chk1 in 2

CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).

FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor targeting FLT3 and CHK1, with IC50 values of 25.63 nM for CHK1, 16.39 nM for FLT3-WT, and 22.80 nM for FLT-D835Y. It displays favorable oral pharmacokinetic properties and kinase selectivity. FLT3/CHK1-IN-2 is applicable in acute myeloid leukemia (AML) research.

GDC-0425 (RG-7602) is an orally administered, selective small molecule inhibitor of checkpoint kinase 1 (ChK1), used in research on various malignancies [1] [2].

p53 Stabilizer 2 (Compound 17a16) is a p53 stabilizing agent. It can induce S-phase arrest and apoptosis in both p53-functional and p53-deficient cancer cells. Additionally, p53 Stabilizer 2 triggers mitochondrial stress and activates two immune checkpoint pathways: NA-PKcs dependent p53 stabilization and the ATR-Chk1 axis activation. It also inhibits tumor growth in p53-deficient xenograft models.

CHK1-IN-8 (example 3-2) is an inhibitor of Chk1, exhibiting an IC50 of less than 10 nM against human Chk1. It is applicable for cancer research.

Potent Chk2 inhibitor (IC50 = 3 nM). Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes. Caldwell et al (2011) Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J.Med.Chem. 54 580 PMID:21186793

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cd

Ziptide, a peptide substrate, is recognized by several serine/threonine protein kinases, such as MAPK activated protein kinase 2 (MAPKAPK2), MAPKAPK3, MAPKAPK5, checkpoint kinase 1 (Chk1), AMP-activated protein kinase (AMPK), and calcium/calmodulin-dependent protein kinase II (CamKII). It serves as a tool in evaluating CamKII activity for the development of inhibitors.

Compound PROTAC-2, also known as PROTAC Chk1 degrader-1, is a potent degrader of Chk1, exhibiting a DC50 of 1.33 μM. It is utilized in cancer research [1].

Jaceosidin (Standard) is a reference standard for research and analysis in studies involving Jaceosidin. Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cdc2-cyclin B1 complex, followed by G2/M cell cycle arrest in endometrial cancer cells. Jaceosidin has immunosuppressive effect through inhibiting T cell proliferation and activation, which is closely associated with its potent down-regulation of the IFN-γ/STAT1/T-bet signaling pathway. The pharmacokinetics of Jaceosidin may be dramatically affected by polymorphic CYP1A2, UGT1A1, and UGT1A7 responsible for the metabolism of Jaceosidin or by the coadministration of relevant CYP1A2 or UGT inhibitors or inducers.

Phosphorylated CHKtide is a synthetic peptide substrate derived from CDC25C, phosphorylated by CHK1/CHK2 as part of one of the DNA repair pathways. It is utilized in assays for cell cycle checkpoint kinases 1 and 2 (CHK1/CHK2), as well as for salt-inducible kinase (SIK).