drak1

BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.

DRAK1/2-IN-2 (Compound Y17) is an inhibitor of DRAK1/2, with IC50 values of 353.2 nM for DRAK2 and 507.4 nM for DRAK1. This compound enhances mitochondrial membrane potential and glucose-stimulated insulin secretion (GSIS). It also combats lipotoxicity-induced apoptosis and significantly suppresses the secretion of the pro-inflammatory cytokine IL-1β, providing anti-inflammatory effects. Additionally, DRAK1/2-IN-2 significantly reduces blood glucose levels in mice and is applicable in diabetes research.

DRAK1/2-IN-1 is a potent inhibitor targeting both DRAK1 and DRAK2, displaying dissociation constants (Kd) of 1 µM and 6 µM, respectively.

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

DRAK2-IN-1 is a highly potent and selective ATP-competitive DRAK2 inhibitor with an IC₅₀ of 3 nM and a Kᵢ of 0.26 nM. It also inhibits DRAK1 with an IC₅₀ of 51 nM.

TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM. Additionally, TNIK-IN-3 demonstrates inhibitory activity against Flt4 (IC50 = 0.030 μM), Flt1 (IC50 = 0.191 μM), and DRAK1 (IC50 = 0.411 μM). This compound holds potential for carrying out research on colorectal cancer (CRC) [1].

CK156 is a potent inhibitor of death-associated protein kinase (DAPK), demonstrating high selectivity. In the DRAK1 NanoBRET assay, CK156 exhibits IC50 values of 182 nM, 34 μM, and 39 μM for DRAK1, CK2a1, and CK2a2, respectively. This compound is valuable for studying autoimmune and inflammatory diseases [1].