mst-1

IHMT-MST1-58 is a STE20-like protein 1 kinase (MST1) inhibitor (IC50:23 nM) with high efficiency, selectivity and oral activity. IHMT-MST1-58 can be used to study type 1 or type 2 diabetes.

XMU-MP-1 is a reversible and selective MST1/2 kinase inhibitor, and its IC50 values for MST1 and MST2 are 71.1 nM and 38.1 nM, respectively.

Cerdulatinib hydrochloride (PRT2070 hydrochloride) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.

Merestinib dihydrochloride (LY2801653 dihydrochloride) is an orally available kinase inhibitor with antitumor activity that inhibits MET, AXL, RON, and MKNK1/2, and inhibits the growth of NTRK fusion-carrying tumors.

U-104 (NSC-213841) is an effective carbonic anhydrase (CA) inhibitor for CA IX( Ki=45.1 nM) and CA XII(Ki=4.5 nM).

Sobuzoxane (MST 16) is an orally active inhibitor of topoisomerase II. It causes irreversible inhibition of cell division and is utilized in research on non-Hodgkin's lymphoma that is resistant to conventional chemotherapy or has relapsed.

Cerdulatinib (PRT2070) is an novel oral dual Syk/JAK inhibitor.

HPK1-IN-7 is an orally active HPK1 inhibitor. It shows selectivity against IRAK4 (59 nM) and GLK (140 nM).

Anti-MST1R Antibody (MOR07692) is a humanized IgG1 monoclonal antibody specifically targeting MST1R.

HTS05585 (Compound Hit-1) is a selective inhibitor of macrophage migration inhibitory factor (MIF) with a Kd value of 0.29 μM determined by microscale thermophoresis (MST) and confirmed through isothermal titration calorimetry (ITC) at 0.32 μM. It suppresses the release of pro-inflammatory factors (TNF-α, IL-6, IL-1β) in macrophages induced by LPS, making it a promising candidate for the study of inflammatory diseases such as sepsis.

BMSpep-57 hydrochloride, a potent macrocyclic peptide, competitively inhibits PD-1/PD-L1 interaction, exhibiting an IC50 value of 7.68 nM. It binds to PD-L1 with dissociation constants (Kds) of 19 nM and 19.88 nM as determined by MST and SPR assays, respectively. This compound enhances T cell functionality by promoting IL-2 production in PBMCs[1].

hnRNPK-IN-1 is a specific ligand that binds to the heterogeneous nuclear ribonucleoprotein K (hnRNPK) with high affinity, evidenced by Kd values of 4.6 μM and 2.6 μM determined using surface plasmon resonance (SPR) and microscale thermophoresis (MST), respectively. This binding event leads to the disruption of hnRNPK's interaction with the c-myc promoter, resulting in the inhibition of c-myc transcription. Additionally, hnRNPK-IN-1 induces apoptosis in Hela cells and exhibits potent anti-tumor activities[1].

Amycolatopsin A is a macrolide polyketide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 0.4 and 4.4 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin A is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 0.08 and 1.2 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

Amycolatopsin B is a bacterial metabolite originally isolated fromAmycolatopsisthat has anticancer activity.1It is cytotoxic to NCI H460 lung and SW620 colon cancer cells (IC50s = 0.28 and 0.14 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

Amycolatopsin C is a polyketide macrolide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 2.7 and 5.7 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin C is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 10 and 5.9 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

BMSpep-57, a potent macrocyclic peptide inhibitor, competitively disrupts the PD-1/PD-L1 interaction, demonstrating a significant inhibitory concentration (IC50) of 7.68 nM. It exhibits binding affinity towards PD-L1 with dissociation constants (Kd) of 19 nM and 19.88 nM in MicroScale Thermophoresis (MST) and Surface Plasmon Resonance (SPR) assays, respectively. This compound enhances T cell functionality by promoting Interleukin-2 (IL-2) production within Peripheral Blood Mononuclear Cells (PBMCs).

Conglobatin B1 is a compound that can be isolated from the Australian Streptomyces MST-91080. It exhibits cytotoxicity against the NS-1 myeloma cell line with an IC50 of 0.084 μg/mL, while demonstrating lower toxicity toward NFF human fibroblasts. Conglobatin B1 is applicable in tumor research.