STK33 Inhibitor

ML281 is a highly selective inhibitor of serine/threonine kinase 33 (STK33) with an IC₅₀ value of 14 nM. ML281 shows 700-fold selectivity over PKA and 550-fold over AurB. ML281 exerts core mechanism by inhibiting STK33: in small cell lung cancer, ML281 downregulates RPS6/BAD signaling phosphorylation, induces apoptosis, and suppresses proliferation, invasion. ML281 reduces STK33-mediated 4-hydroxyphenylpyruvate dioxygenase (HPD) phosphorylation in tyrosinemia . ML281 is suitable for research on STK33 function, KRAS mutation-related cancers (pancreatic cancer, colon cancer, lung adenocarcinoma, etc.), small cell lung cancer, and tyrosinemia-related damage

CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC₅₀ of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive.

DLK-IN-1 (Compound 14) is an orally active, blood-brain barrier-penetrable and selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a K_i value of 3 nM. DLK-IN-1 inhibits Flt3, PAK4, STK33 and TrkA. DLK-IN-1 reduces p-c-Jun. DLK-IN-1 can be used in Alzheimer's disease research.

BRD-8899 is a STK33 inhibitor, with an IC₅₀ of 11 nM.

CDD-2211 is a STK33 inhibitor, with a K_d of 0.018 nM and an IC₅₀ of 5 nM. CDD-2211 has relatively weak inhibitory effects on off-target kinases, with IC₅₀ values of 115 nM for CLK1, 48 nM for CLK2, 187 nM for CLK4, and 78 nM for RET. CDD-2211 can be used for the study of contraception.

STK33-IN-1 (compound 1) is a STK33 inhibitor, with an IC₅₀ of 7 nM.

CDD-2210 is a STK33 inhibitor, with a K_d of 0.1 nM and an IC₅₀ of 38 nM. CDD-2210 has relatively weak inhibitory effects on off-target kinases, with IC₅₀ values of 1209 nM for CLK1, 917 nM for CLK2, 544 nM for CLK4, and 746 nM for RET. CDD-2210 can be used for the study of contraception.

CDD-2212 is a STK33 inhibitor, with a K_d of 1.9 nM and an IC₅₀ of 999 nM. CDD-2212 has relatively weak inhibitory effects on off-target kinases, with IC₅₀ values of 3223 nM for CLK1, 1555 nM for CLK2, 5884 nM for CLK4, and 1093 nM for RET. CDD-2212 can be used for the study of contraception.