibitor of BACE1 and PI3K

GC30777 PI4KIIIbeta-IN-10 PI4KIIIbeta-IN-10是一种有效的PI4KIIIβ抑制剂，IC50为3.6nM。

GC30770 LM22B-10 An activator of TrkB and TrkC

GC30582 Crosstide A peptide substrate for Akt

GC30229 Cbz-B3A Cbz-B3A是mTORC1转导的有效选择性抑制剂，与泛素1、2、4结合，Cbz-B3A还能抑制eIF4E结合蛋白的磷酸化。

GC30156 Brevianamide F (Cyclo(L-Pro-L-Trp))

Cyclo(L-Pro-L-Trp)

An alkaloid with diverse biological activities

GC30056 Danthron (Dantron)

1,8-二羟基蒽醌; Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone

Danthron (Chrysazin, Antrapurol) functions in regulating glucose and lipid metabolism by activating AMPK. Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron used to be a laxativa and now is currently used as an antioxidant in synthetic lubricants, in the synthesis of experimental antitumor agents, as a fungicide and as an intermediate for making dyes.

GC19471 Leniolisib

CDZ173

An inhibitor of PI3Kδ

GC19411 IITZ-01 IITZ-01 是一种有效的溶酶体自噬抑制剂，具有单剂抗肿瘤活性，对 PI3Kγ 的 IC50 为 2.62 μM。

GC19390 YU238259 An inhibitor of homology-dependent DNA repair

GC19355 Umbralisib

TGR-1202; RP5264

A PI3K p110δ inhibitor

GC19328 SF2523 A dual inhibitor of PI3K and BRD4

GC19300 PQR309

PQR309

PQR309 是一种有效的脑渗透性口服生物利用度泛 I 类 PI3K/mTOR 抑制剂，对 PI3Kα、PI3Kδ、PI3Kβ、PI3Kγ 和 mTOR 的 IC50 分别为 33nM、451nM、661nM、708nM 和 89nM .PQR309 在人脑胶质瘤细胞中通过抑制增殖、诱导细胞凋亡、诱导 G1 细胞周期停滞、抑制侵袭和迁移等方式发挥抗肿瘤作用。