p70S6K Inhibitor

Sapanisertib (INK-128; MLN0128; TAK-228) is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.

PF-4708671 is a potent cell-permeable S6K1 inhibitor with a K_i of 20 nM and IC₅₀ of 160 nM.

LY-2584702 tosylate salt is a selective ATP competitive inhibitor of p70S6K with an IC₅₀ of 4 nM. In S6K1 enzyme assay, the IC₅₀ of LY-2584702 is 2 nM.

AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC₅₀s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.

AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC₅₀s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.

308-R is a SGK3/SGK1/S6K1 inhibitor. 308-R exhibits an IC₅₀ of 5 nM against human SGK3, an IC₅₀ of 10 nM against human SGK1, and an IC₅₀ of 1 nM against human S6K1. 308-R can be used in breast cancer research. It is also applicable to studies related to PROTAC synthesis, such as serving as the target protein ligand for PROTAC SGK3 degrader-2 (HY-176823).

CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC₅₀ of 6 μM and a K_i of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.

AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC₅₀s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.

TAS0612 is the orally active inhibitor of RSK、AKT and S6K. TAS0612 has antitumor activity.

AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC₅₀s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.

S6K1-IN-1 is a selective S6K1 inhibitor with an IC₅₀ value of 52 nM. S6K1-IN-1 can be used in the research of obesity and insulin resistance-related diseases.

Hu7691 is an orally active, selective Akt inhibitor with IC₅₀s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.

CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC₅₀ of 6 μM and a K_i of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.

Eudesmin ((-)-Eudesmin) impairs adipogenic differentiation via inhibition of S6K1 signaling pathway. Eudesmin possesses diverse therapeutic effects, including anti-tumor, anti-inflammatory, and anti-bacterial activities.

XL-418 is an orally active dual Akt and p70S6K inhibitor with IC₅₀s of 1 nM for Akt1 and 2 nM for p70S6K. XL-418 inhibits the phosphorylation of ribosomal protein S6 and GSK3β. XL-418 can be used for the study of prostate carcinoma and breast cancer.

LY-2584702 free base is a selective ATP competitive inhibitor of p70S6K with an IC₅₀ of 4 nM. In S6K1 enzyme assay, the IC₅₀ of LY-2584702 is 2 nM.

Hu7691 free base is an orally active, selective Akt inhibitor with IC₅₀s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice.

HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with K_d values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro.

DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation.