dapk

DAPK-IN-2 (WAY-380496) is a DAPK inhibitor. DAPK-IN-2 has potential anticancer activity, regulates autophagy and can be used to study cerebral infarction and ischemic diseases.

TC-DAPK 6 is an ATP-competitive inhibitor of Death-associated protein kinase (DAPK) with IC50s of 69 and 225 nM for DAPK1 and DAPK3.

DAPK Substrate Peptide acetate is a death-associated protein kinase (DAPK, Km = 9 μM) peptide substrate.

3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor. In cells expressing analog-sensitive Plk1 alleles, 3MB-PP1 blocks mitotic progression and cell division arise by targeting Plk1. 3MB-PP1 specifically inhibits analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase with IC50 of 2 μM. 3MB-PP1 can be used for the research of cell division and hypha formation of Candida albicans.

HS38 is a specific and ATP-competitive DAPK inhibitor with Kds of 300 nM, 200 nM, and 280 nM for DAPK1, PIM3, and ZIPK. HS38 can be used in studies about smooth muscle-related disorders.

HS94 (DAPK3 inhibitor HS94) is a selective and potent DAPK3 inhibitor with a Ki value of 126 nM for Pim kinase inhibition and can be used to study hypertension.

DAPK Substrate Peptide TFA is a synthetic peptide used as a substrate for the enzyme death-associated protein kinase (DAPK), with a Michaelis constant (Km) of 9 μM [1].

DAPK Substrate Peptide is a synthetic peptide substrate for death-associated protein kinase (DAPK) [Km = 9 μM].

DAPK1-IN-1 (compound 10) is an inhibitor of Death-associated protein kinase 1 (DAPK1), with a dissociation constant (Kd) of 0.63 μM. It is utilized in the study of Alzheimer's disease.

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].

Quinocetone is an animal growth promoter and potential anti-tumor activity.

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].

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.

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.

UNC9750 is an inhibitor of inositol phosphate multikinase (IPMK), with IC50 values of 31.6 nM for IPMK and 374 nM for IP6K2. It effectively suppresses the accumulation of InsP5, a direct product of IPMK kinase activity, without affecting InsP6 or InsP7 levels. Additionally, UNC9750 inhibits over 75% of the activity of four kinases: DAPK1, DYRK1B, PDGFR, and KDR. This compound is applicable in glioblastoma research.

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.

DIM-C-pPhCO2Me is an antagonist of nuclear receptor 4A1 (NR4A1).

HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor, displaying K_i values of 0.26 μM for DAPK3, 0.208 μM for Pim-3, 2.94 μM for Pim-1, and >100 μM for Pim-2. This compound effectively inhibits LC20 phosphorylation and smooth muscle contraction, and reduces blood pressure in spontaneously hypertensive mice, making it a valuable tool for hypertension research [HS-56].

SGC-STK17B-1 is a potent and selective inhibitor of STK17B/DRAK2 kinase.

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

HS148 is a selective inhibitor of DAPK3 (death-associated protein kinase 3), with a Ki value of 119 nM. Inhibition of DAPK3 by HS148 has been shown to reduce the progression of gastric cancer by activating the ULK1-dependent pathway, which is implicated in cellular autophagy and tumor suppression mechanisms.

TAT-GluN2BCTM is a membrane-permeable peptide that selectively targets active DAPK1 (Death-associated protein kinase 1) for lysosomal degradation, protecting neurons against oxidative stress and NMDAR-mediated excitotoxicity, making it valuable for neuroprotection research studies [1].

STK17A/B-IN-1 (compound 9) is an orally active, potent, and selective inhibitor of STK17A/B, demonstrating an IC50 of 23 nM for STK17A. This compound is utilized in tumor research.

STK17A/B-IN-1 hydrochloride is a potent, selective, orally active inhibitor of STK17A/B, displaying an IC50 value of 23 nM against STK17A. It is utilized in the research of tumors.