sdma

SDMA (Symmetric dimethylarginine) is the most potent endogenous inhibitor of nitric oxide synthase (NOS), with higher levels in patients with end-stage renal disease (ESRD).

MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.

N,N'-Dimethylarginine-d6 (SDMA-d6) is a 2H-labeled N,N'-Dimethylarginine, a 202-Da methylated analog of the amino acid arginine, formed during post-translational methylation by methyltransferases.

SDMA p-Hydroxyazobenzene-p′-sulfonate is the p-hydroxyazobenzene-p′-sulfonate form of SDMA. It acts as an inhibitor of endogenous nitric oxide synthase (NO synthase) and serves as an activator of NF-κB, enhancing the expression of IL-6 and TNF-α. This compound remains stable in serum and plasma, making it a potential biomarker for liver and kidney dysfunction.

SDMA (Standard) is a reference standard for research and analysis in studies involving SDMA. SDMA (Symmetric dimethylarginine) is the most potent endogenous inhibitor of nitric oxide synthase (NOS), with higher levels in patients with end-stage renal disease (ESRD).

MRTX-1719 is a potent and selective inhibitor of the PRMT5/MTA complex with an IC50 value of <10 nM against PRMT5/MTAMTAPDELSDMA cell lines.

Dipentylone hydrochloride (Bk-dmbdp HCl) is a psychoactive synthetic cathinone and sympathomimetic stimulant. Its inhibitory activity towards the dopamine transporter (IC50=0.233µM) is tenfold higher than that towards NET and SERT, inhibiting dopamine uptake and stimulating locomotor activity in mice.

PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.

PRMT5-IN-50 is an orally active selective inhibitor of PRMT5, demonstrating good metabolic stability and low clearance in human liver microsomes. It inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50 values for symmetric arginine methylation inhibition at 1.0 and 536 nM, respectively, and antiproliferative IC50 values at 19 and 1620 nM, respectively. Additionally, PRMT5-IN-50 suppresses tumor growth in mice.

MRTX9768 hydrochloride is a potent, orally active PRMT5 inhibitor. MRTX9768 hydrochloride is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex[1]. MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1].MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors[2][1]. In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow[1]. [1]. Christopher R. Smith, et al. Abstract LB003: Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors. AACR Annual Meeting 2021; April 10-15, 2021 and May 17-21, 2021; Philadelphia, PA.[2]. Yingqing Chen, et al. Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms. Biomed Pharmacother. 2021 Oct 4;144:112252.