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)