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(+)-LRH-1modulator-1 is a stereoisomer of LRH-1modulator-1. LRH-1modulator-1 (compound 6N) is a potent LRH-1 (liver receptor homolog-1) modulator/agonist. LRH-1modulator-1 has anti-inflammatory effects in intestinal organoids. LRH-1modulator-1 induces the anti-inflammatory cytokine IL-10 and reduces the inflammatory cytokines IL-1b and TNFa[1].
KAT modulator-1 (Compound 3) is a KAT modulator. KAT modulator-1 can interact with p300 full-length but not with the catalytic domain. KAT modulator-1 can be used for epigenetics research [1].
LRH-1 Inhibitor-3 is a small molecule that inhibits LRH-1 transcriptional activity, thereby decreasing the expression of target genes associated with cell growth and proliferation. LRH-1 Inhibitor-3 has shown potential in reducing cancer cell proliferation in human pancreatic, colon, and breast adenocarcinoma cell lines. LRH-1 Inhibitor-3 serves as a molecular probe for investigating the role of LRH-1 in various malignancies.
AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus [1].
MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with Kis of 0.25, 41.1, 1.30 nM, respectively[1]
Progranulin modulator-1 (Compound 60) is an orally active enhancer of progranulin (PGRN) secretion. Progranulin modulator-1 enhances the potency of BV-2 cell to increase PGRN levels, has inhibitory effect on hERG and Low cytotoxicity, the PGRN EC50 and hERG IC50 were 83 and 3100 nM, respectively [1].
Immuno modulator-1 (compound 22) inhibits TNFα and IL-2 secretion in human peripheral blood mononuclear cells (hPBMC), with IC50 values of 4.7 and 26 nM, respectively. Immuno modulator-1 shows hERG potassium channel blocking effect, with Inhibitory percentage of 20% at 3 μM [1].
GPR17 modulator-1 (Compound 2-046) is a modulator for G protein-coupled receptor 17 GPR17, with an IC50<10 nM for hGPR17 in CHO. GPR17 modulator-1 exhibits moderate pharmacokinetic characteristics in mice. GPR17 modulator-1 ix blood-brain barrier (BBB) permeable [1].
RGS10 modulator-1 (compound 15) is a potent RGS10 modulator. RGS10 modulator-1 significantly reverses IFNγ-induced RGS10 protein and mRNA expression. RGS10 modulator-1 reverse the IFNγ-induced COX-2 mRNA and iNOS expression [1].
GP130 modulator-1 (compound A33) is a gp130 signaling pathway modulator. GP130 modulator-1 can be used in the study of inflammatory and degenerative disorders [1].
THR-β modulator-1 (compound 1a) is a potent thyroid hormone receptor β modulator. THR-β modulator-1 can be used in research of thyroid hormone receptor related disorders [1].
KCC2 Modulator-1 (Example 52) is a KCC2 modulator with an EC50 value of 0.146 μM. KCC2 Modulator-1 can be used for the research of KCC2 mediated diseases [1].
CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC50 value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV [1].
MRGPRX2 modulator-1 (example 17) is a mas-related g-protein receptor x2 (MRGPRX2) modulator. MRGPRX2 modulator-1 can be used for the research of inflammation, pain and autoimmune disorders [1].
Mitochondria modulator-1 is a mitochondrial regulator that stimulates mitochondrial ATP production. Mitochondria modulator-1 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. Mitochondria modulator-1 has the potential to study mitochondrial diseases [1].
Orexin receptor modulator-1 is an orexin receptor modulator. Orexin receptor modulator-1 can be used for the research of substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension [1].
MRGPRX4 modulator-1 (compound 31-2) is a potent mas-related g-protein receptor X4 (MRGPR X4) modulator, with antagonist activity of IC50 < 100 nM for MRGPR4. MRGPRX4 modulator-1 can be used for researching MRGPR X4 dependent diseases such as itch, pain, and autoimmune disorders [1].
AHL modulator-1 (compound 12) is a modulator of N-acylated L-homoserine lactone (AHL), with the agonism and antagonism of 21% and 42% in cellulase activity and 5% and 32% in potato macerationa, respectively [1].
M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment [1].
Mutant p53 modulator-1 is a mutant p53 modulator. Mutant p53 modulator-1 reduces the progression of cancers that contain a p53 mutation (extracted from patent WO2021231474A1, compound 231B) [1].
Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. Glucocorticoid receptor/NF-κB modulator-1 suppresses the degradation of glucocorticoid receptor (GR) mRNA and GR protein, inhibits the activation of NF-κB signaling pathway. Glucocorticoid receptor/NF-κB modulator-1 downregulates levels of NO, interleukin-6 and tumor necrosis factor-alpha (TNF-α). Glucocorticoid receptor/NF-κB modulator-1 ameliorates sepsis in mouse model [1].
IL-17A modulator-1 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 9. IL-17A modulator-1 inhibits the biological action of IL-17A with a pIC50 of 8.2. IL-17A modulator-1 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders [1].
CB2R/FAAH modulator-1 is a cannabinoid type 2 receptor (CB2R) full agonist with Kis of 14.8 nM and 241.3 nM for CB2R and CB1R, respectively. CB2R/FAAH modulator-1 is a fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 4 μM. CB2R/FAAH modulator-1 decreases pro-inflammatory and increases anti-inflammatory cytokines production [1].
NR2F6 modulator-1 is a potent nuclear receptor subfamily 2, group F, member 6 (NR2F6) modulator. NR2F6 modulator-1 can be used for researching immune modulation and modulation of cancer stem cell activity [1].
M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model [1].
KRAS G12D modulator-1 (compound 6) is a potent KRAS G12D modulator with IC50 values of 1-10 μM for NEA-G12D, PPI-G12D, and p ERK-AGS, respectively. KRAS G12D modulator-1 can be used in research of cancer [1].
AMPA receptor modulator-1 is a potent, orally active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC50 of 9.7, more selective over GluA1/γ-2 (pIC50=5) [1].
P2X2/3 modulator-1 (Compound 46) is a P2X2/3 modulator. P2X2/3 modulator-1 can be used in the study of pain, central nervous system disorders and inflammation [1].
D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile [1].
Fluorogen binding modulator-1 (PubChem SID 125240934) is a fluorogen activating protein (FAP)-fluorogen binding modulator with -log EC50s of 6.61 and 6.37 for AM2.2-β2AR and AM2.2-GPR32, respectively [1].
P53/TLR2 modulator-1 (Compound Z9) is a modulator that targets both the P53 pathway and TLR2 simultaneously, exhibiting anti-radiation activity. P53/TLR2 modulator-1 reduces apoptosis by inhibiting the radiation-induced expression of P53 and Bax. At the same time, it activates the TLR2 pathway, upregulates the expression of downstream proteins MyD88 and P65, and promotes the secretion of cytokines such as IL-6, thus exerting an anti-radiation effect. P53/TLR2 modulator-1 shows significant anti-radiation activity against both AHH-1 cells and HUVECs. It can also increase the survival rate of C57BL/6J mice irradiated with a lethal dose of radiation and reduce the damage to their hematopoietic system, the villous structure of the small intestine, and the spleen caused by radiation. P53/TLR2 modulator-1 can be used in the research of radiation injury-related diseases [1].
Utrophin modulator 1 is a potent utrophin modulator (upregulates utrophin protein levels), with an EC50 of 0.11 μM. Utrophin modulator 1 can be used in study of duchenne muscular dystrophy (DMD) [1].
PKM2 modulator 1 (compound C998) is a potent PKM2 inhibitor. PKM2 modulator 1 shows antiproliferative activity. PKM2 modulator 1 induces apoptosis. PKM2 modulator 1 has the potential for the research of glioblastoma [1].
Autotaxin modulator 1 is an autotaxin (ATX) enzyme inhibitor, extracted from patent WO 2014018881 A1, Compound Example 12b. Autotaxin modulator 1 is expected to be useful for researching demyelination due to injury or disease, as well as for researching proliferative disorders such as cancer [1].
Myosin modulator 1 (Compound B141) is a modulator for myosin, that inhibits ATPase in rabbits psoas, porcine atria and in porcine ventricle, with IC25s of 0.42, 0.13 and 3.09 μM, respectively. Myosin modulator 1 regulates systolic cardiac performance in Sprague Dawley rats [1].
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM [1].
mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments [1].
CB2 modulator 1 (compound 130) is a potent CB2 modulator. CB2 modulator 1 has the potential for immunedisorders, inflammation, osteoporosis, renal ischemia [1].
HIV capsid modulator 1(compound 21a2) is a potent HIV capsid modulator. HIV capsid modulator 1 is a quinazolin-4-one-bearing phenylalanine derivative. HIV capsid modulator 1 has antiviral activities against both HIV-1 and HIV-2 [1].
ALDH2 modulator 1 is a potent and orally active aldehyde dehydrogenase-2 (ALDH2) modulator. ALDH2 modulator 1 reduces blood alcohol levels in mice [1].
GPR41 modulator 1 (compound 10ak) is a potent GPR41 modulator with an EC50 value of 0.679 µM. GPR41 modulator 1 shows agonistic modulator activity [1].
Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 has the potential for inflammatory pain treatment [1].
Pin1modulator 1 (compound IIb-219) is a modulator that specifically targets β-Catenin and inhibits the Wnt pathway. Pin1modulator 1 can be used in the study of Wnt-mediated related diseases, such as cancer [1].
PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with Ki values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC50 of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively [1].
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors [1] .
mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research [1].
PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes [1].
GPR120 modulator 1 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F1. GPR120 modulator 1 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes [1].
IL-17 modulator 1 is an orally active, highly efficacious small molecule IL-17 modulators extracted from patent WO 2020127685. IL-17 modulator 1 can be used for the research of preventing, researching or ameliorating a variety of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis [1].
Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity [1].
Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice [1].
FXR/CES2 modulator 1 (compound LE-77) is a doul modulator that activates FXR and inhibits CES2. FXR/CES2 modulator 1 effectively mitigates the intestinal toxicity of irinotecan [1].
PDK1 allosteric modulator 1 is a molecule targeting PDK1 with a binding affinity of 8 μM. PDK1 allosteric modulator 1 is able to bind to the PIF pocket of PDK1, potentially affecting the biological activity of this kinase [1].
α-Synuclein modulator 1 (Compound 7k) is a modulator for α-synuclein. α-Synuclein modulator 1 exhibits a maximal absorption and emission wavelength of 386 and 603 nm in ACN/PBS (1:1) buffer [1].
GLP-1 Receptor modulator 1 (Compound 7) is a potent GLP-1 receptor positive allosteric modulator. GLP-1 Receptor modulator 1 can be used for the research of obesity and type 2 diabetes [1].
CD33 splicing modulator 1 (Compound 1) is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid lineage cell surface receptor that is known to regulate microglia activity. CD33 splicing modulator 1 increases exon 2 skipping in cellular mRNA pools. CD33 splicing modulator 1 has the potential for the research of neurodegenerative disease including Alzheimer's disease [1].
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease [1].
IL-17 modulator 1 (disodium) is an orally active, highly efficacious IL-17 modulator extracted from patent WO 2020127685. IL-17 modulator 1 (disodium) can be used for the research of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis [1].
RIG-1modulator 1 is an anti-viral compound which can be useful for the treatment of viral infections including influenza virus, HBV, HCV and HIV extracted from patent WO 2015172099 A1.
TSPO/Carbonic Anhydrase Modulator 1 (Compound 3) is a dual modulator for mitochondrial translocator protein and Carbonic Anhydrase with a Ki of 1.340 μM for TSPO and a KA of 10.7 μM for CA VII. TSPO/Carbonic Anhydrase Modulator 1 promotes the production of neurosteroid, increases BDNF gene expression, exhibits neuroprotective efficacy [1].
COP1-ATGL modulator 1 (86) is an orally active modulator for COP1-ATGL axis. COP1-ATGL modulator 1 (86) could increase ATGL protein expression, reduce ATGL ubiquitination and COP1 autoubiquitination, and diminish lipid accumulation in hepatocytes in the nanomolar range [1].
KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 1 potentiates human KCa2.3 channels with an EC50 value of 0.19 μM and 0.99 μM on the rat KCa2.2 channel subtype [1].
CD33 splicing modulator 1 (Compound 1) hydrochloride is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid cell surface receptor known to regulate microglial activity. CD33 splicing modulator 1 hydrochloride increases exon 2 skipping in the cellular mRNA pool and can be used to study neurodegenerative diseases including Alzheimer's disease [1].
GluN2A Allosteric modulator 1 (Compound 11) is an orally active, BBB-penatrable and highly selective GluN2A negative allosteric modulator. GluN2A Allosteric modulator 1 has IC50 values of 0.042 μM and 13 μM for GluN2A and GluN2B, respectively. GluN2A Allosteric modulator 1 can be used for the research of nervous system diseases [1].
IGF-1R modulator 1 (Example 5) is an IGF-1R modulator, with EC50s of 0.29 μM (FGFR1), 0.25 μM (IGF1R), 0.34 μM (TrkA), 0.39 μM (TrkB). IGF-1R modulator 1 can be used for research of diseases characterised by impaired signalling of neurotrophins and/or other trophic factors, such as Alzheimer's disease [1].
CB1R/AMPK modulator 1 (Compound 38-S) is an orally active CB1R/AMPK modulator, with an Ki of 0.81 nM and an IC50 of 3.9 nM for CB1R. CB1R/AMPK modulator 1 activates AMPK. CB1R/AMPK modulator 1 reduces food intake and body weight, and improves glucose tolerance and insulin sensitivity [1].
DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 μM. DPP-4/GPR119 modulator 1 can be used for diabetes research [1][1]. DPP-4/GPR119 modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
FXR/HSD17B13 modulator 1 (compound 6) is a potent modulator of FXR/HSD17B13. FXR/HSD17B13 modulator 1 plays an important roel in metabolic dysfunction-associated steatohepatitis (MASH) research [1].
hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research [1].
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.
5-HT6R/MAO-B modulator 1 (compound 48) is an antagonist of 5-HT6R at Gs signaling and an irreversible MAO-B inhibitor. 5-HT6R/MAO-B modulator 1 exhibits glioprotective properties. 5-HT6R/MAO-B modulator 1 can reverse Scopolamine-induced memory deficits [1]. 5-HT6R/MAO-B modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
SS-RJW100 is a enantiomer of RJW100, which is a racemic agonist of nuclear receptor liver receptor homolog 1(LRH-1) and steroidogenic factor 1(SF-1). SS-RJW100 promotes recruitment of coregulator protein fragments in vitro, recruits the transcriptional intermediary factor 2 (Tif2) coactivator to LRH-1. SS-RJW100 diminishes LRH-1 allosteric activation networks, shows poor thermal stability [1] .
σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain [1].
α5-GABAA receptor modulator 1 (Compound A-4) is a silencing allosteric modulator (SAM) specifically targeting the a5 subunit of the GABAA receptor, suitable for research into central nervous system (CNS) disorders [1].
Anticancer agent 183 (example 48) is a non-agonistic PPARG modulator. Anticancer agent 183 has a high affinity to PPARG (PPARγ). Anticancer agent 183 inhibits kinase-mediated phosphorylation of PPARG. Anticancer agent 183 can used for research on metabolic diseases to avoid side effects [1].
Nrf2-ARE/hMAO-B/QR2 modulator 1 is a Resveratrol-based multitarget-directed ligands with IC50s of 8.05, 9.83 and 0.57 μM for hMAO-B, NRF2 and QR2. Nrf2-ARE/hMAO-B/QR2 modulator 1 has neuroprotection, decreasing ROS production in okadaic acid-treated mice hippocampal slices [1].
RR-RJW100, the enantiomer of RJW100, is an nuclear receptor liver receptor homolog 1(LRH-1) and steroidogenic factor 1(SF-1) agonist. RJW100 can be synthesized as two enantiomers, RR-RJW100 and SS-RJW100, with RR-RJW100 shown to be the more potent LRH-1 agonist. RR-RJW100 is involved in the regulation of metabolic homeostasis and is used in studies of diabetes, liver disease and inflammatory bowel disease [1] .
Iso-RJW100 (compound 24-endo) is a dual-liver receptor homologue-1(LRH-1) and steroidogenic factor-1(SF-1) agonist with pEC50 of 6.4 and 7.2, respectively [1].
ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 μM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 μM). ML-180 has the potential for LRH-1-dependent cancers [1] .
ML179 (SR-1309) is a inverse LRH1/NR5A2 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer [1].
RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC50s of 6.6 and 7.5, respectively [1]. RJW100 also causes strong activation of the miR-200c (miRNA-200c, microRNA-200c) promoter .
1,2-DLPC (1,2-Dilauroyl-sn-glycero-3-phosphocholine) is a ligand for LRH-1 agonists. 1,2-DLPC is a phospholipid used in the synthesis of liposomes. 1,2-DLPC enhances fat breakdown and apoptosis in fat cells through a TNFα-dependent pathway, while also inhibiting palmitate-induced insulin resistance through PPARα-mediated inflammation in muscle cells [1] .
Hsp110/sGC-modulator-1 (compound 17i), an orally active Hsp110/sGC dual-target regulator, exhibits optimal Hsp110 and sGC molecular activities as well as remarkable cell malignant phenotypes inhibitory and vasodilatory effects. Hsp110/sGC-modulator-1 (compound 17i) attenuates pulmonary vascular remodeling and right ventricular hypertrophy via Hsp110 suppression [1].
HS-291 is a HtpG inhibitor of Borrelia burgdorferi (Bb). HS-291 contains BX-2819 (high affinity for Bb HtpG), PEG linker, and Verteporfin (HY-B0146) (a photoactive toxin).HS-291 produces reactive oxygen species under light activation to oxidize HtpG and a discrete protein subset near chaperone proteins and can quickly and irreversibly inactivate Bb [1].
(R)-IL-17 modulator 4 is the R-configure of IL-17 modulator 4 (HY-141692). IL-17 modulator 4 is a proagent of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator .
NLRP3 modulators 1 is the potent modulator of NLRP3. NLRP3 modulators 1 agonizes or partially agonizes NLRP3 that are useful for researching a condition, disease or disorder in which a decrease in LRP3 activity contributes to the pathology (extracted from patent WO2017184746A1, compound 107) [1].
IL-17 modulator 4 is a proagent of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator. IL-17 modulator 4 is promising for the research of IL-17A mediated diseases, including inflammation, autoimmune diseases, infectious diseases, cancer, and precancerous syndrome [1] .
S-Adenosylhomocysteine sulfoxide is an inhibitor of catechol-O-methyltransferase (COMT) with an IC50 value of 860 μM. S-Adenosylhomocysteine sulfoxide can be used in the research of methylation reaction modulators .
Phthalide is a chemical scaffold. Phthalide can be used to synthesize a variety of phthalide derivatives including anti-inflammatory agent, antimicrobial, antioxidant and blood-tumor barrier modulators .
NBD-FTY720 phenoxy hydrochloride is a fluorescently-labeled analog of FTY720. FTY720 (HY-12005) is a potent sphingosine 1-phosphate (S1P) receptors modulator .
PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC50 of 1.5 μM) negative allosteric modulator and mGluR3 (EC50 of 8.9 μM) positive allosteric modulator .
p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. p-fin4 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p-fin4 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene expression. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al [1].
p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .
1,2-DLPC (1,2-Dilauroyl-sn-glycero-3-phosphocholine) is a ligand for LRH-1 agonists. 1,2-DLPC is a phospholipid used in the synthesis of liposomes. 1,2-DLPC enhances fat breakdown and apoptosis in fat cells through a TNFα-dependent pathway, while also inhibiting palmitate-induced insulin resistance through PPARα-mediated inflammation in muscle cells [1] .
p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. p-fin4 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p-fin4 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
Phthalide is a chemical scaffold. Phthalide can be used to synthesize a variety of phthalide derivatives including anti-inflammatory agent, antimicrobial, antioxidant and blood-tumor barrier modulators .
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .
PFDN5 protein selectively binds to cytosolic chaperonin (c-CPN), facilitating targeted protein transfer and promoting nascent polypeptide folding. Beyond its chaperone function, PFDN5 regulates MYC transcriptional activity by forming a heterohexamer. It interacts with MYC's N-terminal domain, showcasing a multifaceted role in cellular processes, bridging protein folding and transcriptional regulation. PFDN5 Protein, Human (His) is the recombinant human-derived PFDN5 protein, expressed by E. coli , with N-His labeled tag.
NS3 protease Protein is a zinc-dependent serine protease.NS3 needs to bind to the viral protein NS4A to enable additional conformation changes that enhance activity and appropriate intracellular localization.NS3 protein induces Caspase-8-mediated apoptosis independently of its protease or helicase activity.NS3 protease Protein, HCV (GST) is the recombinant Virus-derived NS3 protease protein, expressed by E.coli , with N-GST labeled tag.
The VSTM2A protein is a key player in early white and brown preadipocyte differentiation and actively promotes adipogenesis by upregulating the transcription factor PPARG. This regulation operates in BMP4-dependent signaling pathways, highlighting the complex molecular mechanisms involved in differentiation. VSTM2A Protein, Human ( E84K, HEK293, His) is the recombinant human-derived VSTM2A protein, expressed by HEK293 , with C-6*His labeled tag and E84K mutation.
The hemagglutinin HA1 protein is essential for attachment of virions to host cells by binding to sialic acid-containing receptors, inducing virion internalization via clathrin-dependent or clathrin- and caveolin-independent pathways. As a class I viral fusion protein, HA1 determines host range restriction and virulence, mediating fusion between the virion membrane and the endosomal membrane. HA/Hemagglutinin Protein, H3N2 ( EPI189220, sf9, His) is the recombinant Virus-derived HA/Hemagglutinin protein, expressed by Sf9 insect cells , with C-His labeled tag.
ORAI1 Antibody (YA3157) is a non-conjugated IgG antibody, targeting ORAI1, with a predicted molecular weight of 33 kDa. ORAI1 Antibody (YA3157) can be used for WB experiment in human background.
NR5A2 Antibody (YA2472) is a non-conjugated IgG antibody, targeting NR5A2, with a predicted molecular weight of 61 kDa (observed band size: 65 kDa). NR5A2 Antibody (YA2472) can be used for WB experiment in human, mouse, rat background.
5-HT6R/MAO-B modulator 1 (compound 48) is an antagonist of 5-HT6R at Gs signaling and an irreversible MAO-B inhibitor. 5-HT6R/MAO-B modulator 1 exhibits glioprotective properties. 5-HT6R/MAO-B modulator 1 can reverse Scopolamine-induced memory deficits [1]. 5-HT6R/MAO-B modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
1,2-DLPC (1,2-Dilauroyl-sn-glycero-3-phosphocholine) is a ligand for LRH-1 agonists. 1,2-DLPC is a phospholipid used in the synthesis of liposomes. 1,2-DLPC enhances fat breakdown and apoptosis in fat cells through a TNFα-dependent pathway, while also inhibiting palmitate-induced insulin resistance through PPARα-mediated inflammation in muscle cells [1] .
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