IDE1 is an inducer of definitive endoderm 1 (IDE1).
ACT-672125 is a potent CXCR3 antagonist with IC50 value of 239 nM in human blood. ACT-672125 has activity for hERG with IC50 value of 18μM. ACT-672125 can be used for the research of autoimmune diseases[1].
MPO-IN-4 (compound 12) is a potent and selective myeloperoxidase (MPO) inhibitor with an IC500 of 25 nM. MPO-IN-4 has no effect on methyl guanine methyl transferase (MGMT)[1].
Alclometasone dipropionate (Sch 22219) is a steroid compound. Alclometasone dipropionate can be used for the research of dermatitis and skin itch[1][2].
Antcin A is a potent NLRP3 inhibitor that inhibits the assembly and activation of the NLRP3 inflammasome. Antcin A can inhibit Kupffer cell pyroptosis and has liver protective activity. Antcin A can be used to study inflammation, such as non-alcoholic fatty liver disease[1].
Dimethyl fumarate D6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression[1][2][3][4][5][6].
BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM[1]. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC)[2].
Kamebakaurin is a natural compound isolated from Isodon japonicus. Kamebakaurin is a potent inhibitor of NF-κB activation by directly targeting DNA-binding activity of p50[1].
G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer[1].
MALT1-IN-11 (Example 151 in reference Patent) is a MALT1 protease inhibitor (IC50 < 10 nM). MALT1-IN-11 inhibits IL10 secretion with an IC50 of 10-100 nM. MALT1-IN-11 can be used for the research of cancer, autoimmune and inflammatory disorders[1].
2"-O-Galloylhyperin, an active compound isolated from Pyrola incarnate Fisch., possesses anti-oxidative and anti-inflammatory activities. 2"-O-Galloylhyperin has hepatoprotective effect against oxidative stress-induced liver damage[1][2].
Armillarisin A has the potential for the ulcerative colitis (UC) study. Armillarisin A increases IL-4 and lower IL-1β[1].
DOTA-biotin is a DOTA-based small molecule hapten. DOTA-biotin has low tissue and whole-body retention in mice 4 h postinjection[1].
DT-3 is a membrane-permeable protein kinase G Iα inhibitory peptide. DT-3 is a guanylyl cyclase? inhibitor and shows pharmacological blockade of the cGMP–PKG signalling[1].
Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD[1]. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication[2]. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation.
HIV-1 inhibitor-29 (compound 14d2) is a potent HIV-1 inhibitor with an EC50 of 2.18 μM for HIV-1 IIIB. HIV-1 inhibitor-29 has high anti-resistance profile toward F227L/V106A strain (EC50 = 0.974 μM), and exhibits low cytotoxicity in MT-4 cells (CC50 = 211 μM). HIV-1 inhibitor-29 can be used for researching AIDS[1].
Glucocorticoid receptor agonist-1-Gly-Gly-Glu-Gly-Br is a steroid-Linker conjugate used for the synthesis of immunoconjugates linked to proteins[1].
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research[1][2].
Emoxypine succinate is an antioxidant. Emoxypine succinate can be used for the research of post-traumatic[1].
Gingerenone A is a Nrf2-Gpx4 activator with anti-breast-cancer properties. Gingerenone A results a delayed G2/M in cancer cells, following oxidative stress and senescence responses. Gingerenone A also alleviates ferroptosis in secondary liver injury (SLI) in dextran sodium sulfate (DSS)-induced colitis mice. Gingerenone A can be isolated from Zingiber officinale[1][2].
(+)-(3R,8S)-Falcarindiol is a polyacetylene found in carrots, has antimycobacterial activity, with an IC50 of 6 μM and MIC of 24 μM against Mycobacterium tuberculosis H37Ra[1][2]. Antineoplastic and anti-inflammatory activity[2].
ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2.
RIPK3-IN-1 is a RIPK3 type II DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 inhibits RIPK1 and RIPK2 with IC50s of 5.5 and >10 μM. RIPK3-IN-1 is also a c-Met kinase inhibitor with an IC50 of 1.1 μM[1].
FASN-IN-5 (example 11), a FASN inhibitor, can be used for the research of TH17- or CSF1 -mediated disease or disorder such as cancer, immunological disorders, and obesity[1].
Uralsaponin D is a saponin that can be isolated from Glycyrrhiza inflata. Uralsaponin D inhibits phospholipase A2 (PLA2) with an IC50 value of 32.2 μM[1].
Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19[1][2][3][4].
Chamazulene, a natural compound, is an antioxidant-type inhibitor of leukotriene B4 formation[1].
GX-201 is a selective NaV1.7 inhibitor, with an IC50 of <3.2 nM for hNaV1.7[1].
AI-3 is a potent ARE (antioxidant response element) activator. AI-3 increases the NQO1 at the transcript levels and protein expression levels. AI-3 has the potential for the research of oxidative stress related diseases[1].
WS6 is a novel small molecule that promotes β cell proliferation in rodent and human primary islets with EC50 of 0.28 uM(R7T1 cell viability).EC50 value: 0.28 uM [1]Target: β cell proliferation agonistin vitro: WS6 induced up to 4% of rat β cells to proliferate, with an EC50 of 0.4 μM. In the same format, WS6 also induced 3% of human β cells to proliferate, with a similar potency to the rat β cells. WS6 induced R7T1 proliferation in dose response, with EC50 value of 0.28 μM, Proliferation of R7T1 cells, which are cultured in suspension and grow as clusters, was apparent by visible inspection. in vivo: RIP-DTA mice were fed Dox in the drinking water until the onset of overt diabetes (blood glucose reading >300 mg/dL, typically 4-10 days), at which point Dox treatment was discontinued and treatment with WS6 was initiated (5 mg/kg every other day via intraperitoneal injection). Pharmacokinetic studies with WS6 at 50 mg/kg revealed a CMAX of ～5 μM and T1/2 of ～2 h. Treatment with WS6 caused a progressive reduction of blood glucose over time, starting around 2 weeks.