set 2

SET 2 is an antagonist of transient receptor potential vanilloid type 2(TRPV2) with an IC50 of 0.46 μM. SET 2 shows selectivity over TRPV1, TRPV3 and TRPV4.

PFI-2 is an effective, specific and cell-active lysine methyltransferase SETD7 inhibitor (Ki IC50: 0.33 2 nM), 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.

KTX-1001, also referred to as NSD2 inhibitor 161, is an innovative and potent inhibitor of nuclear SET domain-containing protein 2 (NSD2). This compound specifically binds to NSD2, inhibiting its catalytic activity and the mono- and dimethylation of histone H3 lysine 36 (H3K36). Such regulation impacts gene expression involved in cellular processes, including proliferation, which may subsequently slow cancer cell growth. NSD2 is part of the NSD family of histone lysine methyltransferases, which are often overexpressed and dysregulated in various cancer types.

ND-L11B is an effective degrader of the nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with DC50 values of 1.48 μM and 0.8 μM, respectively, and a Dmax close to 80%.

ND-L11B TFA is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with DC50 values of 1.48 μM and 0.8 μM, respectively, and a Dmax of approximately 80%.

JAK2-IN-7, a selective inhibitor targeting Janus Kinase 2 (JAK2), exhibits inhibitory concentrations (IC50) of 3 nM for JAK2, 11.7 nM for SET-2 cells, and 41 nM for Ba F3 V617F cells, indicative of its potency and selectivity. This compound demonstrates more than 14-fold selectivity against JAK1, JAK3, and FLT3, underlining its specificity. JAK2-IN-7 effectively induces cell cycle arrest at the G0 G1 phase and promotes apoptosis in tumor cells, manifesting significant antitumor activities [1].

PFI-2 hydrochloride ((R)-PFI-2 hydrochloride) is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-PFI-2.

NSD2-IN-1 (compound 38) is a potent and highly selective inhibitor of NSD2-PWWP1 (nuclear receptor-binding SET domain 2-PWWP1), with an IC50 value of 0.11 μM. By binding to NSD2-PWWP1, NSD2-IN-1 influences gene expression regulated by NSD2, resulting in apoptosis and cell cycle arrest [1].

BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1 2.

NMS-P953 is a JAK2 inhibitor, displaying significant tumor growth inhibition in SET-2 xenograft tumor model. NMS-P953 has a mechanism of action confirmed in vivo by typical modulation of known biomarkers, and with a favorable pharmacokinetic and safety profile.

MS159 is a potent PROTAC degrader targeting the nuclear receptor binding SET structural domain protein 2 (NSD2), which inhibits tumor cell growth. This compound serves as a valuable chemical tool for investigating NSD2's function in health and disease [1].

DC 432, a potent peptidomimetic inhibitor of N-terminal methyltransferase 1 2 (NTMT1 2) with an IC50 value of 54 nM, incorporates a BM30 peptide enhanced by five arginine residues. It effectively reduces the N-terminal methylation level of the regulator of chromosome condensation 1 and SET proteins in HCT116 cells, demonstrating cell permeability.