Haspin Kinase

LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM).

CHR-6494 is a haspin inhibitor that inhibits histone H3T3 phosphorylation (IC50: 2 nM).

INE963 demonstrates potent cellular activity against Pf 3D7 (EC50 = 6 nM) and achieves "artemisinin-like" kill kinetics in vitro with a parasite clearance time of <24 h. INE963 is also potent against P. falciparum and P. vivax clinical isolates from Brazil and Uganda with EC50's ranging from 0.01 to 7.0 nM

CHR-6494 TFA is a potent haspin inhibitor with an IC50 of 2 nM, inhibiting histone H3T3 phosphorylation. It induces apoptosis in cancer cells, including melanoma and breast cancer, and is useful for cancer research.

Haspin-IN-3 is a potent haspin inhibitor with an IC50 of 14 nM.Haspin-IN-3 has anticancer activity.

AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Which Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL).

LDN-192960 hydrochloride is an inhibitor of Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) and Haspin, with IC50 values of 48 nM and 10 nM, respectively.

MU1920 is an ATP-competitive, selective inhibitor of haspin with an IC50 of 6 nM. In mouse plasma and microsomes, it demonstrates favorable pharmacokinetic properties and metabolic stability. Although it lacks significant anticancer activity, MU1920 is suitable for developing chemical probes.

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

Haspin-IN-1 (compound 2a) is an inhibitor of haspin (haploid germ cell-specific nuclear protein kinase) with an IC50 of 119 nM. It also inhibits CLK1, DYRK1A, and CDK9 with IC50 values of 221 nM, 916.3 nM, and 406.8 nM, respectively. Haspin-IN-1 has potential for developing new anticancer drugs [1].

LDN-209929 dihydrochloride is a potent and selective inhibitor of haspin kinase (IC50= 55 nM), demonstrating 180-fold selectivity versus DYRK2 (IC50= 9.9 μM).

HSK205 is a dual FLT3 and haspin inhibitor, exhibiting potent antitumor activity [1], with an IC50 of 0.187 nM for FLT3.

Haspin-IN-4 (Compound 60) is a selective Haspin inhibitor with an IC50 of 0.01 nM and exhibits anticancer activity, making it suitable for cancer research.

MELK-8a (NVS-MELK8a) is a potent and selective inhibitor of maternal embryonic leucine zipper kinase (MELK), with an IC50 of 2 nM and an IC50 of 0.42 μM in cellular assays. MELK is crucial in regulating mitosis in cancer cells.

LDN-209929 2HCl is a potent and selective inhibitor of haspin kinase.