NU7441 (KU-57788)

Non-specific DNA-PK Inhibitor

PI-103 : DNA-PK, IC50=23 nM; p110α/β/δ/γ, IC50=2 nM/3 nM/3 nM/15 nM; mTOR, IC50=30 nM.

Most Potent DNA-PK Inhibitor

PIK-75 : DNA-PK, IC50=2 nM.

Newest DNA-PK Inhibitor

KU-0060648 : Dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.

Classic DNA-PK Inhibitor

NU7026 : Potent DNA-PK inhibitor with IC50 of 0.23 μM, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR.

CHIR-99021 (CT99021) ^New

CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.

Dorsomorphin (Compound C) ^New

Dorsomorphin is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.

MHY1485 ^New

MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.

NU7026

NU7026 is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR.

KU-0060648

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.

Rapamycin (Sirolimus)

Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

MK-2206 2HCl

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

Features:The first allosteric small molecule inhibitor of Akt to enter clinical development.

CHIR-99021 (CT99021) HCl

CHIR-99021 HCl (CT99021) is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2.

LY294002

LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family.

3-Methyladenine (3-MA)

3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. Solutions of 3-MA are best fresh-prepared by heating.