| DC72799 |
DA 3003-2 |
DA 3003-2 is a potent and selectively Cdc25 inhibitor. DA 3003-2 shows antiproliferative activity. DA 3003-2 induces cell cycle arrest at the G2/M phase and increases the expression of P-tyr15 Cdc2. DA 3003-2 has the potential for the research of prostate cancer. |
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| DC72800 |
PESTAHIVIN
Featured
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PESTAHIVIN is a cell adhesion molecule inhibitor. HUN-7293 selectively inhibits the expression of three cell adhesion molecules (VCAM-1, ICAM-1 and E-selectin) (IC50=1-24 nM). HUN-7293 can be used in the study of inflammatory and autoimmune diseases characterized by overexpression of cell adhesion molecules. |
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| DC72801 |
CAM741 |
CAM741 is a selective VCAM-1 translocation inhibitor. CAM741 selectively inhibits VCAM-1 expression by inhibiting its co-translational translocation within the lumen of the endoplasmic reticulum (ER). CAM741 can be used as a molecular tool and can also be used in the research of chronic inflammation and cancer. |
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| DC72839 |
Culmerciclib maleate |
Culmerciclib maleate is a cyclin dependent kinase (CDK) inhibitor, and has antineoplastic activity. |
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| DC72865 |
Hi 76-0079 |
Hi 76-0079 (NNC0076-0079) is a specfic, small molecule inhibitor of hormone-sensitive lipase (HSL) with IC50 of 0.11 uM.
Hi 76-0079 does not affect ATGL or other lipases (IC50>50 uM).
Hi 76-0079 inhibits lipolysis in vivo. |
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| DC72871 |
FHP01 |
FHP01 (BA103) is a potent, small molecule inhibitor of DDX3X helicase activity with IC50 of 0.3 uM in in vitro enzyme assays, exhibits very effective antiproliferative and killing activity against different breast cancer cell types (IC50=3.058 and 3.21 μM in MDA MB 468 and MDA MB 231, respectively).
FHP01 does not inhibit the ATPase activity of DDX3X and the helicase activity of DDX1 (IC50>100 uM).
FHP01 also inhibited WNT signaling, a key tumorigenic pathway already correlated to DDX3X functions in breast cancer model cell lines.
FHP01 inhibits ER+/PR+ (IC50 = 12.43 and 10.62 μM in MCF7 and T47D cells, respectively) and HER2+ (IC50 = 13.46 μM in SKBR3) cells, but lower in control MCF10A cells (IC50 = 28.71 μM).
FHP01 (45 mg/kg, i.p. injection) suppresses rowth of MDA MB 231 tumor xenografts in nude mice. |
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| DC72874 |
IMU-838 |
Vidofludimus (IMU-838) is a selective and potent second-generation dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 160 nM, shows anti-SARS-CoV-2 activity with EC50 of 7.6 uM in Vero cells.
Vidofludimus inhibits T cell proliferation with EC50 of 11.8 uM, with a similar effect on CpG ODN 2006-PTO dependent B cell proliferation.
Vidofludimus is specific for human DHODH and does not have off-target effect on kinases, is about 7.5-fold and about 64.4-fold more active on human DHODH as compared to rat DHODH and mouse DHODH, respectively.
Vidofludimus inhibits specifically IL–17F, IL–17A and IFN-g expression in PBMCs.
Vidofludimus is 2.6 times more potent in inhibiting DHO oxidation by human DHODH compared to teriflunomide (IC50=420 nM).
Vidofludimus shows inhibition of rat EAE motor signs in a rat experimental autoimmune encephalomyelitis (EAE) model.
Vidofludimus exerts a broad-spectrum activity against a selection of major human pathogenic viruses. |
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| DC72876 |
BDM44768 |
BDM44768 (BDM 44768) is a potent, selective catalytic site inhibitor of insulin-degrading enzyme (IDE) with IC50 of 60 nM (hIDE).
BDM44768 displays excellent selectivity over a panel of metalloproteases (>45-fold selectivity over hNEP and hECE, no significant acitivity against hACE and hMMP-1).
BDM44768 significantly increased concentrations of Aβ1-40 in culture supernatants of human SY5Y neuroblastoma cells.
Acute treatment of mice with BDM44768 (50 mg/kg, i.p.) increases insulin signalling and surprisingly impairs glucose tolerance in an IDE-dependent manner in C57BL/6J mice. |
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| DC72893 |
TP-1454
Featured
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TP-1454 is an activator of PKM2 with AC50 of 10 Nm in biochemical assays.TP-1454 modulates tumor-immune responses by destabilizing T-regulatory cells. |
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| DC72906 |
BCPA
Featured
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BCPA is a Pin1 regulator without cytotoxicity. BCPA attenuates the reduction of Pin1 protein to inhibit receptor activator of RANKL-induced osteoclastogenesis. BCPA regulates osteoclast activation, used to osteoporosis research. |
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| DC73879 |
(3S) ALG-05 |
(3S) ALG-05 is a potent pan-inhibitor of gut microbia tryptophan-indole-lyases (TILs, E.C. 4.1.99.1), exhibits inhibitory activity across TILs with Ki of 7-11 uM. |
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| DC73880 |
(R)-HTS-3 |
(R)-HTS-3 is a small-molecule inhibitor of LPCAT3, an integral membrane acyltransferase in the Lands cycle responsible for generating C20:4 phospholipids. |
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| DC73881 |
(R)-SKBG-1
Featured
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(R)-SKBG-1 is a covalent small molecule ligand of RNA-binding protein NONO, engages NONO Cys145 and suppress an array of cancer-relevant genes and impair cancer cell proliferation. |
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| DC73882 |
(S)-CKi-1
Featured
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(S)-CKi-1 is a selective, covalent inhibitor of creatine kinases (CKs), inhibits recombinant creatine kinase B (CKB) phosphotransfer activity with IC50 of 0.6 uM, depletes creatine phosphagen energetics in cells. |
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| DC73883 |
(S)-IBD3540 |
(S)-IBD3540 is a potent, gut-restricted and orally active small molecule glutamate carboxypeptidase II (GCPII) inhibitor with IC50 of 4 nM, demonstrates anti-colitis activity in both acute and chronic mouse colitis models. |
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| DC73884 |
2,5-pyridinedicarboxylic acid |
2,5-pyridinedicarboxylic acid is a highly selective D-dopachrome tautomerase (D-DT, MIF2) inhibitor with Ki of 17.2 uM, 79-fold selectivity over MIF, effectively blocks the D-DT-induced activation of CD74. |
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| DC73885 |
2-TCPA |
2-TCPA is a potent, specific inhibitor of carbamoyl-phosphate synthetase, aspartate transcarbamoylase, and dihydroorotase (CAD), suppresses SARS-CoV-2 replication in Caco-2 cells with IC50 of 2.36 uM. |
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| DC73886 |
3-mercaptopicolinic acid hydrochloride |
SKF-34288 (3-Mercaptopicolinic acid) hydrochloride is an orally active phosphoenolpyruvate carboxykinase (PEPCK, PCK) inhibitor with Ki of 2-9 uM, an inhibitor of gluconeogenesis. |
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| DC73887 |
4BPPNit |
4BPPNit is a small molecule significantly augmented glycosylation of α-dystroglycan, in part through upregulation of LARGE1 glycosyltransferase gene expression. |
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| DC73888 |
4-Sulfocalix[6]arene hydrate |
4-Sulfonic calix[6]arene is a potent AIM2 inflammasome inhibitor that work by binding competitively to the DNA binding site, dose dependently inhibits AIM2-dependent cell death and IL-1β release. |
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| DC73889 |
4-Sulfocalix[8]arene hydrate |
4-Sulfonic calix[8]arene is a potent AIM2 inflammasome inhibitor that work by binding competitively to the DNA binding site, dose dependently inhibits AIM2-dependent cell death and IL-1β release. |
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| DC73890 |
5M-8OH-Q
Featured
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5M-8OH-Q is a specific small molecule inhibitor of UDP-glucose glycoprotein glucosyltransferase (UGGT), binds a CtUGGTGT24 “WY” conserved surface motif conserved across UGGTs (Kd=47 uM) but not present in other GT24 family glycosyltransferases. |
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| DC73891 |
7-Fluorotryptamine |
7-fluorotryptamine (7FTA) is a potent synthetic agonist of GPRC5A with EC50 of 7.2 uM for inducing GPRC5A-mediated β-arrestin recruitment. |
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| DC73892 |
7-Fluorotryptamine hydrochloride |
7-fluorotryptamine (7FTA) is a potent synthetic agonist of GPRC5A with EC50 of 7.2 uM for inducing GPRC5A-mediated β-arrestin recruitment. |
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| DC73893 |
AD-5584 |
AD-5584 is a potent, brain permeable human Acetyl-CoA synthetase 2 (ACSS2) inhibitor, a key metabolic enzyme involved in regulating fatty acid synthesis and protein acetylation in tumor cells. |
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| DC73894 |
AD-8007 |
AD-8007 is a potent, brain permeable human Acetyl-CoA synthetase 2 (ACSS2) inhibitor, a key metabolic enzyme involved in regulating fatty acid synthesis and protein acetylation in tumor cells. |
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| DC73895 |
AE 51310 |
AE 51310 is a small-molecule inhibitor of Opsin 4/melanopsin (OPN4), has antitumor potential in patient-derived xenograft (PDX) tumors in mice.. |
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| DC73897 |
AGF347 |
AGF347 (AGF-347) is a small molecule inhibitor targeting mitochondrial C1 metabolism at SHMT2 (in vitro Ki=2.19 uM), also directly targers the purine biosynthetic enzymes GARFTase (Ki=3.13 uM) and AICARFTase (Ki=3.72 uM), and SHMT1 (Ki=2.91 uM). |
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| DC73898 |
AGI-25696
Featured
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AGI-25696 (AGI 25696) is a potent and selective inhibitor of methionine adenosyltransferase MAT2A, blocks the growth of MTAP-deleted tumors in vivo. |
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| DC73899 |
AK-3280 |
AK-3280 (AK 3280, GDC 3280, RG 6069) is an orally available, potential novel anti-fibrotic small molecule under investigation for the treatment of interstitial lung diseases. |
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