haspinkinase

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).

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

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

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.

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

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.

Anticanceragent 285 is an orally active anticancer drug that acts as a potent and selective inhibitor of haspin, with an IC50 value of 18 nM. It is utilized in research on colorectal cancer.

FLT3-IN-38 (Flt-3 Inhibitor II) is a compound that acts as an FLT3 inhibitor. It also exhibits off-target effects by inhibiting the serine/threonine kinase haspin, a mitotic signaling coordinator. FLT3-IN-38 has potential applications in cancer research.

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 haspin kinase inhibitor with an IC50 value of 55 nM and approximately 180-fold selectivity over DYRK2 (IC50 = 9.9 μM), LDN-209929 represents an optimized analogue of LDN-192960 that is applied in cell cycle and mitotic regulation research to investigate haspin-dependent phosphorylation events.

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.

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.

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.

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