Novel inhibitors

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Cat. No.	Product Name	Field of Application
DC23748	ML372 Featured	ML372 is a small molecule SMN modulator that increases SMN protein in patient fibroblasts with EC50 of 37 nM; possesses good potency, pharmacokinetics, tolerance, and CNS penetration that are able to increase levels of SMN protein in several model cell lines; increase SMN protein levels in vivo, restore motor function, and prolong survival of SMNΔ7 SMA Mice; improves the righting reflex and extended survival of a severe mouse model of SMA.
DC23445	ML375	ML375 (VU-0483253) is a potent, highly selective M5 NAM with submicromolar potency (human M5 IC50=300 nM, rat M5 IC50=790 nM, M1-M4 IC50> 30 uM), exhibts excellent multispecies PK, high CNS penetration, and enantiospecific inhibition..
DC21327	ML377	ML377 (MLS 0472732) is a small molecule probe that selectively inhibits TAG (Triacylglyceride) accumulation with an IC50 of 1.1 uM, show >45-fold selectivity versus DGAT inhibition and cytotoxicity..
DC20901	ML378	ML378 (CID71710938, JJH-254) is an in vivo active carbamate-based dual inhibitor of lysophospholipase LYPLA1 (APT1) and LYPLA2 (APT2) with IC50 of 122 nM and 245 nM, repectively.
DC23285	ML379	ML379 (CID71576758) is a potent, selective TP53 mutant cancer cells inhibitor with IC50 of 13 nM in sensitive HeLa cells (TP53 mutant).
DC23512	ML381 (VU0488130) Featured	ML381 (VU0488130) is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM).
DC20900	ML382 Featured	ML382 is a potent, selective, positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MrgprX1) with EC50 of 190 nM in cell based Ca2+ imaging assay.
DC20897	ML387	ML387 (CID3474778) is a potent, selective NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD) inhibitor with IC50 of 19 nM.
DC20899	ML388	ML388 is a potent, selective NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD) inhibitor with IC50 of 34 nM.
DC23446	ML389	ML389 is a highly potent, selective vasopressin receptor 1a (V1a-R) antagonist with IC50 of 40 nM.
DC21808	ML395	ML395 is a potent, selective, allosteric phospholipase D2 (PLD2) inhibitor with cellular IC50 of 360 nM, shows >80-fold selectivity over PLD1 (IC50>30 uM).
DC23488	ML398	ML398 (CID72737723) is a potent, selective, highly brain penetrant dopamine 4 (D4) receptor antagonist with IC50/Ki of 130 nM/60 nM.
DC21810	ML399	ML399 (VU0516340) is a potent and cell penetrant menin-MLL inhibitor with IC50 of 90 nM.
DC20903	ML401 (CID73169083) Featured	ML401 (CID73169083) is a potent, functional antagonist of EBI-2 (Epstein-Barr virus-induced gene 2) with IC50 of 1 nM, displays activity in a chemotaxis assay (IC50=6 nM).
DC20902	ML404	ML404 is a small molecule inhibitor of mtPTP, inhibits mitochondrial swelling with EC50 of 4.9 nM, shows no effect on mitochondrial coupling at >100 uM.
DC20456	ML-406 Featured	ML406 is a small molecule Mtb bioA (DAPA synthase) enzyme inhibitor (IC50=30 nM) that shows anti-tubercular activity, dispalys >100-fold selectivity over bioD.
DC21322	ML-60218 Featured	ML-60218 (ML60218) is a broad-spectrum, small molecule inhibitor of RNA polymerase (Pol) III with IC50 of 32 and 27 uM for Saccharomyces cerevisiae and human, respectively.
DC20457	ML-9 hydrochloride Featured	ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
DC22158	MLAF50	MLAF50 is the first small-molecule inhibitor of the REV1 UBM2-Ubiquitin interaction, directly binds to REV1 UBM2 with Kd of 37 uM in SPR assays.
DC10360	MLi-2 Featured	MLi-2 is an a potent, highly selective, orally available, brain penetrant inhibitor of LRRK2 with an IC50 of 0.76 nM.
DC23469	MLN 3897	MLN 3897 is a potent, specific and orally active antagonist of CCR1 with IC50 of 0.8 nM in competition binding assays, 500-fold selectivity over CCR5.
DC7469	MLN0905	MLN0905 is a mall-molecule and potent inhibitor of PLK1 with IC50 of 2 nM.
DC5086	Ixazomib(MLN2238) Featured	MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM.
DC23447	MLN3126	MLN3126 (MLN 3126, MLN-3126) is a potent, selective, orally available CCR9 antagonist with IC50 of 6.3 nM (CCL25-induced calcium mobilization).
DC12255	MLN-4760 Featured	MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).
DC9365	MLN8054 Featured	MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM; exhibits more than 40-fold selective for Aurora A than Aurora B.
DC10221	MLR-1023	MLR-1023 is a chemical compound which inhibits acid secretion in animal models and also acts as a bronchodilator in histamine-challenged animals.
DC21328	MLS 0038949	MLS 0038949 is a potent, selective tissue-nonspecific alkaline phosphatase (TNAP) inhibitor with IC50 of 0.19 uM, shows no activity against IAP and PLAP (IC50>100 uM).
DC21329	MLS 0263839 Featured	MLS 0263839 is a potent, specific inhibitor of the phosphatase PHOSPHO1 with IC50 of 0.14 uM, shows minimal cross-inhibition of TNAP and no inhibition of ENPP1 activity.
DC21326	MLS-0322825	MLS-0322825 is a novel potent low-molecular-weight protein tyrosine phosphatase (LMPTP) inhibitor with IC50 of 3.3 uM.

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Novel inhibitors

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