NR-160 (NR160) is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 30 nM, shows SI (75-1847 )over all HDAC class I isoforms.NR-160 induced α-tubulin acetylation (ac-α-tubulin) in treated acute myeloid leukemic (AML) cell line HL60, but not histone H3 (ac-H3) (a marker for the inhibition of class I HDACs).NR-160 enhances the cytotoxicity induction of bortezomib, epirubicin and daunorubicin on a panel of seven leukemia cell lines

NPG9 (NSR inhibitor NPG9) is a small molecule inhibitor of streptococcus agalactiaenisin resistance protein (NSR) with 58% inhibition at 100 uM (specific growth inhibition assay).

NPD4928 (NPD 4928) is a small molecule that enhances ferroptosis via inhibition of ferroptosis suppressor protein 1 (FSP1).NPD4928 enhanced the sensitivity of various cancer cells to GPX4 inhibitor RSL3.

NP627 (NP-627) is a specific small-molecule inhibitor of protein kinase C deltaI (PKCδI) with Kd of 1 nM.NP627 inhibits the cleavage of PKCδI in adipocyte (at 10 nM) and decreases PKCδI kinase activity.NP627 does not inhibit other PKC isozyme activities.NP627 prevents caspase-3 mediated cleavage of PKCδI, significantly inhibits PKCδI catalytic fragment release, decreases inflammation and apoptosis, and significantly improves mitochondrial metabolism in human adipocytes from obese individuals.

NP10679 (NP 10679) is a potent, orally active, NMDA receptor subunit 2B (GluN2B)-selective inhibitor of NMDA receptor with IC50 of 23 nM, with no significant effect on GluN2A/C/D (IC50>100 uM).NP10679 demonstrates high pH sensitivity, NP10679 exhibits both a potent IC50 at pH 6.9 of 23 nM with a ratio of IC50 at pH 7.6 to that at pH 6.9 (referred to as pH Boost) of 6.2 fold.NP10679 reduced infarct volume n a dose-dependent manner with an ED50 of 1 mg/kg IP dose and a maximum infarct volume reduction of 52% in MCAo experiments.NP10679 perturbed motor coordination or function in mice.

NOS31 is a potent, selective NADPH oxidase 1 (Nox1) inhibitor with IC50 of 2.0 uM.NOS31 inhibited ROS production in CaCO2 cells in a dose-dependent manner, inhibits NOXO1/NOXA1-induced ROS production.NOS31 is much less potent with other Nox enzymes Nox2, Nox3, Nox4, and Nox5 in HEK293 reconstitution systems (>15-fold selectivity).NOS31 inhibited the proliferation of several colon cancer cell lines in vitro (CaCO2, HT-29, DLD-1, RKO, and HCT-116), with no direct antioxidant activity nor cytotoxity.

NN-390 (NN390) is a potent, selective HDAC6 inhibitor with IC50 of 9.8 nM, >200-550-fold selectivity over other HDAC isoforms.NN-390 inhibits primary cells of treatment-refractory Group 3 MB cells (SU_MB002) with IC50 of 2.33 uM.NN-390 is the first HDAC6-selective inhibitor to show therapeutic potential in metastatic Group 3 medulloblastoma (MB), an aggressive pediatric brain tumor often associated with leptomeningeal metastases and therapy resistance.NN-390 selectively targets cell population with a 44.3-fold therapeutic margin between patient-derived Group 3 MB cells in comparison to healthy neural stem cells.NN-390 demonstrated a 45-fold increased potency over HDAC6-selective clinical candidate citarinostat.

NLRP3-IN-3 is a potent and selective inhibitor of NLRP3 inflammasome with IC50 of 1.26 nM in THP1 cells, showing good pharmacokinetic profiles with oral bioavailability.

NHB1109 is a potent, selective, orally active PTPRD phosphatase inhibitor with IC50 of 0.6 uM, displays selectivity over PTPRS, PTPRF, PTPRJ or PTPN1/PTP1B phosphatases.NHB1109 exhibited no substantial potency at other protein tyrosine phosphatases screened, no significant potency at any of the targets of clinically-useful drugs identified in EUROFINS screens.NHB1109 (200 mg/kg) is well tolerated by mice.NHB1109 is a good candidate to advance to in vivo studies in addiction paradigms and toward human use to reduce reward from addictive substances.

NH4-6 is a potent, selective pan SIRT1-3 inhibitor with IC50 of 3.0/0.032/2.3 uM for SIRT1/2/3, respectively.NH4-6 does not inhibits SIRT5 and SIRT6.NH4-6 (30 mg/kg) significantly impaired tumor growth in HCT-116 tumor xenograft.

NH4-13 is a potent, SIRT2-selective inhibitor with IC50 of 87 nM, no inhibition against SIRT1/3/5/6 (CI50>50 uM).NH4-13 (30 mg/kg) significantly impaired tumor growth in HCT-116 tumor xenograft.

NEU-4438 (NEU4438) is a potent inhibitor of P. falciparum with EC50 of 13 nM (T. brucei), demonstrates improved aqueous solubility (880 uM) compared to NEU-1953; reduced parasitemia 109 fold in trypanosome-infected mice.

NDI-031407 (NDI 031407) is a novel potent, selective TYK2 inhibitor with IC50 of 0.21 nM in radiometric assays, 20 fold selectivity over JAK3 (4.2 nM), 147 fold for JAK2 (31 nM), and 220 fold for JAK1 (46 nM).NDI-031407 has high potency in cell line and primary cell assays for TYK2-dependent cytokines (IL-12, IC50=118 nM) over TYK2-independent cytokines (GM-CSF).NDI-031407 blocks IL-23–induced STAT3 phosphorylation and IL-17A production in human CD4+ T cells.NDI-031407 inhibits disease progression in the SKG model of Spondyloarthritis (SpA).NDI-031407 suppresses systemic IL-23–induced type 3 immunity in vivo.

ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM; ND2158 demonstrates high selectivity against 334 kinases, and >1000-fold over IRAK1. ND2158 blocked TNF production, collagen-induced arthritis, and gout formation in mice, suppressed LPS-induced TNF production, alleviated collagen-induced arthritis, and blocked gout formation in mouse models. IRAK4 inhibition promoted killing of ABC DLBCL lines harboring MYD88 L265P, by down-modulating survival signals, including NF-κB and autocrine IL-6/IL-10 engagement of the JAK-STAT3 pathway. In ABC DLBCL xenograft models, IRAK4 inhibition suppressed tumor growth as a single agent, and in combination with the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib or the Bcl-2 inhibitor ABT-199.

NCATS-SM5637 (NSC 791985) is a potent, selective mutant IDH1 inhibitor with IC50 of 81/72 nM for IDH1 mutant R132H/R132C, respctively.NCATS-SM5637 showed higher tumoral concentrations that corresponded to lower 2-HG concentrations in engineered mIDH1-U87-xenograft mouse model, compared with the approved drug AG-120 (ivosidenib).

NBI-98782 (alpha-dihydrotetrabenazine) is a potent, selective vesicular monoamine transporter (VMAT2, SLC18A2) inhibitor with Ki of 0.97 nM.Acute NBI-98782 decreased mPFC, dSTR, hippocampus, and NAC DA, 5-HT, and NE efflux, while increasing that of DOPAC, HVA, and 5-HIAA.NBI-98782 suppressed clozapine-, olanzapine- and risperidone-induced DA efflux in both mPFC and dSTR, and ACh efflux in mPFC.NBI-98782 attenuated PCP-induced DA, 5-HT, NE and Glu efflux, and AMPH-induced DA and NE efflux, in both mPFC and dSTR, as well as PCP- and AMPH-induced hyperlocomotion.

NBD-14273 is a CD4-mimetic, small-molecule HIV-1 entry inhibitor with IC50 of 0.13 uM.NBD-14273 showed both improved antiviral activity and selectivity index (SI) against HIV-1HXB2 compared to NBD-14136.NBD-14273 displayed potenct against a large panel of 50 HIV-1 Env-pseudotyped viruses representing clinical isolates of diverse subtypes.

NaV1.7 inhibitor 51 is a highly potent, selective, orally active NaV1.7 inhibitor with IC50 of 10.7 nM in FLIPR membrane potential assay, no significant activity against NaV1.5 (IC50>10 uM).NaV1.7 inhibitor 51 shows good selectivity against other NaV isoforms and minimal inhibition at 10 uM for the resting state across different NaV isoforms.NaV1.7 inhibitor 51 exhibits state-dependent block of human, monkey, and mouse NaV1.7 with a similar potency range.NaV1.7 inhibitor 51 shows significant effects on the CCI-induced neuropathic pain model.

NAH-C3-GPKK is a potent, selective protein N-terminal methyltransferase 1 (NTMT1) bisubstrate inhibitor with Kiapp of 7 nM in endogenous proteomes.NAH-C3-GPKK also potently inhibit a methyltransferase complex HemK2-Trm112 (also known as KMT9-Trm112, IC50=0.3 uM).NAH-C3-GPKK is the first potent inhibitor for HemK2/KMT9.

N205 is a novel anti-malaria compound with in vitro IC50 of 1.3 nM against Plasmodium falciparum (3D7); demonstrates excellent rodent pharmacokinetic and in vivo antimalarial efficacy studies in the mouse Plasmodium berghei and Plasmodium falciparum Pf3D70087/N9 severe combined immunodeficiency (SCID) mouse models.

MyoMed-946 is a small moelcule that inhibits MuRF1 (TRIM63) activity and MuRF1/MuRF2 expression; MyoMed-946 inhibits MuRF1 expression/activity in vivo and is able to attenuate skeletal muscle atrophy and dysfunction in mice treated with monocrotaline to induce right ventricular hypertrophy and subsequent cardiac cachexia. MyoMed-946 attenuates skeletal muscle strength loss in mouse model for type 2 diabetes mellitus (T2DM), with no significant effects on serum glucose. MyoMed-946 attenuates induction of MuRF1 in tumor stressed muscles. MyoMed-946 also rescues citrate synthase and complex-1 activities in tumor-stressed muscles. MuRF1 (muscle-specific RING finger protein-1) is a muscle-specific ubiquitin ligase that regulates muscle catabolism during chronic wasting states, both MuRF1 and MuRF2 participate in glucose and, also, in lipid regulation.

MV1035 (MV-1035) is a novel small molecule that reduce U87 GBM cells migration and invasiveness, targeting m6A demethylase ALKBH5, also inhibits ALKBH2; MV1035 directly inhibits active recombinant ALKBH5 protein and, consequently, negatively regulates CD73 protein expression without affecting CD73 mRNA transcription. In PD-GSCs, MV1035 has a synergistic effect with TMZ in reducing cell viability and their ability to form spheres. MV1035 is able both to reduce the expression of MGMT and to inhibit ALKBH2 activity.

MU1787 is a potent, highly selective HIPK inhibitor with IC50 of 285/123/283 nM for HIPK1/2/3, repectively.MU1787 is highly selective across the kinome in a broad panel of 373 human kinases, does not inhibits HIPK4 at 10 uM.

MU1700 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 13 and 6 nM, respectively.MU1700 inhibits only ALK1/2/6 and no additional off targets by kinome-wide screening against 369 protein kinases at 1 uM.MU1700 affects phosphorylation of SMAD1/5/8 that corresponds to BMP branch of signalling wchich is mediated also by ALK1/2 kinases.MU1700 is suitable chemical probe for in vivo disease models, and has remarkably high brain penetrance (mice, PO, 1 g/kg).

MU1656 (MU 1656 ) is a potent, highly selective inhibitor of histone methyltransferase DOT1L with IC50 of 2 nM; MU1656 displays highly selectively against a panel of 37 methyltransferases. MU1656 is more metabolically stable and significantly less toxic in vivo than pinometostat.

Mtb CoaBC inhibitor 1f is a direct small molecule inhibitor of Mtb 4'-phosphopantothenoyl-l-cysteine synthetase (PPCS, CoaB) domain of the bifunctional Mtb CoaBC (IC50=15.6 uM).Mtb CoaBC inhibitor 1f inhibit CoaBC uncompetitively with respect to 4'-phosphopantothenate, the substrate for the CoaB-catalyzed reaction.Mtb CoaBC inhibitor 1f inhibits Mtb growth in whole-cell activity against Mtb H37Rv (MIC=25.9 uM).

MT16-205 (MT 16-205) is a potent, selective, covalent UCHL1 inhibitor with IC50 of 600 nM, no inhibition agianst UCHL3 (IC50>10 uM).MT16-205 inhibited both UCHL1 and the structurally unrelated DUB USP30 with similar potency.MT16-205 displayed cell proliferation cytotoxicity in human embryonic kidney cells (HEK293) with IC50 of 350 nM, MT16-205 effectively engaged UCHL1 in cells with IC50 of 830 nM.

MT16-001 is a selective, covalent inhibitor of deubiquitinating enzyme UCHL1 with IC50 of 580 nM, no inhibitory effect against UCHL3 (IC50>30 uM).MT16-001 inhibits structurally unrelated DUB USP30 with similar potency.MT16-001 showed cytotoxicity in human embryonic kidney cells (HEK293) with EC50 of 730 nM, effectively engaged UCHL1 in cells with EC50 of 550 nM.MT16-001 showed excellent selectivity for UCHL1 across the UCH family: UCHL1, UCHL3, UCHL5 and BAP1.

MSC2711186 is a potent, selective, cell active pan-SRPK with IC50 of 2.7/8.1/0.59 nM for SRPK1/2/3, repectively.MSC2711186 does not show any activity towards the CLKs, and is selective in an in vitro kinase panel from Reaction Biology at 1 µM against 395 Kinases.MSC2711186 displayed an IC50 of 98 nM on SRPK1 and 40 nM on SRPK3 in intact cells and 44 nM on SRPK1, 149 nM on SRPK2 and 40nM on SRPK3 in lysed cells in NanoBRETTM assay.Serine-arginine protein kinases (SPRKs) are a subfamily of serine-threonine kinases, regulating pre-mRNA splicing in response to extracellular stimuli by phosphorylating serine/arginine (SR)-rich splicing factors. The human genome encodes three SRPK genes, SRPK1, SRPK2 and SRPK3. While SRPK1 has been detected in many human tissues at varying expression levels, SRPK2 and SRPK3 exhibit a more tissue-specific expression.

MS910 (MS-910) is the first CRBN-recruiting MEK1/2 degrader (PROTC) with HT29 DC50 of 118/55 nM for MEK1/2 degradation, respectively.MS910 displays antiproliferation potency against HT29 cell with GI50 of 330 nM, degrade MEK1 and MEK2 and inhibit pERK signaling in a time-dependent manner.