UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively. 了解更多

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity. 了解更多

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α. 了解更多

Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity. 了解更多

Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 ?M. 了解更多

Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. 了解更多

Dexanabinol exhibits not only the antioxidant and neuroprotective activities in brain but also anti-inflammatory activity by inhibiting NF-κB and decreasing cytokines such as TNFα and interleukin-6, which could ensure the integrity of BBB and reduce cell apoptosis and death. 了解更多

MethADP is a specific CD73 inhibitor. 了解更多

5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively. 了解更多

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα. 了解更多

LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis. 了解更多

JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL). 了解更多

Ralfinamide (FCE-26742A) is an orally available Na+ blocker derived from α-aminoamide, with function of suppressing pain. 了解更多

Trifarotene (CD5789) is a retinoic acid receptor (RAR) agonist with Kdapp of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively. 了解更多

SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. 了解更多

RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). 了解更多

Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively. 了解更多

BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ. 了解更多

Rimacalib is a Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ. 了解更多

THS-044 binding stabilizes the HIF2α PAS-B folded state, for regulating HIF2 activity in endogenous and clinical settings. 了解更多

Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. 了解更多

WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122?±?30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells. 了解更多

STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. 了解更多

(RS)-MCPG is a non-selective group I/group II metabotropic glutamate receptor antagonist. 了解更多

D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR. 了解更多

Dexrazoxane is an intracellular iron chelator and an inhibitor of topoisomerase IIα. 了解更多

2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways. 了解更多

Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation. 了解更多

Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo. 了解更多

BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression. 了解更多

SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface. 了解更多

Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. Rosamultin has inhibitory effects against HIV-1 protease. Rosamultin has the potential for treating H2O2-induced oxidative stress injury through its antioxidant and antiapoptosis effects. 了解更多

Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2. 了解更多

Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM]. 了解更多

CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. 了解更多

L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway. 了解更多

SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression. 了解更多

BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC50 of ~10 μM. 了解更多

Tomatine is an glycoalkaloid that occurs in the extract of leaves of wild tomato plants. It has been found to inhibit the growth of various fungi and bacteria. It is used as a precipitating agent for steroids. 了解更多

Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. 了解更多

Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. 了解更多

4BP-TQS is an allosteric agonist of α7 subunit-containing neuronal nicotinic acetylcholine receptors (nAChRs). 了解更多

BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. 了解更多

Hyodeoxycholic (HDCA) acid是二级胆汁酸，是肠道细菌的代谢副产物之一。 了解更多

Tamsulosin是一种α1a-选择性α受体阻滞剂，用于对症治疗前列腺增生（BPH）。 了解更多

Deoxygalactonojirimycin Hydrochloride是一种有效且选择性的Alpha-gal A（Alpha-半乳糖苷酶）抑制剂。 了解更多

Lipoic acid是衍生自辛酸的有机硫化合物。ALA通常在动物体内制成，并且对于有氧代谢至关重要。 了解更多

BOP sodium salt是新型的双重alpha9beta1/alpha4beta1整联蛋白抑制剂。 了解更多

R-BC154是高亲和力的荧光α4β1/α9 9β1抑制剂。 了解更多