Haspin Kinase Inhibitor

CHR-6494 is a potent inhibitor of haspin, with an IC₅₀ of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer.

INE963 is a potent and fast-acting blood-stage antimalarial agent, with an EC₅₀s of 3-6 nM. INE963 is potential for single-dose cures in uncomplicated malaria.

Haspin-IN-3 (compound 8l) is a potent haspin inhibitor with IC₅₀ of 14 nM. Haspin-IN-3 has anticancer effects.

LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC₅₀s of 10 nM and 48 nM, respectively.

LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC₅₀s of 10 nM and 48 nM, respectively.

LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC₅₀=55 nM) with180-fold selectivity verses DYRK2 (IC₅₀=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 (HY-13455).

MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC₅₀ of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC₅₀s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells.

MU1920 is an ATP-competitive, selective inhibitor for haspin with an IC₅₀ of 6 nM. MU1920 exhibits good pharmacokinetic properties and metabolic stability in mouse plasma and microsomes without obvious anticancer effects, which can be used for development of chemical probes.

HSK205 is a dual FLT3 and haspin inhibitor, with IC₅₀ of 0.187 nM for FLT3. HSK205 has antitumor activity.

Haspin-IN-2 (compound 4) is a potent and selective haspin inhibitor with an IC₅₀ of 50 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC₅₀s of 445 nM and 917 nM, respectively.

Haspin-IN-4 (Compound 60) is a selective inhibitor of Haspin with an IC₅₀ value of 0.01 nM. Haspin-IN-4 possesses anticancer activity and can be used in cancer research.

Anticancer agent 285 is an orally active anticancer agent with highly effective and selective haspin-inhibiting IC₅₀ = 18 nM) activity. Anticancer agent 285 can be used for the study of colorectal cancer_[1].

Haspin-IN-1 (compound 2a) is a haspin inhibitor with an IC₅₀ of 119 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC₅₀s of 221 nM and 916.3 nM, respectively.

CHR-6494 TFA is a potent inhibitor of haspin, with an IC₅₀ of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer.

LDN-209929 is a potent haspin kinase inhibitor, with IC₅₀ values of 55 nM and 9.9 μM for Haspin and DYRK2, respectively.

FLT3-IN-38 (Flt-3 Inhibitor II) is a FLT3 inhibitor. FLT3-IN-38 has off-target effects and inhibits serine/threonine kinase haspin. Haspin is a mitotic signal coordinator. FLT3-IN-38 can be used for cancer research.