Nigratine (6E11) is a highly specific, non-ATP competitive inhibitor of RIPK1 kinase (IC50=1.6 uM), inhibits necroptosis and ferroptosis.Nigratine inhibits necroptotic cell-death induced by TNF-α in Jurkat-Fadd def cells with IC50 of 4.6 uM.Nigratine is significantly more potent than the specific RIPK1 necroptosis inhibitor, Nec-1s.Nigratine (50 uM) strongly inhibits the ferroptotic cell death induced by excess of glutamate, erastin, and RSL3, in both murine HT22 and human SH-SY5Y cell lines, protects SH-SY5Y human neuroblastoma cell line from cell death triggered by both class I and II-inducers of ferroptosis.Nigratine protects porcine kidney epithelial LLC-PK1 cell line from lipid peroxidation and cell death triggered by RSL3.Nigratine protects human bronchial organoids from necroptosis and ferroptosis.

TRIM24 inhibitor X is a potent TRIM24 bromodomain inhibitor for synthesis dTRIM24..

Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.

A small molecule inhibitor (IC50=0.3 uM) of DEAD-box polypeptide 3 (DDX3), a human host factor required for the replication of several DNA and RNA viruses.

Potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2)

Tinlarebant (LBS-008) is an orally active non-retinoid RBP4 (retinol-binding protein 4) antagonist. Tinlarebant can be used for the research of the Stargardt disease.

ALK-001 is a vitamin A analog potentially for the treatment of Stargardt’s disease.

Encequidar (HM30181) is a potent selective inhibitor of MDR1 (ABCB1, P-gp) with IC50 of 0.63 nM.Encequidar (HM30181) effectively blocked transepithelial transport of paclitaxel in MDCK monolayers.Encequidar (HM30181) does not inhibit MRP1 (ABCC1), MRP2 (ABCC2), and MRP3 (ABCC3), and partially inhibited BCRP (ABCG2) only at very high concentrations.Oral co-administration of paclitaxel and HM30181 showed a tumor-inhibitory strength equal or superior to that of intravenous paclitaxel in the xenograft model in nude mice.

SS-1-148 is a potent, selective inhibitor of human ornithine δ-aminotransferase (hOAT) with Ki of 60 uM, shows excellent selectivity over other related aminotransferases (e.g., GABA-AT).

E1231 (E-1231) is a small molecule SIRT1 activator with EC50 of 0.83 uM, interactes with recombinant human SIRT1 protein and deacetylated liver X receptor-alpha (LXRα).

AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with Kds of 1.8 and 3.1 μM, respectively.

7,12-Dimethylbenz[a]anthracene (DMBA) is an immunosuppressor as well as a potent organ-specific carcinogen.

Macrocyclic peptide D4-2 is a macrocyclic peptide consisting of 15 amino acids that binds to the ectodomain of mouse SIRPα (Kd=10 nM, IgV-B6 SIRPα) and efficiently blocks CD47-SIRPα interaction in an allosteric manner (IC50=0.18 uM).

Darizmetinib (HRX-0215, HRX0215) is a potent, selective inhibitor of MKK4 (MAP2K4/SEK1), shows potential for promoting liver regeneration or reducing or preventing hepatocyte death.

Myt1-IN-4 (compound 181) is a potent Myt1 inhibitor with an IC50 of <10 nM. Myt1-IN-4 has anticancer effects.

GZD824 dimesylate (HQP1351 dimesylate) is an orally bioavailable pan-Bcr-Abl inhibitor with potency against a wide range of Bcr-Abl mutants and the native enzyme (IC50=0.34 nM). GZD824 dimesylate has antitumor activity.

MMV-667492 (MMV 667492, MMV667492) is a novel potent Ezrin inhibitor with Kd of 29.4 nM.

RAS activator compound 1 is a small molecule RAS activator compound that increases the rate of SOS-catalyzed nucleotide exchange in vitro with EC50 of 14 uM; targets SOS1 induced biphasic modulation of RAS-GTP and ERK phosphorylation levels, through negative feedback on SOS1 that regulates the interaction between SOS1 and GRB2.

AK778 (Col001) is a small-molecule compound that inhibits the interaction of Hsp47 with collagen, competitively inhibits the interaction and causes the inhibition of collagen secretion by destabilizing the collagen triple helix. .

LXRβ agonist 17 is a novel, potent, orally active liver X receptor β (LXRβ) agonist with Ki/EC50 of 3/21 nM, displays 27-fold selectivity over LXRα; also exhibits excellent selectivity against other nuclear hormone receptors (>3,000-fold); induces the expression of LXR target genes in vitro and in vivo.

MRTX-282 is a novel KRas G12D inhibitor.

Cenobamate, a sodium channel blocker, enhances GABAergic transmission and has the potential to be a versatile CNS drug.

NNZ2591 (cyclo-L-glycyl-L-2-allylproline)1 is an investigational synthetic analog of cyclic glycine-proline (cGP), a breakdown product of human insulin-like growth factor 1 (IGF-1), that has been chemically modified to increase its half-life, stability, and oral bioavailability.

DYRK2 inhibitor C17 is a potent, selective DYRK2 inhibitor with IC50 of 9 nM, weakly inhibits DYRK3 (IC50=68 nM), and does not inhibit DYRK1A/1B (IC50>2000 nM).C17 showed outstanding selectivity for the human kinome containing 467 other human kinases.C17 showed synergistic 4E-BP1 phosphorylation suppression combined with AKT and MEK inhibitors.C17 impeded the store-operated calcium entry process (ORAI1 channel).

RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM.

SJ432 (SJ-432) is a potent, highly selective BET BD2 inhibitor with Kd of 6/2 nM (BRD2-BD2/BRD4-BD2), displays 80/152-fold selectivity over BD1, respectively.SJ432 is more water soluble than SJ018 (40 uM vs <0.1 uM).SJ432 potently inhibits MV4-11 cell growth with GI50 of 8 nM, is more effective than JQ1 at reducing levels of MYC protein in NB cell lines, upregulated p21& GADD45H and downregulated CCND2 & ODC1, C-MYC target genes.SJ432 (15 mg/kg, i.p.) significantluy reduced tumor volumes in pediatric NB xenograft SK-N-AS, with essentially no loss in body weight.

ALS-I, an acid-Liable surfactant, is adopted for in-solution enzymatic digestions, can help to solubilize hydrophobic proteins. ALS-I is significantly enhanced peptide recovery for mass spectrometry (MS) mapping in the study of the proteomes of regenerating rat retina and mouse brain.

Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.

SSCI-2 is a highly potent, selective NaV1.7 inhibitor with IC50 of 9 and 17 nM on human and rhesus Nav1.7 channels, respectively.SSCI-2 showed robust selectivity over other human and rhesus Nav channel paralogs, with the exception of Nav1.2 channels (IC50 183 nM for hNaV1.2), shows no other channels and receptors in 114 enzymatic, radioligand binding, and cellular assays.SSCI-2 also exhibits high potency in manual patch clamp experiments (IC50=24/62 nM for huma/rhesus Nav1.7 channels).SSCI-2 inhibits withdrawal responses to noxious heat in rhesus monkeys.