nsd

NSD-1034 is an amino acid decarboxylase inhibitor.

Lem-14-1189, a LEM-14 derivative, is a potent NSD inhibitor of the nuclear receptor binding SET domain, and has inhibitory effects on NSD1, NSD2, and NSD3, with IC50 of 418 μM, 111 μM, and 60 μM, respectively. LEM-14-1189 has potential anticancer activity and can be used to study multiple myeloma (MM) and diseases of the blood system.

UNC8153 TFA is a selective and potent NSD2 protein degrader with anticancer activity.UNC8153 TFA induces NSD2 degradation in MM.1S multiple myeloma cells and inhibits the proliferation of MM.1S cells.

NSD-IN-4 (Compound A8) is a potent and orally active inhibitor of NSD3, inducing apoptosis in a dose-dependent manner. It demonstrates significant antitumor activity against lung squamous cell carcinoma.

NSD-IN-3 (compound 3) serves as a potent inhibitor of the nuclear receptor binding SET domain (NSD). It effectively targets NSD2-SET and NSD3-SET, displaying IC 50 values of 0.81 μM and 0.84 μM, respectively. This compound also impedes the dimethylation of histone H3K36 and suppresses the expression of genes targeted by NSDs in non-small cell lung cancer cells. Furthermore, NSD-IN-3 promotes s-phase cell cycle arrest and induces apoptosis [1].

NSD2-PWWP1-IN-3 (compound 36) is an effective inhibitor of NSD2-PWWP1, with an IC50 value of 8.05 µM. It has potential applications in cancer research.

NSD2-PWWP1-IN-2 (compound 33) is a potent NSD2-PWWP1 inhibitor, exhibiting an IC50 value of 1.49 µM, indicating its potential utility in cancer research.

NSD2-PWWP1-IN-1 (compound 31) is a potent inhibitor of NSD2-PWWP1 with an IC50 value of 0.64 µM, demonstrating potential applications in cancer research.

NSD2-PWWP1 ligand 1 (compound 34) is a small-molecule ligand that targets the NSD2-PWWP1 domain, with a potency of pIC50: 8.2. NSD2 is a large multidomain protein with functions in histone modification and reading. Dysregulation of the histone methyltransferase nuclear receptor binding SET domain 2 (NSD2) can lead to various hematological and solid malignancies. Binding of NSD2-PWWP1 ligand 1 to NSD2 reduces its enzymatic activity and inhibits tumor development.

(Rac)-NSD2-PWWP1-IN-4 (compound 7) is a potent inhibitor of NSD2-PWWP1, with IC50 and Kd values of 0.21 and 0.15 μM, respectively. This compound is useful for tumor research.

NSD2/H3K36me2 modulator-1 is an orally active modulator targeting NSD2/H3K36me2. It competitively binds to the SAM pocket of NSD2, effectively inhibiting NSD2 expression and H3K36me2 methylation. This compound can also reverse epithelial-mesenchymal transition (EMT), inhibit cell migration, and induce G0/G1 phase arrest and apoptosis (apoptosis). Additionally, NSD2/H3K36me2 modulator-1 reduces mitochondrial membrane potential (MMP) and promotes reactive oxygen species (ROS) generation. It is used in research for developing epigenetic anticancer strategies targeting NSD2 in hepatocellular carcinoma (HCC).

NSD2-PWWP1-IN-5 (Compound 13) is a potent inhibitor of NSD2-PWWP1, exhibiting a Kd of 78 nM. It competitively blocks NSD2-PWWP1 from recognizing H3K36me2 and DNA, thereby weakening its binding to nucleosomes. NSD2-PWWP1-IN-5 inhibits the proliferation of U2OS osteosarcoma cells and induces cell cycle arrest and apoptosis (apoptosis). This compound is useful in osteosarcoma research.

NSD2-IN-5 (Compound 198) is an NSD2 inhibitor with an IC50 value ranging from 0.001 μM to 0.01 μM. It is utilized for cancer research.

NSD2-PWWP1-IN-6 (Compound 16) is an effective NSD2-PWWP1 inhibitor with a Kd of 30 nM. It competitively blocks NSD2-PWWP1's recognition of H3K36me2 and DNA, thereby reducing its binding capacity to nucleosomes. NSD2-PWWP1-IN-6 is applicable for cancer research.

NSD2-IN-6 is a selective inhibitor of NSD2, with an IC50 of 3.8 nM for NSD2 and 274 nM for NSD1. It reduces H3K36me2 levels and reverses cellular plasticity by restoring androgen receptor (AR) signaling pathways. In organoid models, NSD2-IN-6 prompts a transition of cell states from cluster 2 and cluster 3 to cluster 1. In vivo, it exhibits antitumor activity by reversing tumor cell plasticity, inhibiting growth, and promoting apoptosis. NSD2-IN-6 is useful for research in prostate cancer.

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].

NSD3-IN-1, a histone methyltransferase NSD3 inhibitor, demonstrates an IC50 of 28.58 μM.

NSD3-IN-2, a potent inhibitor of NSD3, exhibits an IC50 value of 17.97 μM. It effectively inhibits the growth and proliferation of non-small cell lung cancer (NSCLC) cell lines, including H460, H1299, and H1650, demonstrating significant anticancer activity.

NSD3-IN-3, a potent inhibitor of NSD3, demonstrates significant anticancer activity by inhibiting the growth and proliferation of the non-small cell lung cancer cell line H460, with an IC50 value of 1.86 μM.

NSD2-IN-4 is a potent, selective inhibitor of the NSD2-SET domain, showing promise for the treatment of diseases related to NSD2 [1].

PROTAC NSD3 degrader-1 (compound 56) is a targeted degradation agent for the Nuclear receptor binding SET domain protein NSD3. It effectively induces NSD3 degradation in NCI-H1703 and A549 lung cancer cell lines, with DC50 values of 1.43 and 0.94 μM, respectively. Additionally, it hinders H3K36 methylation, triggers apoptosis, arrests the cell cycle, and diminishes the expression of NSD3-related genes, including CDC25A, ALDH1A1, and IGFBP.

Aldrin-transdiol is a metabolite of dieldrin. Aldrin-transdiol may be used in insecticides.

Transdermal Peptide is a 11-amino acid peptide, binds to Na+/K+-ATPase beta-subunit (ATP1B1), and enhances the transdermal delivery of many macromolecules. Transdermal Peptide (TD1) binds to ATP1B1, and mainly interacts with the C-terminus of ATP1B1 in yeast and mammalian cells. The interaction affects the expression and localization of ATP1B1 and epidermal structure, but can be antagonized by the exogenous competitor ATP1B1 or be inhibited by ouabain. Inhibition of Transdermal Peptide binding to ATP1B1 causes decreased delivery of macromolecular drugs across the skin[1]. [1]. Wang C, et al. Role of the Na(+)/K(+)-ATPase beta-subunit in peptide-mediated transdermal drug delivery. Mol Pharm. 2015 Apr 6;12(4):1259-67.

Transdermal Peptide TD-1 HCl is a novel peptide for enhanced transdermal drug delivery that facilitates the penetration of the skin barrier by several drugs and large hydrophilic proteins, such as insulin and human growth hormoneb.