Empagliflozin (BI-10773)
CAS 864070-44-0
Empagliflozin is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2..
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SRT1720
CAS 925434-55-5
SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities agaiinst SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.
Anacetrapib(MK0859)
CAS 875446-37-0
Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.
Lonidamine
CAS 50264-69-2
Lonidamine is an orally administered small molecule hexokinase inactivator.Target: OthersLonidamine is a derivative of indazole-3-carboxylic acid, which for a long time, has been known to inhibit aerobic glycolysis in cancer cells. It seems to enhance aerobic…
SIRT2 Inhibitor II, AK-1
CAS 330461-64-8
AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor.
Desogestrel
CAS 54024-22-5
Desogestrel(Org-2969) is a third-generation 19-nortestosterone derivative progestogen; is contained in many oral contraceptive preparations, both combined (COCs) to ethinyl-estradiol (EE) or alone in a progestin-only pill (POP).
Glutaminase Inhibitor II, BPTES
CAS 314045-39-1
BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM.
TUG-770
CAS 1402601-82-4
TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.
Ozanimod (RPC1063)
CAS 1306760-87-1
Ozanimod is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410±160 pM and 11±4.3 nM in [35S]-GTPγS binding, respectively.
CH-223191
CAS 301326-22-7
CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 blocks the binding of TCDD to AhR with an IC50 of 0.03 µM.
BVT 2733(BVT.2733)
CAS 376640-41-4
BVT 2733 is a new, small molecule, non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
TUG891
CAS 1374516-07-0
TUG-891 is a potent and selective agonist of the long chain free fatty acid (LCFA) receptor 4.
3-TYP
CAS 120241-79-4
3-TYP is a selective SIRT3 inhibitor, with an IC50 of 16 nM, more potent over SIRT1 (IC50=88 nM), SIRT2 (IC50=92 nM).
Aldose reductase-IN-1
CAS 1355612-71-3
An inhibitor of aldose reductase with IC50 of 28.9 pM; extracted from Patent WO2014113380 A1 and US20130225592.
AGK2
CAS 304896-28-4
AGK2 is a selective SIRT2 inhibitor with IC50 of 3.5 μM. AGK2 can also inhibit SIRT1 and SIRT3 with IC50 of 30 and 91 μM, respectively.
LTI-291
CAS 1919820-28-2
LTI-291 is an activator of glucocerebrosidase (Gcase) extracted from patent WO 2017192841 A1.
GNE-617
CAS 1362154-70-8
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
Epiandrosterone
CAS 481-29-8
Epiandrosterone is a steroid hormone with weak androgenic activity. Epiandrosterone is naturally produced by the enzyme 5α-reductase from the adrenal hormone DHEA.
BMS-986020
CAS 1257213-50-5
BMS-986020 is an LPA1 antagonist.target: LPA1BMS-986020 is in Phase 2 clinical development for treating idiopathic pulmonary fibrosis. BMS-986020 selectively inhibits the LPA receptor, which is involved in binding of the signaling molecule lysophosphatidic…
CYM5442
CAS 1094042-01-9
CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442…
AG-120 (Ivosidenib)
CAS 1448347-49-6
Ivosidenib (AG-120) is a mutant isocitrate dehydrogenase 1 (IDH1) inhibitor with an IC50 of 12 nM for mouse IDH1R132H.
Etrasimod(APD334)
CAS 1206123-37-6
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
R(+)-Etomoxir free acid
CAS 124083-20-1
Etomoxir ((R)-(+)-Etomoxir) is a potent inhibitor of carnitine palmitoyltransferase-I (CPT-1).
SBC-110736
CAS 1629166-02-4
SBC-110736 is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor extracted from patent WO2014150395A1, Figure 1.
7ACC2
CAS 1472624-85-3
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.IC50 value: 11 nM ([14C]-lactate influx) [1]Target: MCT inhibitor; lactate transport…
AMG-837
CAS 865231-46-5
AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to…
Cobicistat (GS-9350)
CAS 1004316-88-4
Cobicistat is a potent, and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50 of 30-285 nM.
AL 082D06(D-06)
CAS 256925-03-8
AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.
Selonsertib（GS-4997）
CAS 1448428-04-3
Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3±0.07.
SCD1 inhibitor
CAS 1231243-91-6
A novel stearoyl-CoA desaturase1 (SCD1) inhibitor.The compound exhibited robust in vivo activity with dose-dependent desaturation index lowering effects. For the detailed information of SCD1 inhibitor, the solubility of SCD1 inhibitor in water, the solubility…
Substance P free acid
CAS 71977-09-8
Substance P, Free Acid is a native substance P analog, but shows no biological activity of substance P.
AICAR (Acadesine)
CAS 2627-69-2
AICAR is a cell-permeable AMP-activated protein kinase (AMPK) activator.
Darapladib
CAS 356057-34-6
Darapladib is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with IC50 of 0.25 nM.
Bazedoxifene
CAS 198481-32-2
Bazedoxifene is a selective estrogen receptor modulator (SERM) currently in development for osteoporosis prevention and treatment.modulatorPreclinical and clinical studies with bazedoxifene demonstrate more tissue selectivity than other SERMs. In particular,…
GW0742
CAS 317318-84-6
GW0742 is a high affinity PPAR β/δ agonist with an IC50 of 1 nM for human PPARδ, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.
Cinacalcet (AMG-073) HCl
CAS 364782-34-3
Cinacalcet hydrochloride is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Coenzyme Q9
CAS 303-97-9
Coenzyme Q9, a nine isoprenyl group-containing member of the ubiquinone family, is a normal constituent of human plasma.
AZ-33(AZ33)
CAS 1370290-34-8
AZ-33 is a selective lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 0.5 μM and a Kd of 0.093 μM[1].
EPI-001
CAS 227947-06-0
EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of 6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 exhibits anti-tumor activity in vitro and in…
Dichlorphenamide (Diclofenamide)
CAS 120-97-8
Dichlorphenamide(Diclofenamide) is a carbonic anhydrase inhibitor that is used in the treatment of glaucoma.Dichlorphenamide is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class. This drug has the same side-effects as…
Liraglutide
CAS 204656-20-2
Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used clinically to treat type 2 diabetes mellitus.
LSN3154567(Nampt-IN-1)
CAS 1698878-14-6
Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
EX-527(Selisistat)
CAS 49843-98-3
Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC50 of 98 nM.
3PO
CAS 18550-98-6
3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) IC50 valueTarget: PFKFB3 isozyme
PF-3274167（cligosiban）
CAS 900510-03-4
Cligosiban (PF-3274167) is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM.
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