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BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe [1].
(±)-Pantothenic acid ((±)-Pantothenate), a B-vitamin, is an essential vitamin required for the biosynthesis of coenzyme A (CoA) in mammalian cells. Pantothenic acid has protective activity against valproic acid (VPA)-induced neural tube defects (NTD) in CD-1mice[1].
Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1mice[1].
Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1mice[1] .
Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1mice[1] .
YPLP is a yeast-derived peptide Tyr-Pro-Leu-Pro, which exhibits activity in anti fatigue mechanisms through the nuclear factor erythroid-2-related factor 2 (Nrf2)- and AMP-activated protein kinase (AMPK) pathway. YPLP is orally active [1].
RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression [1].
CD1A Human Pre-designed siRNA Set A contains three designed siRNAs for CD1A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
CD1B Human Pre-designed siRNA Set A contains three designed siRNAs for CD1B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
CD1C Human Pre-designed siRNA Set A contains three designed siRNAs for CD1C gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
CD1D Human Pre-designed siRNA Set A contains three designed siRNAs for CD1D gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
CD1E Human Pre-designed siRNA Set A contains three designed siRNAs for CD1E gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity [1].
5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment [1].
Pharmacokinetic Analysis ICR Male Mice[1]
Amitivir (LY 217896), a thiadiazole derivative, possesses broad antiviral activity against orthomyxo- and paramyxoviruses. Amitivir is effective against influenza A and B viruses [1] .
Clovibactin TFA is the TFA salt form of Clovibactin (HY-P10027). Clovibactin TFA is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors [1].
3,3-Dimethyl-1-butanol (DMB) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-Dimethyl-1-butanol inhibits the signaling pathway of p65 NF-κB and TGF-β1/Smad3. 3,3-Dimethyl-1-butanol has potential applications in cardiovascular disease (CVD) [1] .
Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is an orally active mycotoxin produced by Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [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.
Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis [1].
AJS1669 free acid is a potent and orally available glycogen synthase (GS) activator. AJS1669 improves glucose metabolism and reduces body fat mass in mice[1].
xStAx-VHLL is a PROTAC β-catenin degrader that manifests strong inhibition of Wnt signaling and sustains degradation of β-catenin in cancer cells and the intestinal organoids derived from wild-type and APC –/–mice. xStAx-VHLL can be used as a promising anticancer agent [1].
Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model [1].
FOXO1-IN-3 is a highly-selective and orally active FOXO1 inhibitor. FOXO1-IN-3 reduces hepatic glucose production in mice. FOXO1-IN-3 improves insulin sensitivity and glucose control in db/db mice without causing weight gain [1].
Antitumor agent-51 possesses potent and selective inhibitory for osteosarcoma cell growth and migration with IC50 of 21.9 nM in MNNG/HOS cells. Antitumor agent-51 has a considerable bioavailability and a low toxicity [1].
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) [1].
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity [1].
KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect [1].
GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes [1].
GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes [1].
IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity [1].
6bK TFA is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK TFA increases circulating insulin in high-fat-fed mice. Acute administration of 6bK TFA enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice[1].
Lysophosphatidylcholines is an orally active lysolipid and a component of oxidized low density lipoprotein (LDL). Lysophosphatidylcholines induces cell injury, the production of IL-1β and apoptosis. Lysophosphatidylcholines has a proactive effect on sepsis [1] .
As-358 (hydrochloride) has inhibitory effects against Ebola virus and Marburg virus with IC50s of 9.1 μM and 18.1 μM, as well as exhibits good in vivo safety [1].
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth [1]. PROTAC BTK Degrader-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.
Spilanthol is an orally active analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial and insecticidal compound.pilanthol can induce cAMP to inhibit negative regulation of urinary concentration mechanism. Spilanthol can be use as diuretic research [1] .
[Pro3]-GIP (Mouse) is a GIP receptor antagonist (IC50: 2.6 μM). [Pro3]-GIP (Mouse) improves glucose tolerance and insulin sensitivity in ob/ob mice. [Pro3]-GIP (Mouse) can be used for research of type 2 diabetes [1] .
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability [1].
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect [1].
Keap1-Nrf2-IN-10 (compound 15) is a potent NQO1 inducer. Keap1-Nrf2-IN-10 inhibits oxidative stress by decreasing the levels of MDA, ROS, NQO1 in the liver for gamma-irradiated mice. Keap1-Nrf2-IN-10 improves the survival of gamma-irradiated mice[1].
4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor, also acting as a relatively weak urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice[1] .
GEM144 is a potent and orally active DNA polymerase α(POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts [1].
P2X7 receptor antagonist-4 (Compound 14a) is a P2X7R antagonist. The P2X7 receptor antagonist-4 values of P2X7R IC50 in human and mouse are 64.7 and 10.1 nM, respectively. P2X7 receptor antagonist-4 can inhibit the activation of NLRP3 inflammasome, thereby inhibiting the expression of caspase-1, gasdermin D, IL-1β and IL-18 in the damaged kidney of sepsis mice[1].
BET-IN-21 (compound 16) is a blood-brain barrier-permeable extra terminal domain (BET) inhibitor with the Ki of 230 nM. BET-IN-21 inhibits microglia activation and has ameliorative effects on experimental autoimmune encephalomyelitis mice[1].
HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease [1].
mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice[1].
Glp-Amyloid-β (3-40) Peptide (human) (AβpE3-40) is a minor amounts of pyroglutamate-modified Aβ isolated from from 24-month-old Amyloid precursor protein (APP) transgenic Mice[1].
VU6001966 (compound 15m) is a potent and cross the blood-brain barrier mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator with IC50s of 78 nM and >30 µM for mGlu2 and mGlu3, respectively. VU6001966 can serve as an mGlu2 PET tracer [1].
PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature [1].
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice[1].
VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice[1]. VU0360172 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Yhhu6669 is an anti-HBV agent. Yhhu6669 inhibits HBV DNA. Yhhu6669 inhibits HBV replication by inducing the formation of DNA-free capsids. Yhhu6669 decreases HBV DNA and HBcAg in AAV/HBV-infected mice. Yhhu6669 has favorable PK properties [1].
SP4e is an activator of PPAR-γ, with the EC50 of 739 nM in HK-2 cells. SP4e reduces the blood glucose levels and lipid peroxidation, and increases glutathione levels and catalase activityin the Swiss albino mice[1].
SP4f is an activator ofPPAR-γ, with the EC50 of 826 nM in HK-2 cells. SP4f reduces the blood glucose levels and lipid peroxidation, and increases glutathione levels and catalase activityin the Swiss albino mice[1].
J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases [1].
URB447 is a peripherally restricted CB1 cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB1-dependent responses. URB447 can be used for research of obesity [1].
BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research [1].
Antitubercular agent-20 (Compound 2d) is an orally active antitubercular agent. Antitubercular agent-20 shows excellent activity against MTB H37Rv and MDR-MTB strains (MIC: ＜0.016 µg/ml). Antitubercular agent-20 has low cytotoxicity and good tolerance in BALB/c mice[1].
17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells [1]. 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
(E/Z)-E64FC26 is a mixture complex of E-E64FC26 and Z-E64FC26. E64FC26 (E-E64FC26) is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC50s of 1.9, 20.9, 25.9, 16.3, and 25.4 μM against PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6. E64FC26 shows anti-myeloma activity [1] .
E64FC26 is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC50s of 1.9, 20.9, 25.9, 16.3, and 25.4 μM against PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6, respectively. E64FC26 shows anti-myeloma activity [1].
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and miceTLR7, respectively. DSR-6434 has a strong antitumor effect [1] .
Borapetoside E can be isolated from T. crispa. Borapetoside E improves hyperglycemia, insulin resistance, hepatic steatosis, hyperlipidemia, and oxygen consumption in obese mice. Borapetoside E also inhibits SREBPs expression in the liver and adipose tissue [1].
γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active γ-secretase modulator with an IC50 of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease [1].
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia) [1].
α-Glucosidase-IN-49 (compound C23) is a potent inhibitor of α-Glucosidase, with IC50 of 0.52 μM. α-Glucosidase-IN-49 has oral bioactivity that can reduce blood glucose and improve glucose tolerance in mice[1].
PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min [1].
PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min [1].
TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca 2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity [1] .
Metallo-β-lactamase-IN-6 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.56 μM, 29.50 μM and 5.78 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-6 displays potent synergistic antibacterial activity with Meropenem against engineered Escherichia coli strains and intractable clinically isolated Pseudomonas aeruginosa producing VIM-2 MBL [1].
L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC50: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test [1] .
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research [1].
Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers [1].
Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice[1] .
FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD) [1].
Peginterferon beta-1a (Peginterferon β-1a) is the first pegylated interferon beta-1a molecule. Peginterferon beta-1a induces cancer cells apoptosis and shows anti-tumor activities in nude mice models. Peginterferon beta-1a can be used for the research of cancer and multiple sclerosis (RMS) [1].
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity [1].
TUG-469 is a selective free fatty acid receptor 1(FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes [1] .
SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC50=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty [1].
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice[1].
Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca 2+ channels inhibitor with an IC50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain [1].
Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/obmice[1] .
IKKβ-IN-1 is a potent and orally active IkappaB (IKK-β) inhibitor with IC50 of 0.20 μM. IKKβ-IN-1 can reduce PGE2 and TNF-α production in mouse macrophage cells. IKKβ-IN-1 has the ability to protect mice against septic shock induced mortality [1].
L-Sepiapterin (Sepiapterin) is a precursor of the endothelial nitric oxide synthase (eNOS) cofactor tetrahydrobiopterin (BH4). L-Sepiapterin improves endothelial dysfunction in small mesenteric arteries from db/db mice, and induces angiogenesis. L-Sepiapterin inhibits cell proliferation and migration of ovarian cancer cells via down-regulation of p70 S6K-dependent VEGFR-2 expression [1] .
FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>[1].
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) [1].
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/obmice[1] .
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models [1].
AMXT1501 is a novel inhibitor of the polyamine transport system. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells [1].
CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice[1].
5-Hydroxymethyl-2'-deoxyuridine is a nucleoside analog. 5-Hydroxymethyl-2'-deoxyuridine inhibits the replication of multiple human leukemia cell lines with IC50 values of 1.7-5.8 μM. 5-Hydroxymethyl-2'-deoxyuridine prolongs the survival of mice carrying L1210 leukemia. 5-Hydroxymethyl-2'-deoxyuridine can be used for the research of cell replication and leukemia [1] .
Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice[1].
S-F24 is an antifungal agent with excellent broad-spectrum. S-F24 inhibits CYP3A4 with an IC50 value of 0.4 μM. S-F24 displays a good safety profile with high selectivity, low hemolytic effects, and low tendency to induce resistance. S-F24 can be used for research on fungal infections [1].
MICAL1 Human Pre-designed siRNA Set A contains three designed siRNAs for MICAL1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
MICAL2 Human Pre-designed siRNA Set A contains three designed siRNAs for MICAL2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
MICAL3 Human Pre-designed siRNA Set A contains three designed siRNAs for MICAL3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1(MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain [1].
Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis [1] . Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC) [1].
ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity [1].
Lipid X is a novel monosaccharide precursor of Lipid A (the active moiety of gram-negative endotoxin). Lipid X is protective against endotoxin administered to mice and sheep and against life-threatening gram-negative infections in mice[1].
5-PAHSA increases insulin sensitivity, and has orally active anti-inflammatory and neuroprotective effects in mice HFD-induced diabetes mice. 5-PAHSA can be used for research of neurological dysfunction in diabetics [1] .
Phenytoin-d10 is the deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[1][2].
AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice[1].
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor) [1] .
mGAT3/4-IN-1 (compound 19b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.31 and 5.24, respectively. mGAT3/4-IN-1 exhibits a significant tactile allodynia reduction in diabetic neuropathic mice[1].
DPPC-d9 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
DPPC-d62 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
Neuropeptide S(Rat) TFA is a potent endogenous neuropeptide S receptor (NSPR) agonist (EC50=3.2 nM). Neuropeptide S(Rat) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Rat) TFA also reduces anxiety-like behavior in mice.
DPPC-d9-1 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice[1] .
Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction [1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .
TYA-018 is an orally active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect heart function in mice. TYA-018 also enhances energetics in mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation [1].
retro-inverso TAT-Beclin 1 D-amino acid is has higher activity and resistance to proteolytic degradation in vivo compared to L-amino acids peptide. TAT-Beclin 1 can induce autophagy in peripheral tissues in adult mice as well as in the central nervous system of neonatal mice[1] .
AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells [1]. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines .
Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1] .
Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1] .
Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1] .
Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1] .
Diacylglyceride, a natural scaffolding lipid, is a hapten that binds to CD1b. Diacylglyceride can be combined with carrier proteins and used in the design of antigens [1].
Phenytoin- 15N2, 13C is the 13C and 15N labeled Phenytoin[1]. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[2][3].
GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 dihydrochloride stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 dihydrochloride also prevents the d-Fenfluramine-induced head-twitch response in mice[1] .
GBR 12935 is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 also prevents the d-Fenfluramine-induced head-twitch response in mice[1] .
Neuropeptide S(Mouse) TFA is a potent endogenous neuropeptide S receptor (NPSR) agonist (EC50=3 nM). Neuropeptide S(Mouse) TFA induces mobilization of intracellular Ca 2+. Neuropeptide S(Mouse) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Mouse) TFA also reduces anxiety-like behavior in mice.
OAB-14, is a Bexarotene (HY-14171) derivative, improves Alzheimer's disease-related pathologies and cognitive impairments by increasing β-amyloid clearance in APP/PS1mice. OAB-14 effectively ameliorates the dysfunction of the endosomal-autophagic-lysosomal pathway in APP/PS1 transgenic mice[1] .
Tetrathiomolybdate, an orally active anti-copper agent, reduces copper levels in the body. Tetrathiomolybdate has a protective effect on collagen-induced arthritis in mice. Tetrathiomolybdate also reduces blood sugar, but has no effect on mice with hereditary diabetes (db/db). Tetrathiomolybdate inhibit angiogenesis, also shows antiangiogenic effects in malignant pleural mesothelioma [1] .
Nv-CATH is an antibacterial peptide of frog origin. Nv-CATH has broad-spectrum antibacterial activity against gram-positive and gram-negative bacteria. Nv-CATH significantly protects mice from fatal infections caused by Staphylococcus aureus. Nv-CATH protects mice from bacterial infection through antimicrobial immunoregulatory duality [1].
Pulchinenoside A is a natural triterpenoid saponin that enhances synaptic plasticity in the adult mouse hippocampus and facilitates spatial memory in adult mice.
Chlorthiamid is a broad-spectrum herbicide. Chlorthiamid is an olfactory toxicant with a high in vivo covalent binding in the olfactory mucosa of mice[1].
Cytidine-5'-triphosphate- 13C,d1 (Cytidine triphosphate- 13C,d1 dilithium; 5'-CTP- 13C,d1) dilithium is deuterium and 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Oxolinic acid-d5 is the deuterium labeled Oxolinic acid. Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice[1][2][3].
Anserine-d4 is the deuterium labeled Anserine. Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1][2].
D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell. D-panthenol exhibits nephroprotective effect in AKI, promotes tissue repair and regeneration.
CAD031 is a derivative of the Alzheimer's disease (AD) targeting agent J147 (HY-13779) with neuroprotective and memory-enhancing properties. CAD031 enhances memory in mice, improves dendritic structure, and stimulates cell division in the germinal zone of the brain in aged mice. CAD031 is more active than J147 in human neural stem cell assays [1].
Acesulfame potassium is an artificial sweetener. Acesulfame potassium (long-term) affects cognitive functions, potentially via altering neuro-metabolic functions in mice[1].
Dibutyl maleate, the diester of the Maleic Acid, can be used as an intermediate of pharmaceutical synthesis. Dibutyl maleate can enhance contact sensitization to Fluorescein isothiocyanate in mice[1].
Acesulfame is an artificial sweetener. Acesulfame affects cognitive functions, potentially via altering neuro-metabolic functions in mice with long-term [1].
GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines. Not only, GSK1795091 inhibits tumor growth and increases the survival in mice model, but results in long term survival in influenza challenge model in mice[1] .
Juncusol, a phenanthrenoid found in Juncus setchuenensis, possesses anxiolytic effect. Juncusol is associated with metabolic changes in cortical serotonin/dopamine levels in Mice[1].
Tilifodiolide ((-)-Tilifodiolide) is a lactone, which can be isolated from the roots of Salvia tiliaefolia. Tilifodiolide has anti-inflammatory activity in mice model [1].
Phenylquinone (2-Phenylbenzoquinone) causes pain and induces writhing in mice, and is often used in experiments to test the effectiveness of analgesics or anesthetics [1] .
NOSO-502 is an inhibitor of bacterial translation. NOSO-502 exhibits inhibitory activity against Enterobacteriaceae. NOSO-502 has good safety and antibacterial properties [1].
NSC-370284 is a selective inhibitor of ten-eleven translocation 1(TET1) and 5-hydroxymethylcytosine (5hmC). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5 [1].
CHI3L1-IN-1 (Compound 30) is an inhibitor for Chitinase-3-like protein 1(CHI3L1) (YKL-40) with IC50 of 50 nM. CHI3L1-IN-1 inhibits hERG channel with an IC50 of 2.3 μM [1].
Mahanimbine is an orally active alkaloid from Murraya koenigii. Mahanimbine inhibits progression of high-fat diet (HFD)-induced metabolic complications in mice[1].
Pildralazine (Propyldazine) is a hydralazinelike antihypertensive vasodilator containing a free hydrazine group. Pildralazine is orally active, has no significant carcinogenicity in mice model [1] .
Preclamol is a dopamine (DA) agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. Preclamol inhibits the locomotor activity of mice and rats in low doses [1].
Pentadecanoyl ethanolamide is derivate of endougenous lipid amides, the N-acylethanolamines. Pentadecanoyl ethanolamide exhibits anticonvulsant efficacy in electroshocked mice without significant toxicity [1].
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
Citric acid- 13C3 is the 13C labeled Citric acid[1]. Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[2][3][4].
Pabinafusp alfa (JR-141) is a transferrin receptor-targeting antibody consisting of Iduronate 2-sulfatase (HY-P76399) and an anti-human transferrin receptor antibody. Pabinafusp alfa is blood-brain permeable and prevents heparan sulfate (HS) deposition in the central nervous system of mucopolysaccharidosis II (MPS II) mice. Pabinafusp alfa improves learning and prevents central nervous system neuronal damage in mice[1].
9,10-Dihydroxystearic acid is an oxidation product of oleic acid. 9,10-Dihydroxystearic acid can improve glucose tolerance and insulin sensitivity in KKAy mice[1].
SCH 32615 is an enkephalinase (the enzymes responsible for the degradation of endogenous enkephalins) inhibitor. SCH 32615 can enhance surgery- and pregnancy-induced analgesia in mice[1] .
SIK1 activator 1 exhibited remarkable inhibitory activity on hepatic gluconeogenesis by enhancing the SIK1 phosphorylation and ameliorated the hyperglyceamia of type 2 diabetic mice.
Microcystin-RR (Cyanoviridin RR) is a potent and orally active protein phosphatase inhibitor. Microcystin-RR induces Apoptosis and ER stress in mice liver [1] .
Alistin (Carcinine; β-Alanylhistamine) is a selective histamine H3 antagonist with antioxidant activity and neuroprotective effects on the retina of oxidatively stressed mice[1] .
Phenazoviridin is a free radical scavenger. Phenazoviridin shows strong inhibitory activity against lipid peroxidation in rat brain homogenate and exhibits antihypoxic activity in mice[1].
MF59 is a immunologic adjuvant. MF59 significantly influnces immunogenicity of influenza vaccines. MF59 reduces the viral load in the lungs of challenged mice[1].
RO7075573 (compound 3) is an antibiotics that targets the lipopolysaccharide (LPS) transport machine in Acinetobacter. RO7075573 protects mice from A. baumannii infections [1] .
Choline tosylate is a nucleophilic compound that inhibits phospholipase A2 and phospholipase C. Choline tosylate inhibits tumor growth in mice by inhibiting the formation of diacylglycerol (DAG) [1] .
SAK3 is a potent T-type voltage-gated Ca 2+ channels (T-VGCCs) enhancer. SAK3 enhances Cav3.1 and Cav3.3 T-type Ca 2+ channel currents. Acute SAK3 administration improves memory deficits in olfactory-bulbectomized mice[1]. SAK3 inhibits amyloid β plaque formation in APP-KI mice by activating the proteasome activity .
3-Methylhistamine dihydrochloride is a degradation product of histamine. 3-Methylhistamine dihydrochloride, a methylated product of histamine, is associated with immune response and shows upregulation in the vaccinated mice[1] .
Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice[1].
Wilfortrine is a bioactive sesquiterpene alkaloid. Wilfortrine exhibits immunosuppresive effects. Wilfortrine also can inhibit leukaemia cell growth in mice and shows anti-HIV activity [1].
Anti-inflammatory agent 7 inhibits proinflammatory cytokines by blocking the NF-κB/MAPK signaling pathway in LPS-treated RAW 264.7 cells as well as mice.
SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice[1].
(R)-Preclamol is a dopamine (DA) agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. (R)-Preclamol inhibits the locomotor activity of mice and rats in low doses [1].
Feruloyl tyramine, an amide compound, can be isolated from ethanol extract of hemp seed. Feruloyl tyramine injected into the lateral ventricle caused hypothermia and dyskinesia in mice[1].
SC 34301 (Enisoprost) is a potent and orally active PGE1 analog. SC 34301 significantly reduces bacterial translocation and improves survival for burned mice[1] .
SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a Ki value of 0.9 microM. SKF 91488 dihydrochloride inhibits the methylation of labeled histamine in mice[1].
Sodium metatungstate (Sodium polyoxotungstate) is a NTPDase inhibitor, with Ki values of 2.58 μM, 3.26 μM, and 28.8 μM for NTPDase 1 (CD39), NTPDase 3 and NTPDase 2 respectively [1]. Sodium metatungstate has anti-inflammatory and anti-cancer effect. Sodium metatungstate inhibits ATP breakdown but also blocks central synaptic transmission [1] .
SY-640 is an Acetamide derivative and has potent hepatoprotective effect. SY-640 reduces Propionibacterium acnes and Lipopolysaccharide-induced liver injury in mice[1] .
Neoechinulin A is an isoprenyl indole alkaloid that exhibits scavenging, neurotrophic factor-like, and anti-apoptotic activities. Neoechinulin A induces memory improvements and antidepressant-like effects in mice[1] .
Xanthine oxidoreductase-IN-2 (Compound IVa) is a xanthine oxidoreductase (XOR) inhibitor with the IC50 of 7.2 nM. Xanthine oxidoreductase-IN-2 shows hypouricemic effects in mice[1].
Glycyrin is a PPAR-γ ligand of licorice. Glycyrin can decrease the blood glucose levels of genetically diabetic mice. Glycyrin also shows antibacterial activity [1] .
R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice[1].
Paynantheine-d3 is a deuterium labeled Paynantheine. Paynantheine is an alkaloid that can be isolated from Mitragyna speciosa. Paynantheine can decrease alcohol intake in mice[1] .
Speciogynine-d3 is a deuterium labeled Speciogynine. Speciogynine is an alkaloid that can be isolated from Mitragyna speciosa. Speciogynine can decrease alcohol intake in mice[1] .
Pseudoginsenoside F11 (Ginsenoside A1), a component of Panax quinquefolium (American ginseng), has been demonstrated to antagonize the learning and memory deficits induced by scopolamine, morphine and methamphetamine in mice.
KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice[1].
Cytochalasin C is a cell-permeable fungal toxin and induces the formation of nuclear rodlets. Cytochalasin C is 10 times less toxic in mice than is cytochalasin D [1] .
Uvaol, a triterpene present in olives and virgin olive oil, possesses anti-inflammatory properties and antioxidant effects. Uvaol attenuates pleuritis and eosinophilic inflammation in ovalbumin-induced allergy in mice[1].
Aurodox is an antibiotic obtained from a streptomyces variant, Aurodox can against a number of gram-positive bacteria. Aurodox shows a very low toxicity in mice and promoted poultry growth [1].
YVAD-CHO is an interleukin-1β converting enzyme (ICE, caspase 1) inhibitor that can partially delay motoneurone death in lesioned facial nerve mice[1].
Rubicordifolin is a natural product that can be isolated from Rubia cordifolia. Rubicordifolin inhibits the growth of sarcoma ascites in mice. Rubicordifolin has significant cytotoxic activity both in vitro and in vivo [1].
Digitoxose (D-(+)-Digitoxose), a natural product, specifically and competitively inhibits glucose-stimulated insulin release from islets in lean and obese mice. Digitoxose can be used in diabetes research [1].
MS438 is a potent thyrotropin receptor (TSHR) agonist with an EC50 of 53 nM. MS438 binds to the serpentine portion of the TSHR. MS438 induces T4 secretion in mice[1].
Isocampneoside I is an acylated phenethyl oligosaccharide that can be isolated from Cistanche deserticola (Orobanchaceae). Isocampneoside I inhibits D-galactose-induced cytotoxicity and protects primary hepatocytes in mice[1].
(S)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1(GLP-1R). (S)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice[1].
(S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1(GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice[1].
Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na + channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[1] .
XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.
Phenytoin sodium (5,5-Diphenylhydantoin sodium salt) is a potent Voltage-gated Na + channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[1] .
Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α [1].
Neocurdione is a hepatoprotective sesquiterpene isolated from Curcuma zedoaria rhizome. Neocurdione exerts potent effect on D-galactosamine- (D-Gain) and lipopolysaccharide- (LPS) induced acute liver injury in mice[1].
BRL 37344 sodium (BRL 37344A) is a specific β3-adrenergic receptor agonist. BRL 37344 sodium treatment significantly lowers the body weight of obese mice[1].
DL-AP7 is a competitive NMDA antagonist and an anticonvulsant. DL-AP7 blocks the NMDA-induced convulsions and impairs learning performance in a passive avoidance task in mice[1].
RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist [1]. RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice .
Astrophloxine is a fluorescent imaging probe capable of targeting antiparallel dimers. Astrophloxine can be used to detect aggregated Aβ in brain tissue and cerebrospinal fluid samples of Alzheimer's disease (AD) mice[1].
Icofungipen is an orally active antifungal agent. Icofungipen is the representative of beta amino acids, is toxic against Candida species. Icofungipen protects infected mice survival from C. albicans infection [1].
Collagen Type II Fragment is an anti-inflammatory peptide that potently inhibits collagen-induced arthritis (CIA) in mice. Collagen Type II Fragment can be used for research on inflammation and immunity [1].
BO-0742, a derivative of AHMA and N-mustard, is a potent anti-cancer agent. BO-0742 significantly suppresses the growth of xenografts of human breast and ovarian cancers in mice[1].
Tolbutamide is an orally active KATP inhibitor. Tolbutamide inhibits cell proliferation, stimulates exocytosis of glucagon and reduces fetal lethality of mice. Tolbutamide can be used in the research of diabete [1] .
L-Homocysteine thiolactone hydrochloride is an intramolecular thioester of Homocysteine. Homocysteine thiolactone hydrochloride prevents translational incorporation of homocysteine into proteins. L-Homocysteine thiolactone hydrochloride can induce elevated HHcy (hyperhomocysteinemia) in mice[1] .
Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both agent-sensitive and resistant cells of P388 leukemia in mice[1].
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice[1].
Iboxamycin is a potent antibiotic candidate bearing a fused bicyclic amino acid residue. Iboxamycin is orally bioavailable, safe and effective in researching both Gram-positive and Gram-negative bacterial infections in mice[1] .
HX531 is a potent RXR antagonist with an IC50 of 18 nM [1]. It has been shown to reduce triglyceride content in white adipose tissue, skeletal muscle, and the liver of mice on a high fat diet .
Anthramycin, a member of the pyrolobenzodiazepine (PBD) family, is a potent antibiotic. Anthramycin has potent antitumor activity. Anthramycin can act as an potent antagonist of cholecystokinin in the central nervous system in mice[1] .
Piperilate (Pipethanate) is one of the mixtures of hetrazepine derivative PAF antagonists with anticholinergics, can be used for bronchial asthma research. Piperilate also causes hypotension and rescues mice poisoned by the organophosphates [1] .
Adhesamine, dumbbell-shaped molecule, activates MAPK/FAK pathway. Adhesamine promotes adhesion and growth of mammalian cells. Adhesamine accelerates the differentiation and improves the survival of mice hippocampal neurons in primary culture [1].
Protoplumericin A is a bioactive ingredient of Plumeria obtusa L. attenuates. Protoplumericin A mitigated lipopolysaccharide (LPS) -induced acute lung injury in mice. Protoplumericin A can be used to study the LPS-induced anti-inflammatory effect [1].
F-1394 is an orally active acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor that inhibits dietary cholesterol absorption in mice. F-1394 can be used in cardiovascular disease research [1].
RB-6145 is an orally active pro-drug of the hypoxic cell radiosensitizer RSU 1069. RB-6145 acts a hypoxic cell radiosensitizer and cytotoxin but reduces systemic toxicity in mice[1].
HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer [1].
AZD5213 is a selective and competitive human H3 receptor antagonist with a pKi value of 9.3 for hH3R. AZD5213 can be used for the research of sleep and cognitive regulation [1] .
Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside is a orally active phenolic compound that can be isolated from the Geranium species. Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside has anti-inflammatory activities and has potential application in edema and aortic endothelium-dependent relaxation injury [1].
ERK-IN-7 (Example 10), an analogue of SHR2415 (HY-151367), is a potent ERK inhibitor with IC50 of 5 nM and 7 nM against ERK1 and ERK2, respectively [1].
TLR7 agonist 17 (compound 20) is a potent TLR7 agonist with EC50 values of 12 nM and 17 nM for hTLR7 and mTLR7, respectively. TLR7 agonist 17 shows anticancer activity [1].
D-Glucose- 13C,d-1 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research [1].
Diuron is a phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (2,500 ppm, dietary) increases the incidence of urinary bladder urothelial carcinomas in male and female mice by 73 and 27%, respectively.
Antimicrobial photosensitizer-1 is a promising candidate as the antimicrobial photosensitizer for combating pathogenic microorganism infections. Antimicrobial photosensitizer-1 exhibits an impressive antimicrobial efficacy in S. aureus-infected mice wounds [1].
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour [1].
Pimprinine is a potent monoamine oxidase inhibitor, could be isolated from fermented broths. Pimprinine has antioxidative activity and anticonvulsant activity. Pimprinine inhibits tremorine-induced tremors and analgesia in mice[1] .
β-Maaliene can be isolated from the fresh leaves of Vitex densiflora (Maaliene) and is the main component in the isolate. β-Maaliene can significantly reduce the exercise capacity of mice at certain doses [1].
GR 196429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. GR 196429 produces both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release in mice[1].
LY81067, a diaryltriazine, effectively protects against Pentylenetetrazole- and Picrotoxin-induced convulsions in mice. LY81067 exerts its anticonvulsant effects by binding to or near Picrotoxin (HY-101391) binding sites [1].
Tulisokibart (PRA023) is a humanized IgG1-κ monoclonal antibody targeting to TNFSF15/TL1A. Tulisokibart can be used to study a variety of inflammatory/fibrotic diseases, such as Crohn's Disease (CD) .
Ac-rC Phosphoramidite- 13C,d1 is deuterium and 13C-labeled Ac-rC Phosphoramidite (HY-W042357). Ac-rC Phosphoramidite is used for the oligoribonucleotide phosphorodithioate modification (PS2-RNA).
Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A [1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
PXS-4728A (BI-1467335) is a selective, orally active inhibitor of semicarbazide-sensitive amine oxidase (SSAO). PXS-4728A ameliorates chronic obstructive pulmonary disease in mice[1].
SAHM1, a peptide mimetic of a dominant negative form of mastermind-like (MAML), inhibits canonical Notch transcription complex formation. SAHM1 can be used for the research of allergic airway inflammation in mice[1] .
BBS-4 is a potent and selective inducible nitric oxide synthase (NOS2) dimerization inhibitor, with an IC50 of 0.49 nM. BBS-4 can protect mice from the cardiovascular dysfunction of sepsis [1].
SH-42 is a potent and selective inhibitor of human Δ 24-dehydrocholesterol reductase (DHCR24), with an IC50 of 42 nM. SH-42 can lead to a significant increase in plasma desmosterol levels of mice[1].
Ferulic acid 4-O-sulfate (Ferulic acid 4-sulfate) is a metabolite of Ferulic acid (HY-N0060). Ferulic acid 4-O-sulfate relaxes arteries and lowers blood pressure in mice[1].
Pterosin A is an orally active anti-diabetic agent. Pterosin A promotes glucose uptake, increases serum insulin, and improves hyperglycemia and glucose intolerance in diabetic mice. Pterosin A can be isolated from Pteridium aquilinum[1] .
RCB-02-4-8 is an ionizable cationic lipid that is used to form lipid nanoparticles (LNPs) to deliver mRNA. RCB-02-4-8 can improve the efficiency of lung transfection in mice[1].
Tucaresol is an orally bioavailable immunopotentiatory drug that show to enhance T-helper-cell activity, with the induction of increased IL-2 and IFN-γ levels in mice and humans. Tucaresol has anti-HIV effect [1].
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant [1] .
MCTR3 is a potent cytokine of pro-resolving mediating maresin conjugates in tissue regeneration (MCTR), which reduces the inflammatory response and promotes the tissue regeneration. MCTR3 exhibits potency in ameliorating LPS-induced acute lung injury and arthritis [1] .
Bruceantin(NSC165563) is first isolated from Brucea javanica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.
Pterosin B, a indanone found in bracken fern (Pteridium aquilinum), is an inhibitor of salt-inducible kinase 3 (Sik3) signaling. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3 [1] .
Tin protoporphyrin IX dichloride (SnPPIX) is a potent Heme oxygenase-1(HO-1) inhibitor. Tin protoporphyrin IX dichloride sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mice model [1].
Plantamajoside is a phenylpropanoid glycoside isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside has protective effects on LPS-induced acute lung injury (ALI) mice model. Plantamajoside has the potential for the treatment of pulmonary inflammation [1].
JH-X-119-01 hydrochloride is a potent and selective interleukin-1 receptor-associated kinases 1(IRAK1) inhibitor. JH-X-119-01 hydrochloride ameliorates LPS-induced sepsis in mice[1].
BAM(8-22), a proteolytically cleaved product of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner [1].
Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent [1] .
Acid Ceramidase-IN-1 is a potent and oral bioavailable acid ceramidase (AC, ASAH-1) inhibitor (hAC IC50=0.166 μM). Acid Ceramidase-IN-1 has excellent brain penetration in mice[1].
Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application [1].
Foralumab (NI-0401) is a potent, orally active human monoclonal antibody targeting the CD3. Foralumab modulates immune responses by human cells in NSG mice that were reconstituted with human hematopoietic stem cells [1].
Eucommiol is a natural product that can be isolated from the roasted leaves of E. ulmoides. Eucommiol inhibits growth of Molt 4B cells. Eucommiol reduces spontaneous activity and increases the sleep ratio in mice[1] .
Me-IQ (Methyl-IQ), an orally active heterocyclic amine, is carcinogenic and mutagenic. Me-IQ is several hundred-fold more mutagenic in liver than in lung microsomal preparations from uninduced mice and rabbits [1] .
Volvaltrate B is an anticancer agent, iridoid, can be obtained from the root of valerian (Valeriana officinalis). Volvaltrate B is effective against ovarian tumors in female mice. Volvaltrate B has the potential to study cancer [1] .
PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
8-Deazafolic acid is an antimicrobial drug for the folate-dependent bacteria, Streptococcus faecium (ATCC 8043) and Lactobacillus casei (ATCC 74691). 8-Deazafolic acid has activity against lymphoid leukemia L1210 in mice[1].
Lividomycin A is a broad-spectrum aminoglycoside antibiotic. Lividomycin A shows antimicrobial activity. Lividomycin A shows a positive protecting effect for the experimental infections in mice with several bacteria such as S. aureus, P. aeruginosa, Klebsiella pneumoniae and Escherichia coli[1].
DL-threo-PDMP hydrochloride is the hydrochloride form of DL-threo-PDMP that is a competitive glucosylceramide synthase (GCS) inhibitor. DL-threo-PDMP resensitizes refractory testicular germ cell tumors and epithelial ovarian cancer orthoxenografts to cisplatin in mice[1].
Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms [1] .
(E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice[1].
Chrysomycin B is an antibiotic isolated from a strain of Streptomyces. Chrysomycin B causes DNA damage in the human lung adenocarcinoma A549 cell line and inhibits topoisomerase II. Chrysomycin B suppresses the growth of transplantable tumors in mice.
BAM(8-22) TFA, a proteolytically cleaved product of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner [1].
Kadsurin, a natural compound from the stems of Kadsura heteroclita (Schizandraceae), results in significant decreases of CCL4- induced lipid-peroxidation products, such as thiobarbituric acid reactive substances (TBA-RS), conjugated dienes and fluorescent products in the liver of mice[1].
Anticancer agent 28 showed good antitumor activity in H22 allogeneic mice in vivo. Its potency in K562 cells was 50 times that of oridonin, and its < b > IC < sub > 50 < / sub > < / b > value was 0.09 μ M。
Polystyrene can form Polystyrene microplastics (PS-MPs), a hazardous material with potential toxicity. Polystyrene microplastics is harm to zebrafish heart and induces male reproductive toxicity in mice[1] . MCE provides Polystyrene products in solution packaging.
Andrographiside is a labdane diterpenoid glucoside that can be isolated from the leaves of Andrographis paniculata Nees. Andrographiside has antihepatotoxic and antioxidative effects. Andrographiside shows protective effects on mice with hepatotoxicity induced by carbon tetrachloride or tert-butylhydroperoxide (tBHP) [1].
Boc5 is a non-peptidic glucagon-like peptide-1 receptor agonist. Boc5 causes sustained glycemic control and weight loss in diabetic mice. Boc5 can be used in research of diabetic [1] .
Anti-inflammatory agent 46 (compound 7h) is an anti-inflammatory agent with nitric oxide (NO) inhibitory effect. Anti-inflammatory agent 46 binds to iNOS with low energies, inhibits swelling in mice (at dose of 10 mg/kg) [1].
J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. J-1048 can inhibit TAA-induced liver fibrosis in mice by explicitly blocking the TGF-β/Smad signaling pathway [1].
CDK2-IN-19 (Compound 32) is a selective and orally active CDK2 inhibitor (Ki: 0.18 nM). CDK2-IN-19 shows anticancer activity in mice bearing OVCAR3 tumors [1].
Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice[1].
2-Propyl-2-pentenoic acid is a metabolite of Valproic acid (HY-10585). 2-Propyl-2-pentenoic acid has a facilitating action on the acquisition of conditioned behavior with negative reinforcement in mice[1].
Medical fluorophore 33 is a novel quinoline-isoquinoline salt. Medical fluorophore 33 exhibits a strong fluorescent signal, good microsomal stability and high biocompatibility in vivo. Medical fluorophore 33 has antitumor activity in colorectal cancer mice[1].
MCAAD-3 is a near-infrared Aβ imaging probe with blood-brain barrier penetrability. MCAAD-3 has a strong affinity for Aβ polymers (Ki >106 nM) and can label Aβ plaques in the brains of transgenic mice[1].
A-71497 is the 3-formyl derivative of the antibiotic Tosufloxacin (HY-B1802). A-71497 can produce high plasma levels of tosufloxacin upon both oral and subcutaneous administration to mice[1].
Kp7-6, a Fas mimetic peptide, is a Fas/FasL antagonist. Kp7-6 protects cells from Fas-mediated apoptosis, and protects mice from Fas-mediated hepatic injury [1] .
NLRP3-IN-30 (Compound A14) is a potent NLRP3 inhibitor, with an IC50 of 44.43 nM. NLRP3-IN-30 has highly oral bioavailability (F is 83.09% in mice) [1].
Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM [1]. Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice .
Bruceine E is a quassinoid from seeds of Brucea javanica (L.) Merr, exhibiting hypoglycemia effect [1]. Bruceine E exhibits blood glucose lowering effect in both nondiabetic mice and Streptozotocin (STZ)-induced diabetic rats at lower dose .
Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model [1].
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice[1] .
Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1(TPH1) and TPH2 inhibitor with IC50s value of 33 nM and 7 nM, respectively, and shows robust reduction of intestinal serotonin (5-HT) levels in mice[1].
Osemozotan hydrochloride (MKC242) is a selective 5-HT1A receptor agonist. Osemozotan hydrochloride decreases the number of c-Fos-positive cells caused by MAMP in mice. Osemozotan hydrochloride can be used for the research of depressive disorder [1] .
CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model [1].
Cupressuflavone is a natural product that can be found in Cupressus macrocarpa. Cupressuflavone exhibits anti-inflammatory and antiulcerogenic activities. Cupressuflavone also show protective effects against CCl4-induced hepato- and nephrotoxicity in mice[1] .
KS370G is an orally active hypoglycemic and cardiovascular protective agent. KS370G improves left ventricular hypertrophy and function in pressure-overload mice heart. KS370G reduces renal obstructive nephropathy [1] .
ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) [1].
Gymnoside I (compound 1) is a glycosidoxybenzyl 2-isobutylmalic acid. Gymnoside I shows antiallergic activity in passive cutaneous allergic reaction (PCA) in mice. Gymnoside I can be used in research to treat asthma, neurasthenia and chronic hepatitis [1].
TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice. TAT-M2NX can be used to study ischemic neuronal damage [1].
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia [1] .
Ethoxyquin dimer is a dimer of Ethoxyquin (HY-B1425). Ethoxyquin dimer is an antioxidant. Ethoxyquin dimer can more readily accumulate in liver and adipose tissue compared with Ethoxyquin. Ethoxyquin above 10?mg/kg shows hepatotoxicity in mice[1].
9A1P9 is a multi-tail ionizable cationic phospholipid. 9A1P9 induces membrane destabilization. 9A1P9 can be used for CRISPR-Cas9 gene editing in mice[1].
(E)-SI-2 is an isomer of SI-2, an inhibitor of the steroid receptor coactivator SRC-3. SI-2 has anticancer activity and increases the number of cytotoxic immune cells in mice with breast cancer [1].
MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC50 of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation [1].
Benzyl alcohol is an aromatic alcohol, a colorless liquid with a mild aromatic odor. Benzyl alcohol is an inhibitor of P450 enzyme. Benzyl alcohol mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice[1] .
Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis [1].
ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA [1]. ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats .
Antipain is a protease inhibitor isolated from Actinomycetes. Antipain inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain restricts uterine DNA synthesis and function in mice[1] .
Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride restricts uterine DNA synthesis and function in mice[1] .
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice[1] .
Teglarinad chloride (GMX1777) is a proagent of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis [1] .
Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa [1].
BC-1258, an F-box/LRR-repeat protein 2 (FBXL2) activator, can stabilize and upregulate FBXL2 levels. BC-1258 induces apoptosis of tumorigenic cells, and profoundly inhibits tumor formation in mice[1].
CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model [1] .
Caprochlorone has antiviral activity against orthopoxvirus. Caprochlorone can inhibit cell penetration by virus, also delays release of newly formed virus from the cell. Caprochlorone decreases the titers of influenza virus in infected-mice lungs [1] .
6,9,12,15-Hexadecatetraenoic acid-ethyl ester is an orally active n-1PUFA. 6,9,12,15-Hexadecatetraenoic acid-ethyl ester intake can reduce plasma triglyceride content in mice[1].
Bavunalimab (Anti-Human CTLA4xLAG3) is a bispecific human anti-CTLA-4/LAG-3 monoclonal antibody. Bavunalimab activates T cells in NSG mice. Bavunalimab can be used for the research of cancer [1].
Hedragonic acid is an oleane-type triterpenoid compound, which can be isolated from the stems and roots of the southern snake vine. Hedragonic acid is a ligand and agonist for FXR. Hedragonic acid protected mice from liver damage caused by acetaminophen overdose and reduced liver inflammation [1].
Org 48762-0 is a potent, orally active and selective p38 inhibitor with EC50 of 0.1 μM. Org 48762-0 reduces LPS-induced TNFα release and prevents bone damage in collagen-induced arthritis in mice[1].
Chebulanin, a polyphenol acid, exerts its anti-inflammatory and anti-arthritic effects via inhibiting NF-κB and MAPK activation in collagen-induced arthritis mice. Chebulanin inhibits the nuclear translocation of p38 and p65 in LPS-stimulated macrophages [1].
NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E [1] .
Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].
NF-κB-IN-11 (Compound 3i) is a NF-κB inhibitor. NF-κB-IN-11 inhibits TNF-α induced activation of NF-κB pathway, and inhibits nuclear translocation of NF-κB. NF-κB-IN-11 down-regulates the expression levels of phosphor-IKK, IκBα, and NF-κB p65. NF-κB-IN-11 has anti-inflammatory activity, and alleviates dextran sulfate sodium-induced colitis in mice. NF-κB-IN-11 (p.o.) shows a MTD more than 1852 mg/kg in mice acute toxicity assay [1].
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice[1] .
γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).
Platycoside E is a platycodigenin-type saponin isolated from the root of Platycodon grandiflorum with haemolytic activity and adjuvant potential. Platycoside E promotes the production of the sera OVA-specific IgG2a and IgG2b antibody in the ovalbumin (OVA)-immunized mice[1].
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model [1].
iMDK is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice[1].
VU 0255035 is a highly selective, competitive and brain penetrant muscarinic M1 receptor antagonist with an IC50 of 130 nM. VU 0255035 reduces pilocarpine-induced seizures in mice. VU0255035 is used to examine the role of the M1 receptor in diverse situations [1].
Callophycin A, a red seaweed derived metabolite, possessing potent activity against Candida albicans with MIC of 62.5~250 mg/L. Callophycin A significantly reduces fungal burden of vaginal candidiasis induced mice, also decreases inflammatory response and immune molecules [1].
HEPPS (EPPS) is a buffering agent with the useful pH range from 7.3 ~ 8.7. HEPPS reduces Aβ-aggregate-induced memory deficits and rescues cognitive deficits in mice. EPPS is orally active and penetrates the blood-brain barrier [1].
Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease [1].
Efineptakin alfa (NT-17) is a long-acting recombinant human IL-7. Efineptakin alfa supports the proliferation and survival CD4 + and CD8 + cells in both human and mice. Efineptakin alfa can be used for glioblastoma research [1].
ccc_R08 is a non-cytotoxic and orally active cccDNA inhibitor that reduces cccDNA levels in the liver of HBV-infected mice. ccc_R08 can be used in the study of HBV virus (hepatitis B virus) infection [1] .
ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC50 of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice[1].
VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice[1].
FR-901235 is a new type of immunoactive substance produced by an imperfect fungus, Paecilomyces carneus F-4882. FR-901235 partially restored the impaired delayed-type hypersensitivity to sheep red blood cells in tumor-bearing mice[1].
CP7-FP13-2 is a peptide with antivirulence factor and antibacterial activity. CP7-FP13-2 inhibits the formation of Staphylococcus aureus biofilm and has good antibacterial efficacy in mice[1].
SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC50 of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice[1].
NJK14047 inhibits p38 MAPK and the differentation of naive T-cells to Th1 and Th17 cells. NJK14047 ameliorates the collage-induced rheumatoid arthritis and Imiquimod (HY-B0180)-induced psoriasis in mice[1].
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation [1].
DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research [1].
sEH/HDAC6-IN-1 (compound M9) is a selective, orally active dual inhibitor for sEH and HDAC6, with IC50s of 2 nM, 0.72 nM and 5 nM, for human sEH, murine sEH and HDAC6, respectively. sEH/HDAC6-IN-1 reveals analgesic and anti-inflammatory effects [1].
JAK3-IN-12 (compound 5k) is a highly potent JAK3 inhibitor with IC50 values of 9.5 nM, 18 nM and 42 nM for JAK3, JAK1 and JAK2, respectively. JAK3-IN-12 can be used for researching rheumatoid arthritis [1].
PD-L1-IN-6 (Compound 16) is an orally active inhibitor for PD-L1 expression in neutrophil by targeting STAT3 with KD of 90.5 nmol/L. PD-L1-IN-6 promotes neutrophil-mediated antifungal immunoresponse [1].
U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model [1] .
Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice[1].
MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice[1].
L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure [1] .
8-Epidiosbulbin E acetate, a furanoid, is abundant in Dioscorea bulbifera L.. 8-Epidiosbulbin E acetate exhibits broad-spectrum plasmid-curing activity against multidrug-resistant (MDR) bacteria. 8-Epidiosbulbin E acetate induces liver injury in mice[1] .
Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice[1].
O-2050 is a high affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2 receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice[1].
Strictosidinic acid, an orally active glycoside indole monoterpene alkaloid isolated from Psychotria myriantha leaves, inhibits precursor enzymes of 5-HT biosynthesis and reduces the 5-HT levels. Strictosidinic acid has peripheral analgesic and antipyretic activities in mice[1] .
Cinnamtannin A2, a tetrameric procyanidin, can increases GLP-1 and insulin secretion in mice. Cinnamtannin A2 could upregulate the expression of corticotrophin releasing hormone. Cinnamtannin A2 exhibits antioxidant, anti-diabetic and nephroprotective effect [1] .
Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].
M62812 (free base) is a toll-like receptor 4 (TLR4) signal transduction inhibitor. M62812 can suppress endothelial cell and leukocyte activation and prevents lethal septic shock in mice. M62812 can be used for the research of sepsis [1].
PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research [1].
Flaccidoside II inhibits proliferation and induces apoptosis in Malignant peripheral nerve sheath tumors (MPNSTs) cell lines. Flaccidoside II ameliorates collagen-induced arthritis in mice. Flaccidoside II is an active triterpenoid saponin constituent from Anemone flaccida rhizome [1] .
KPZ560 is a potent inhibitor of HDAC1 and HDAC2, with IC50s of 12 nM and 68 nM, respectively. KPZ560 can increase in the spine density of granule neuron dendrites of mice and inhibitor cell growth of breast cancer cell line MCF [1].
CM-10-18 is a potent and orally active inhibitor of both α-glucosidases I and II in vitro and in treated animals. CM-10-18 inhibits DENV infection of cultured human cells and reduces the peak viremia of DENV in mice[1].
Ferroptosis-IN-4 (compound 6k) is a ferroptosis inhibitor with EC50 value of 20 μM. Ferroptosis-IN-4 has no obvious cytotoxicity. Ferroptosis-IN-4 has a protective effect in glycerol-induced RM-AKI mice with alleviating kidney dysfunction [1].
hMAO-B-IN-6 (compound 17d) is a potent and selective inhibitor of hMAO-B with an IC50 of 67.02 nM. hMAO-B-IN-6 significantly improves Scopolamine (HY-N0296)-induced cognitive impairment in AD mice[1].
(R,R)-BD-AcAc 2 ((R,R)-Ketone Ester), a ketone monoester, can be used as a source of oral nutritional ketones. (R,R)-BD-AcAc 2 can elevate plasma levels of β-hydroxybutyrate and acetoacetate, blood glucose, blood Na + levels and blood creatinine levels after oral administration in mice. (R,R)-BD-AcAc 2 can partly prevent muscle weakness in septic mice. (R,R)-BD-AcAc 2 has potential to improve exercise performance and endurance in animal body. (R,R)-BD-AcAc 2 can also be used to research Parkinson’s disease or diabetes [1] .
Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727) [1]. Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3 . Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice .
Inarigivir (ORI-9020) is a dinucleotide antiviral drug that can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus. Inarigivir (ORI-9020) act as a RIG-I agonist to activate cellular innate immune responses [1] .
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa [1].
Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning [1] .
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats [1] .
iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice[1].
Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice[1] .
TMPRSS6-IN-1 (compound 8) is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to TTSPs (transmembrane serine protease). TMPRSS6, is a type II TTSP, the genetic reduction of which will improve symptoms of hemochromatosis and beta thalassemia in mice[1].
Hyptadienic acid is a triterpene acid that can be isolated from the leaves of Perilla frutescens. Hyptadienic acid inhibits 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice with an ID50 value of 0.13 mg/ear. Hyptadienic acid can be used for the research of inflammation [1].
TAT-CIRP is a a small peptide, refers to Trans-trans-activating (Tat)-cold-inducible RNA binding protein. TAT-CIRP is an inhibitor of myeloid differentiation protein 2 (MD2). TAT-CIRP exhibits robust neuroprotection against ischemic and hemorrhagic stroke in mice[1].
PSMA-IN-2 is an inhibitor of PSMA with a Ki value of 1.07 nM. PSMA-IN-2 displays favorable in vivo NIR imaging (λEM = 1088 nm, λex = 808 nm), and can be used for NIRII image-guided tumor resection surgery in PSMA-positive tumor-bearing mice[1].
Verazine ((-)-Verazine) is an anti-Fungal Agent that can be found in the dried roots and rhizoma of Veratrum maackii Regel. Verazine causes DNA damage in the cerebellum and cerebral cortex of mice in a dose-dependent manner. Verazine can be used in the study of fungal infections and neurological diseases [1] .
LB244 is a homologue of BB-Cl-amidine, which is an orally effective STING inhibitor (EC50=0.8 μM) and can be used to inhibit STING-dependent inflammatory diseases. The pharmacokinetic properties of LB244 indicate limited oral activity in mice[1].
RMI-61140 is an orally active neuroleptics. RMI-61140 decreases spontaneous motility and muscle tone in mice. RMI-61140 increases barbit urate-induced sleep and causes eyelid ptosis. RMI-61140 can be used for schizophrenia research [1].
L-Glutamic acid monosodium hydrate is a nutritional additive and flavoring agent. L-Glutamic acid monosodium hydrate can reduce obesity and induce metabolic disorders associated with oxidative stress. L-Glutamic acid monosodium hydrate induces oxidative stress,DNA damage and apoptosis in the liver and brain tissues of mice[1] .
BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice[1].
NN1177 (NNC9204-1177) TFA is a long-acting GLP-1/glucagon receptor co-agonist. NN1177 TFA can induce a dose-dependent body weight loss in diet-induced obese (DIO) mice[1] .
Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice[1] .
Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice[1] .
Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades [1].
Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD) [1] .
Tussilagone, a major active component in Tussilago farfara, has anti-inflammatory effect. Tussilagone ameliorates inflammatory responses in dextran sulphate sodium-induced murine colitis. Tussilagone inhibits the inflammatory response and improves survival in cecal ligation and puncture (CLP)-induced septic mice[1] .
NIR-Thiol dinitrobenzenesulfonate has both absorption and emission in the NIR region. NIR-Thiol dinitrobenzenesulfonate responds to thiol with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-Thiol dinitrobenzenesulfonate is capable of imaging endogenously produced thiol in living cells and mice[1].
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A) [1].
Ser@TPP@CUR is a Curcumin (HY-N0005) derivative. Ser@TPP@CUR effectively ameliorates injured renal tubular epithelial cells and improves renal functions of acute kidney injury (AKI) mice. Ser@TPP@CUR can be used for the research of AKI [1] .
Oleoyl-D-lysine is a selective Glycine Transporter-2 (GlyT2) inhibitor based on lipid. Oleoyl-D-lysine reverses neuropathic pain in mice, shows antidrowsiness effect on chronic neuropathic pain. Oleoyl-D-lysine is safe and effective without respiratory depression [1].
8-Chloroadenosine (8-Cl-Ado), a unique ribonucleoside analog, depletes endogenous ATP that subsequently induces the phosphorylation and activation of AMPK. 8-Chloroadenosine induces autophagic cell death. 8-Chloroadenosine effectively inhibited in vivo tumor growth in mice[1].
Demethyleneberberine chloride is a natural mitochondria-targeted antioxidant. Demethyleneberberine chloride alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine chloride could serve as a AMPK activator for researching non-alcoholic fatty liver disease (NAFLD) [1] .
sEH inhibitor-16 is a soluble epoxide hydrolase (sEH) inhibitors with an IC50 of 2 nM. sEH inhibitor-16 reduces the inflammatory damage in Cerulein (HY-A0190)-induced acute pancreatitis (AP) in mice and can be used for inflammation/immunology research [1].
HJC0152 (free base) is an orally active and potent inhibitor of STAT3. HJC0152 (free base) inhibits cell cycle progression and induces apoptosis. HJC0152 (free base) significantly suppresses MDA-MB-231 xenograft tumor growth in mice[1].
Fulvotomentoside B is a saponin isolated from Lactobacillus flavus. Fulvotomentoside compounds can significantly reduce serum glutamate pyruvate transaminase (SGPT) and triacylglycerol (GT) levels in mice poisoned by CCl4, d-galactosamine (d-gal) and acetaminophen, and significantly alleviate liver pathology. damage [1].
cpm-1285 induces apoptosis by functionally blocking intracellular Bcl-2 and related death antagonists. cpm-1285 shows strong binding potency to Bcl-2 with an IC50 value of 130 nM. cpm-1285 reduces tumor burden in mice[1].
Antitrypanosomal agent 19 (compound 10) is an orally available antitrypanosomal agent. Antitrypanosomal agent 19 effectively inhibits the growth of trypanosomatids T. b. brucei, T. b. gambiense and T. b. rhodesiense, mitigating the Human trypanosomiasis (HAT)-induced acute infectious toxicity in mice[1].
Anti-inflammatory agent 66 (compound 8) is a pterostilbene derivative with anti-inflammatory activity. Anti-inflammatory agent 66 inhibits pro-inflammatory cytokines by blocking the LPS-induced NF-κB/MAPK signaling pathway and effectively alleviates DSS-induced acute colitis in mice[1].
AChE/Aβ-IN-5 (compound AV-2) is a bifunctional inhibitor that targets AChE and auto-induced Aβ (Amyloid-β) aggregation. AChE/Aβ-IN-5 can significantly improve scopolamine- and Aβ-induced cognitive impairment in mice[1].
UK4b is a highly selective microsomal prostaglandin E2 synthase-1(mPGES-1) inhibitor. UK4b possesses anti-inflammatory and analgesic effects. UK4b can block the growth of abdominal aortic aneurysms in mice[1].
Duvakitug is a humanized IgG1-λ2 monoclonal antibody targeting to TNFSF15/TL1A. Duvakitug' main expression system is CHOK1SV cells endogenously expressing glutamine synthetase (GS). Duvakitug can be used in the study of Crohn's Disease (CD) .
RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport [1] .
Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer [1].
Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research [1].
Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice[1] .
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase[1].
T-peptide, a Tuftsin analog, can be used for the research of human immunodeficiency virus (HIV) infection. T-peptide prevents cellular immunosuppression and improves survival rate in septic mice. T-peptide also can inhibit the growth of residual tumor cells after surgical resection [1] .
ML372 inhibits survival motor neuron (SMN) protein ubiquitination, increases SMN protein stability without affecting mRNA expression. ML372 improves spinal muscular atrophy (SMA) in mice. ML372 is brain penetrant and has a reasonable exposure and half-life in vivo [1].
CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma [1].
Almurtide (nor-MDP), a muramyl dipeptide derivative with anti-inflammatory and anti-tumor activity. Almurtide also shows protective effects against intraperitoneal Pseudomonas aeruginosa infection or intravenously Candida albicans infection in mice. Almurtide also inhibits the carcinogenic Friend leukemia virus [1] .
Riboxin (IDP), an orally active purine derivative-hypoxanthine rlboside, has antihypoxic and antihyperthermic activity. Riboxin also has an antiarrhythmic action in cats, rabbits, and mice with cardiac rhythm disorders induced by Ouabain. Riboxin protects animals against the noxious effects of γ-irradiation [1] .
GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) [1]. GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
RG33 Peptide is a diabetes inhibitor that significantly improves glucose clearance in insulin-resistant mice. RG33 Peptide effectively solubilizes lipid vesicles and promotes cholesterol efflux in cultured macrophages. RG33 Peptide is used in research into type 2 diabetes (T2D) [1].
A8SGLP-1 is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 reduces blood glucose in db/db mice without affecting its function [1].
Z-Leu-Leu-Leu-fluoromethyl ketone (Z-LLL-FMK) is a cysteine protease inhibitor. Z-Leu-Leu-Leu-fluoromethyl ketone inhibits SARS infection. Z-Leu-Leu-Leu-fluoromethyl ketone also protects mice against a T. crassiceps challenge [1] .
QL-1200186 is anorally activeand selective inhibitor ofTYK2. Oral administration of QL-1200186, dose-dependently inhibitsinterferon-γ(IFNγ) production afterinterleukin-12(IL-12) challenge and significantly ameliorates skin lesions in psoriatic mice[1].
UCM-13207 (compound 21) is a selective ICMT inhibitor that ameliorates basic progeria-like features. UCM-13207 can improve the survival rate of LmnaG609G/G609G mice in the mouse premature aging model [1].
Ansamitocin P 3' (Antibiotic C 15003P3') is an anti-tumor antibiotic. Ansamitocin P 3' prolongs the survival of mice with leukemia P388, melanoma B16, leukemia L1210, sarcoma 180, Ehrlich carcinoma and mast cell tumor P815 [1].
Berubicin (RTA 744 free base; WP 744) is a 4'-O-benzyldoxorubicin that inhibits P-gp and MRP1-mediated efflux and has anticancer activity. Berubicin inhibits glioblastoma multiforme (GBM) and exhibits cytotoxicity. Berubicin has poor bioavailability in mice[1].
Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1] .
DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice[1] .
Celosin I, an oleanane-type triterpenoid saponin isolated from the seeds of Celosia argentea L, could be used as chemical markers for the quality control of C. argentea seeds. Celosin I exhibits significant hepatoprotective effect on carbon tetrachloride-induced and N,N-dimethylformamide-induced hepatotoxicity in mice[1] .
NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues . NNMTi promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice[1].
GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice[1] .
MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice[1] .
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice[1] .
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].
HP1328 is a potent inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1328 is a benzoimidazole scaffold-based compound. HP1328 significantly reduces the leukemia burden and prolongs the survival of mice with FLT3/ITD leukemia [1].
Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model [1].
SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice[1].
KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research [1].
Anticancer agent 108 (Compound 3.10) is a potent P-gp inhibitor with significant antitumor activity and less toxicity to normal and pseudonormal cells. Anticancer agent 108 (Compound 3.10) had no acute toxic effect on С57BL/6 mice[1].
M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis [1].
ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC50 of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses [1].
β-Amyloid (1-16) rat is a β-amyloid peptide (Abeta), a metal-binding domain fragment of amyloid. Three amino acid substitutions in β-Amyloid (1-16) rat that differ from humans render rats and mice less susceptible to AD-like neurodegeneration [1].
Tridocosahexaenoylglycerol (TG-DHA) is an orally active dietary supplement that improves autoimmune encephalomyelitis in mice. Tridocosahexaenoylglycerol shows beneficial effects on neurodegenerative diseases and also improves macular function in diabetic retinopathy. Tridocosahexaenoylglycerol can be used for research on neurological diseases, inflammatory immune diseases, and metabolic diseases [1] .
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively [1].
IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2 [1].
Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning [1] .
ND-336 is a selective inhibitor of matrix metalloproteinase (MMP)-2, MMP-9, and MMP-14, with Kis of 85, 150, and 120 nM, respectively. ND-336 accelerates diabetic wound healing in mice by lowering inflammation and by enhancing angiogenesis and re-epithelialization of the wound [1] .
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis [1].
PAL-4 (compound 4) is a potent, selective and reversible Lysophospholipase-like 1(LYPLAL1) activator with EC50 value of 0.39 μM and 0.49 μM for mice LYPLAL1 and huamn LYPLAL1, respectively. PAL-4 can be used for researching metabolic disorders [1].
Cyclic HPMPC is a potent antiviral agent. Cyclic HPMPC can increase arterial oxygen saturation levels in lethal vaccinia virus (IHD strain)-infected mice. Cyclic HPMPC improves the outcome of congenital guinea pig cytomegalovirus (GPCMV) infection and decreases viral replication in guinea pig model [1] .
Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate causes renal toxicity in mice[1] .
JNc-440 is a potent antihypertensive agent. JNc-440 can enhance the interaction of TRPV4 and Ca 2+-activated potassium channel 3 (KCa2.3) in endothelial cells. JNc-440 can also enhance vasodilation, and exerted antihypertensive effects in mice[1].
GPR119 agonist 2 (compound 43) is an orally active GPR119 agonist. GPR119 agonist 2 shows good pharmacokinetic characteristics in rodents and can effectively improve glucose tolerance in mice and rats. GPR119 agonist 2 has the potential to study type 2 diabetes [1].
LNP Lipid-8 (11-A-M) is an ionizable lipid, which can be used for lipid nanoparticles (LNP) to deliver siRNA to T cells without targeting to ligands. LNP LIPs-8 loaded with GFP siRNA (siGFP), and significantly causes GFP gene silencing in mice model [1].
PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC50: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%) [1].
KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell [1].
A8SGLP-1 TFA is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 TFA reduces blood glucose in db/db mice without affecting its function [1].
TMDJ-035 is a selective RyR2 inhibitor. TMDJ-035 suppresses abnormal Ca 2+ waves and transients in isolated cardiomyocytes from RyR2-mutated mice. TMDJ-035is a tool for studying the mechanism and dynamics of RyR2 channel gating [1].
α-Glucosidase-IN-44 (compound IT4) is an inhibitor of α-glucosidase with IC50 value of 2.35 μM. α-Glucosidase-IN-44 has an oral activity. α-Glucosidase-IN-44 suppresses fasting blood glucose levels in diabetic mice[1].
β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice[1].
Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice[1] .
GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats [1] .
GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats [1] .
Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning [1] .
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research [1] .
GLP-1(32-36)amide TFA, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide TFA could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice[1] .
Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity [1].
YC-001 is an inverse agonist and antagonist of rod opsin. YC-001 reversibly binds rod opsin and stabilizes the rod opsin structure. YC-001 protects mice from bright light-induced retinal degeneration. YC-001 has the potential for the research of retinal degeneration [1].
3β-Hydroxylanosta-8,24-dien-21-al is a lanostane-type triterpene. 3β-Hydroxylanosta-8,24-dien-21-al can inhibit the tumor promotion, reducing the percentage of mice bearing papillomas [1].
Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis [1] .
Sergliflozin etabonate (GW-869682X) is a potent and orally active sodium glucose cotransporter (SGLT2) inhibitor. Sergliflozin etabonate shows antidiabetic and antihyperglycemic effects. Sergliflozin etabonate significantly reduces non-fasting blood glucose levels in diabetic mice. Sergliflozin etabonate has the potential for the research of diabetes [1].
KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice[1] .
Zymosan A (Zymosan A from Saccharomyces cerevisiae) is a TLR2 agonist, that targeting TLRs can prevent and suppress IR-induced intestinal injury. Zymosan A exhibits a significant radioprotective effect, and protects IR-induced intestinal injury in mice. Zymosan A promotes the regeneration of intestinal stem cells (ISCs), after IR injury [1].
NFL-NH2 is a mitochondrial-targeted near-infrared ratiometric fluorescent probe. NFL-NH2 can rapidly detect NO levels associated with the inflammatory damage degree in rheumatoid arthritis (RA) mice models by ratiometric fluorescence imaging. The excitation wavelength and emission wavelength are 650 nm and 780 nm, respectively [1].
NNC 55-0396 is a highly selective T-type calcium channel blocker with an IC50 value of 6.8 μM for Cav3.1 T-type channels. NNC 55-0396 can be used for the research of neurological disease research [1] .
D-Mannose is a C-2 superpolymer of glucose that occurs naturally in many plants and fruits. D-Mannose has anti-inflammatory and antitumor activity. D-Mannose plays an important role in immune regulation [1] .
PMEDAP is a potent inhibitor of human immunodeficiency virus (HIV) replication. PMEDAP has anti-murine cytomegalovirus (MCMV) activity. PMEDAP is a very potent inhibitor of Moloney murine sarcoma virus (MSV)-induced tumor formation and associated mortality [1] .
NADH-IN-1 has NADH:ubiquinone oxidoreductase inhibitory activity with an IC50 value of 27 μM. NADH-IN-1 can effectively stimulate glucose uptake in vitro. NADH-IN-1 is readily metabolised by the liver. NADH-IN-1 can be used for researching diabetes [1].
MRGPRX1 agonist 3 (compound 1f) is a potent Mas-related G protein-coupled receptor X1(MRGPRX1) positive allosteric modulator with an EC50 value of 0.22 μM. MRGPRX1 agonist 3 can be used for researching neuropathic pain [1].
5-Methoxycanthin-6-one is an orally active inhibitor of Leishmania strains. 5-Methoxycanthin-6-one shows cytotoxicity with an IC50 of 5.44 μg/mL against Ailanthus altissima cells [1] .
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor [1].
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC), a cyclic RGD peptide which has high affinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors [1].
Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML [1].
Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro[1].
JC2-11 is an inhibitor of inflammatory corpuscles. JC2-11 inhibits domain-containing protein NLRC 4, absent in melanoma 2 (AIM 2) and non-canonical (NC) inflammatory corpuscles. JC2-11 reduces the secretion of caspase-1 (p20), the cleavage of gasdermin D (GSDMD), and the releases of IL-1β and lactate dehydrogenases (LDH) in inflammatory bodies. JC2-11 inhibits the activation of inflammatory bodies by destroying the production of reactive oxygen species and the activity of caspase-1[1].
PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes [1] .
c-Myc inhibitor 9 (compound 332) is a c-Myc inhibitor with an logEC50 of ≥6. c-Myc inhibitor 9 inhibits tumor growth in nude mouse models. c-Myc inhibitor 9 can be used for cancer research [1].
Subtilisin (Compound proteinase) (EC 3.4.21.62) is a proteolytic enzyme, isolated from Bacillus licheniformis. Subtilisin (Compound proteinase) has catalytic activity in anhydrous dimethyl formamide. Subtilisin (Compound proteinase) can be used as a catalyst for easy coupling between sugars and amino acids [1] .
Lutikizumab (ABT-981) is an anti-IL-1α and IL-1β dual variable domain immunoglobulin. Lutikizumab binds and inhibits IL-1α and IL-1β. Lutikizumab can be used for the research of osteoarthritis [1].
MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the iNOS activity and reduces the expression of p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity [1].
Cisd2 agonist 1 (Compound 4q) is a Cisd2 agonist (EC50: 34 nM). Cisd2 agonist 1 enhances the Cisd2 expression and improves the pathological changes in the fatty livers. Cisd2 agonist 1 has good metabolic stability. Cisd2 agonist 1 can be used for research of NAFLD [1].
HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacterium tuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacterium tuberculosis infection [1].
Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury [1] .
Cyclovalone (Beveno) is a synthetic curcumin derivate, which inihibits cyclooxygenase and exhibits anti-inflammatory, antitumor and antioxidant activities [1]. Cyclovalone inhibits cell proliferation in normal and malignant prostatic cells. Cyclovalone ist orally active .
COE-PNH2 exhibits antibacterial activity against Mycobacterium abscessus (Mab) with MIC90 of 26 μM. COE-PNH2 affects the integrity of the bacterial envelope and mycomembrane. COE-PNH2 reveals intracelluar penetration without mitochondrial toxicity [1].
Leukotriene B4 ethanolamide (LTB4 ethanolamide) is an antagonist and a partial agonist for Leukotriene B4 (LTB4) receptor 1(BLTR1). Leukotriene B4 ethanolamide ameliorates the tumor progression, which is only asscociated with inflammation [1] .
OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) [1].
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice[1] .
Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[1] .
Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice[1] .
L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1] .
Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice[1].
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice[1].
TAT-Gap19, a Cx mimetic peptide, is a specific connexin43 hemichannel (Cx43 HC) inhibitor. TAT-Gap19 does not inhibits the corresponding Cx43 GJCs. TAT-Gap19 traverses the blood-brain barrier and alleviate liver fibrosis in mice[1] .
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1) [1]. GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice .
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1) [1]. GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice .
Inarigivir (ORI-9020) ammonium is a dinucleotide antiviral drug that can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus. Inarigivir (ORI-9020) ammonium acts as a RIG-I (Retinoic acid-inducible gene-I) agonist to activate cellular innate immune responses [1] .
Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD) [1] .
Antroquinonol ((+)-Antroquinonol), a ubiquinone derivative from the mushroom Antrodia camphorata, has hepatoprotective, anti-inflammatory, and anti-cancer effects [1]. Antroquinonol can be used for the research of colon cancer . Antroquinonol reduces oxidative stress by enhancing the Nrf2 signaling pathway and inhibits inflammation and sclerosis in focal segmental glomerulosclerosis mice .
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice[1].
ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research [1].
NIOCH 14 is a antiviral agent and a pro-agent. NIOCH 14 has antiviral activity against orthopoxviruses. NIOCH 14 can significantly lower proportions of infected mice, and virus production levels in the lungs. NIOCH 14 can be used for researching anti-smallpox [1] . NIOCH 14 shows anti-orthopoxvirus activity.
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects [1] .
RXFP2 agonist 2 is a selective，orally active and allosteric RXFP2 agonist with an EC50 value of 0.38 µM. RXFP2 agonist 2 induces osteoblast mineralization. RXFP2 agonist 2 increases bone formation in female mice. RXFP2 agonist 2 has the potential for the research of osteoporosis [1].
NLRP3-IN-17 is a potent, selective and orally active NLRP3 inflammasome inhibitor with an IC50 value of 7 nM. NLRP3-IN-17 significantly inhibits NLRP3 dependent IL-1β secretion in mice and can be used for chronic inflammatory diseases research [1].
GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
GLP-1 receptor agonist 10 (compound 42) is an agonist of GLP Receptor. GLP-1 receptor agonist 10 inhibits food intake and reduces glucose excursion in mice. GLP-1 receptor agonist 10 can be used in the study of type 2 diabetes (T2DM) and obesity [1].
PAD4-IN-2 (compound 5i) is a PAD4 inhibitor (IC50=1.94 μM). PAD4-IN-2 inhibits tumor growth in mice by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils [1].
Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases [1] .
Antibacterial agent 150 (compound 5g) is an antibacterial agent with potent antibacterial activity against both Gram-positive bacteria and Gram-negative bacteria (MIC values ranging from 1-32 μg/mL). Antibacterial agent 150 can increase survival rate of MRSA (Methicillin-resistant Staphylococcus aureus)-infected mice[1].
RORγt inverse agonist 31 (14g) is a potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 0.428 μM. RORγt inverse agonist 31 can alleviate the severity of Imiquimod (HY-B0180)-induced psoriasis in mice[1].
Chb-M′ (Compound Conjugate 1) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. Chb-M′ induces the p53-dependent apoptosis and inhibits cancer cell growth. Chb-M′ inhibits tumor growth in PANC-1 xenograft mice[1].
Albofungin (Antibiotic P-42-1) is isolated from the culture filtrate of Actinomyces tumemacerans strain INMI.P-42. Albofungin shows highly active on a wide variety of gram-positive bacteria and fungi. Albofungin shows cytotoxic to HeLa cell cultures and exhibited antitumor activity on EHRLICH ascites tumor in mice.
7-Deoxy-trans-dihydronarciclasine, an alkaloid, is a tobacco mosaic virus (TMV) inhibitor (IC50: 1.80 μM). 7-Deoxy-trans-dihydronarciclasine is an anti-neuroinflammatory agent. 7-Deoxy-trans-dihydronarciclasine decreases the Aβ and APP levels in the cerebral cortex of Tg2576 mice[1] .
7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro [1].
GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
RGH-560 (compound 53) shows highly advanced α7 nAChR positive modulator properties and favorable physicochemical features. RGH-560 has robust procognitive in vivo potential. RGH-560 can be used to study Scopolamine (HY-N0296) -induced amnesia in mice[1].
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR [1].
FR900098 is an antimalarial agent that inhibits 1-deoxy-d-xylulose-5-phosphate (DXP) reductoisomerase. FR900098 has no significant acute toxicity or genotoxicity, and does not have the ability to cause chromosome breakage or heterogeneity. FR900098 has no effect on bone marrow red blood cells in NMRI mice[1].
Odevixibat-d5 is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis [1].
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe −/− Irs 2+/−mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation .
MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice[1].
CADD522 is a RUNX2-DNA binding inhibitor (downregulates RUNX2-mediated transcription of downstream target genes), with an IC50 of 10 nM. CADD522 inhibits primary tumor growth and experimental metastasis of tumor cells in the lungs of immune-compromised mice. CADD522 can be used in study of cancer [1] .
Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice[1] .
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research [1] .
TAT-Gap19 TFA, a Cx mimetic peptide, is a specific connexin43 hemichannel (Cx43 HC) inhibitor. TAT-Gap19 TFA does not inhibits the corresponding Cx43 GJCs. TAT-Gap19 TFA traverses the blood-brain barrier and alleviate liver fibrosis in mice[1] .
MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively [1].
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy [1].
AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity [1] . AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway .
C12-200 is an ionizable cationic lipid and auxiliary lipid. C12-200 is commonly used for mRNA delivery. Administration of human erythropoietin (EPO) mRNA or factor VII siRNA increased and decreased serum factor VII levels, respectively, in LNPs mice containing C12-200 [1] .
DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage [1].
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO.ErSO-DFP displays antitumor activity and leads to profound regression of MCF-7 tumors in mice model [1].
ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model [1].
Corydalmine hydrochloride inhibits spore germination of some plant pathogenic as well as saprophytic fungi [1]. Corydalmine hydrochloride acts as an oral analgesic agent, exhibiting potent analgesic activity . Corydalmine hydrochloride alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway .
JMV 390-1 (Compound 6a) is a potent multipeptidase inhibitor. JMV 390-1 behaves as a full inhibitor of the major neurotensin (NT)/neuromedin N (NN) degrading enzymes in vitro with IC50 values from 30 to 60 nM. JMV 390-1 increases endogenous recovery of NT and NN from slices of mice hypothalamus depolarized with potassium [1].
ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research [1].
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice[1] .
SIMR3030 is a potent SARS-CoV-2 PLpro inhibitor with an IC50 value of 0.0399 µg/mL. SIMR3030 shows antiviral activity. SIMR3030 decreases SARS-CoV spike, ORF1b, IFN-α, IL-6 mRNA expression. SIMR3030 exhibits a satisfactory safety profile in mice[1].
Bozepinib is a PKR (RNA-dependent protein kinase) activator and potently inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces PKR-mediated apoptosis and synergizes with IFNα to trigger apoptosis, autophagy and senescence. Bozepinib also demonstrates in vivo antitumor and antimetastatic efficacy in xenografted nude mice[1] .
Mosnodenvir (JNJ-1802) is a pan-serotype dengue antiviral agent with a high barrier to resistance, and is safe and well-tolerated. Mosnodenvir blocks the NS3-NS4B interaction within the viral replication complex. Mosnodenvir shows picomolar to low nanomolar in vitro antiviral activity in mice[1] .
Suffruticosol A is a neuroprotective agent that restores scopolamine-induced cellular neurodegenerative damage. Suffruticosol A ameliorates hippocampal cholinergic deficits and partially enhances BDNF signaling. Suffruticosol A has neuromodulatory effects in a Scopolamine (HY-N0296)-induced model, restoring memory and cognitive performance in mice. Suffruticosol A can be isolated from seeds of P. lactiflora [1].
Urumin has antiviral activity against the human influenza A virus. Urumin inhibits the growth of PR8 influenza virus (IC50: 3.8 μM). Urumin targets the conserved stalk of H1 hemagglutini, and is effective at neutralizing drug-resistant H1 influenza viruses. Urumin protects naive mice from lethal influenza infection [1].
CMPF can be found in trace constituent of urine and blood. CMPF is a biomarker of type 2 diabetes. CMPF can act on the β cell and induces impaired mitochondrial function. CMPF decreases glucose-induced ATP accumulation, and induces oxidative stress. CMPF reverses hepatic lipid accumulation and improves insulin sensitivity in obese mice[1] .
Stevisalioside A (Compound 2) can be isolated from Stevia serrata roots. Stevisalioside A is an orally active antidiabetic agent. Stevisaliosides A inhibits PTP1B (IC50: 526.8 μM). Stevisalioside A reduces blood glucose levels and the postprandial peak in oral glucose and insulin tolerance tests in Streptozotocin (HY-13753) induced hyperglycemic mice[1].
TASP0277308 is a highly selective S1P1 antagonist. TASP0277308 possesses immunomodulatory activities, including lymphopenia, a block in T cell egress from the thymus, marginal zone B cell displacement, and the upregulation of CD69 expression on lymphocytes. TASP0277308 can be used for the research of collagen-induced arthritis in mice[1].
Benzyl alcohol (Standard) is the analytical standard of Benzyl alcohol. This product is intended for research and analytical applications. Benzyl alcohol is an aromatic alcohol, a colorless liquid with a mild aromatic odor. Benzyl alcohol is an inhibitor of P450 enzyme. Benzyl alcohol mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice[1] .
pNPS-DHA (Compound 19) is an orally active DHA-ethanolamide (DHEA) derivative that has antiallergic activity. pNPS-DHA inhibits IgE-dependent passive cutaneous anaphylaxis (PCA) reaction in mice. pNPS-DHA has anti-degranulating activity in RBL-2H3 mast cells with an IC50 of 15 μM [1].
FR900098 sodium is an antimalarial agent that inhibits 1-deoxy-d-xylulose-5-phosphate (DXP) reductoisomerase. FR900098 sodium has no significant acute toxicity or genotoxicity, and does not have the ability to cause chromosome breakage or heterogeneity. FR900098 sodium has no effect on bone marrow red blood cells in NMRI mice[1] .
C12-113 is a lipidoid delivery agent that can be used to transfect siRNA into cells. C12-113 can also be combined with other lipids to form lipid nanoparticles (LNPs) for the delivery of mRNA encoding the spike glycoprotein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in mice[1] .
α-Glucosidase-IN-57 (Compound 10c) is a competitive and orally active α-glucosidase inhibitor with an IC50 value of 0.180 μM and a Ki of 0.15 μM. α-Glucosidase-IN-57 can reduce fasting and overall blood glucose levels in mice, and can be used for anti-diabetes research [1].
Odevixibat- 13C6 is 13C labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis [1].
Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis[1] .
Pavurutamab (AMG-701) is a bispecific T cell engager molecule that anti-CD3 and anti-B cell maturation antigens (BCMA). Pavurutamab has an extended half-life based on Pacanalotamab (HY-P99798). The Fc of Pavurutamab is coupled to molecules to improve pharmacokinetic parameters. Pavurutamab has potential applications in immune regulation and multiple myeloma (MM) [1] .
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice[1] .
Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM [1] . Apocynin improves acute lung inflammation in Carrageenan (HY-125474)-induced pleurisy mice model . Apocynin can also be used for cancer research . Apocynin reverses the aging process in mesenchymal stem cells to promote osteogenesis and increases bone mass .
Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice[1] .
USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model [1] .
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1(PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis [1] .
13-Oxo-9E,11E-octadecadienoic acid, an isomer of 9-oxo-ODA, is a potent PPARα activator derived from tomato juice. 13-Oxo-9E,11E-octadecadienoic acid decreases plasma and hepatic triglyceride in obese diabetic mice[1].
BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL) [1].
Menthol is an analgesic and TRPM8 modulator. TRPM8 is a cold temperature sensing ion channel, and Menthol can regulate TRPM8 to exert analgesic and anti-irritation mechanisms. Menthol stimulates cold receptors and produces a cooling sensation by inhibiting Ca ++ currents in neuronal cell membranes. Menthol also improves oral nicotine rejection in mice[1] .
Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects [1] .
Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature [1].
Corydalmine (L-Corydalmine) inhibits spore germination of some plant pathogenic as well as saprophytic fungi [1]. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity . Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway .
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue [1].
LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression [1].
RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice[1].
Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice[1].
PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion [1].
LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity [1] .
Antiproliferative agent-4 (compound 2y) has excellent anti-proliferative activity against certain cancer cell lines. Antiproliferative agent-4 reduces the mitochondrial membrane potential, and increases the apoptosis rate and the level of ROS on EC109. Antiproliferative agent-4 inhibits tumour growth in nude mice, with low toxicity [1].
SAE-14 (compound SAE-14) is a potent, specific GPR183 antagonist with an IC50 value of 28.5 nM, can antagonize 7α, 25-OHC–induced calcium mobilization with IC50 value below 50 nM in HL-60 cells. GPR183 antagonist-1 can reverse allodynia in mice[1].
M47 is a small molecule that selectively destabilizes Cryptochrome 1 (CRY1) and increases degradation of the CRY1 in the nucleus. M47 enhances apoptosis in Ras-transformed P53-deficient mouse skin fibroblast lines and enhances life span in p53 knockout mice. M47 can be used in research of cancer [1].
AMPD2 inhibitor 2 (compound 21) is a potent AMP deaminase 2 (AMPD2) inhibitor with IC50s of 0.1 μM and 0.28μM for hAMPD2 and mAMPD2, respectively. AMPD2 inhibitor 2 has the potential for evaluating the physiological role of AMPD2 in mice maintained on a high fat diet [1].
Bevonescein (ALM-488) is a novel, intravenously-administrated fluorescein-conjugated peptide that binds nerve-associated connective tissue, labels peripheral nerves under real-time fluorescence imaging (FL) in living mice and human ex vivo nerve tissue. Bevonescein is a peptide-linked tracer which fluorescently labeled both intact and degenerated nerves [1] .
FITC-labeled Tominersen (sodium) is the Tominersen labeled with FITC. Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD).
I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research [1].
AUTEN-67 (Autophagy enhancer-67) is an orally active autophagy enhancer and MTMR14 inhibitor. AUTEN-67 has anti-aging and neuroprotective effects. AUTEN-67 protects neurons from stress-induced cell death. AUTEN-67 also restores nesting behavior in a mice model of Alzheimer disease [1].
Taxamairin B is a potent anti-inflammatory agent. Taxamairin B decreases proinflammatory cytokines (TNF-α, IL-1β and IL-6) expression and the production of NO and ROS in LPS-induced RAW264.7 cells. Taxamairin B exhibits significant
protective effects in LPS-induced acute lung injury in mice[1] .
CW 008, a derivative of pyrazole-pyridine, is a CREB or PKA pathway agonist. CW 008 also is a stem cell differentiating agent. CW 008 stimulates osteoblast differentiation of human MSCs and increases bone formation in ovariectomized mice. CW008 promotes osteogenesis by activating cAMP/PKA/CREB signaling pathway and inhibiting leptin secretion [1] .
PB94 is a selective HDAC11 inhibitor (IC50=108 nM). PB94 can be radiolabeled as [11C]-PB94 for use in positron emission tomography (PET), as well as brain uptake and metabolic properties in administered live animals. PB94 improves neuropathic pain in mice and could be used to study neurological indications [1].
Isozaluzanin C (Dehydrozaluzanin c-derivative) is an anti-inflammatory agent that can be isolated from Saussurea lappa and has immunomodulatory effects. Isozaluzanin C improves tissue damage (lung, kidney, and liver) and excessive inflammation in mice induced by LPS (HY-D1056) or CRKP infection. Isozaluzanin C can be used in the study of bacterial infections and sepsi [1] .
Paquinimod-d5 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice[1] .
Oxolinic acid (Standard) is the analytical standard of Oxolinic acid. This product is intended for research and analytical applications. Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice[1] .
Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. [1] .
SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD +. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD + in mice[1] .
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity [1]. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice .
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats [1] .
L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1] .
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice[1].
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue [1].
S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism [1] .
VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice[1] .
NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser 70 and c-Myc at Thr 58 and Ser 62 through activation of both ERK1/2 and PKCα[1]. NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones [1].
AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia [1].
JPE-1375 is a complement C5a receptor 1(C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases [1].
Eritoran （E5564 free base） is a Toll-like receptor 4 (TLR4) antagonist. Eritoran protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran inhibits pathogenesis of filovirus infection. Eritoran has anti-inflammatory activity [1] .
MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease [1].
FC-11 is a Tubulin inhibitor that effectively inhibits tumor growth in mice. FC-11 can also induce endoplasmic reticulum (ER) stress to generate excess reactive oxygen species (ROS), leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-11 can be used in cancer research [1].
Cisd2 agonist 2 (compound 6) is an orally active Cisd2 activator (EC50=191 nM), while the Cisd2 levels is correlated with nonalcoholic fatty liver disease (NAFLD). Cisd2 agonist 2 has no significant toxicity in vivo in Cisd2hKO-het mice (heterozygous hepatocyte-specific Cisd2 knockout) [1].
BO-1 is a benzoate ester with antibacterial activity. BO-1 inhibits multidrug-resistant Staphylococcus aureus, and acts function synergistically with antibiotic, such as Ciprofloxacin (HY-B0356). BO-1 can reverse the resistance of antibiotic-resistant S. aureus strains, and decreases the level of inflammatory factors IL-6 and C-reactive protein in vivo in mice[1].
3-tert-Butyl-4-methoxyphenol is a PROTAC linker, belongs to alkyl/ether class, with insecticidal activity. 3-tert-Butyl-4-methoxyphenol also induced increased activities of glutathione (GSH) S-transferase and epoxide hydrolase in the liver and forestomach tissues of A/HeJ mice, regulating the carcinogen metabolism system [1] .
PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model [1].
NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM [1].
Fortunellin, is a flavonoid, that can be isolated from the fruits of Fortunella margarita (kumquat). Fortunellin exhibits little toxicity to mice and suppresses inflammation and ROS generation in H9C2 cells induced by LPS. Fortunellin protects against fructose-induced inflammation and oxidative stress by enhancing AMPK/Nrf2 pathway. Fortunellin can be used for diabetic cardiomyopathy research [1].
Paquinimod-d5-1 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice[1] .
γ-Glutamylvaline is an activator of CaSR with anti-inflammatory activity. γ-Glutamylvaline inhibits TNF-α-induced proinflammatory cytokine production and increases Wnt5a expression. γ-Glutamylvaline activates calcium-sensing receptor pathways in adipocytes of 3T3-L1mice and prevents low-grade chronic inflammation [1].
Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells [1].
MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1[1].
Meglumine (Methylglucamine) is an orally active amino sugar derived from sorbitol. Meglumine has anti-inflammatory and antitumor activity. Meglumine is often used as an excipient in active molecules and with iodinated compounds in contrast agents such as meglumine and meglumine iodide [1] .
7-aminocephalosporanic acid (7-ACA) is a HSP90β inhibitor and an antibiotic. 7-Aminocephalosporanic acid is the core chemical structure of the synthesis of cephalosporin antibiotics and an effective β-lactamase inhibitor [1] .
Rubusoside is a diterpene glycoside that is also a sweetener and solubilizer with anti-angiogenic, anti-cancer, anti-obesity, anti-allergic and anti-asthmatic effects. Rubusoside attenuates airway hyperresponsiveness and reduces inflammatory cells in bronchoalveolar lavage fluid (BALF), reducing OVA (HY-W250978)-induced airway inflammation. Rubusoside also prevents palmitic acid-induced lipotoxicity in pancreatic INS-1 cells, reduces the transport of human glucose transporters GLUT-1 and fructose GLUT-5, and inhibits NF-κB and α-amylase (α-amylase) [1] .
JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM) [1].JR-AB2-011 decreases the phosphorylation level of Akt, decreases MMP2 activity, thereby reducing the ability of tumor cells to migrate and invade. JR-AB2-011 also induces non-apoptotic cell death .
GIP (3-42), human acts as a glucose-dependent insulinotropic polypeptide (GIP) receptor antagonist, moderating the insulin secreting and metabolic actions of GIP in vivo [1].
AAA-10 is an orally active gut bacterial bile salt hydrolases (BSH) inhibitor, with IC50s of 10 nM, 80 nM against B. theta rBSH and B. longum rBSH respectively [1].
NF-κB/PON1-IN-1 (Compound 16) is a NF-κB/PON1 pathway inhibitor. NF-κB/PON1-IN-1 has antioxidant (IC50 = 45.76 µM) and hepatoprotective activities [1].
CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model [1].
SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy [1].
Renin inhibitor-1 (compound 26) is a potent and orally active renin inhibitor with IC50s of 0.9, 1.8 nM for rh-renin and hPRA, respectively. Renin inhibitor-1 shows antihypertensive efficacy. Renin inhibitor-1 has the potential for the research of hypertension and cardiovascular/renal diseases [1].
Anti-infective agent 4 (compound 73) is an orally active inhibitor of Trypanosoma cruzi with an IC50 value of 0.016 μM. Anti-infective agent 4 effectively reduces parasite burden in vivo. Anti-infective agent 4 can be used for the research of infection [1].
Bulaquine (CDRI 80/53) is a potent antimalarial agent which is an analogue of Primaquine (HY-12651A). Bulaquine affects multiple metabolism pathways and shows inhibition effect on Plasmodium cynomolgi infection. Bulaquine can be used for the research of malaria [1] .
Bofutrelvir (FB2001) is a SARS-CoV-2 main protease M pro inhibitor with an IC50 value of 53 nM and an EC50 value of 0.53 μM. Bofutrelvir exhibits potent antiviral efficacy against several current SARS-CoV-2 variants with EC50 values of 0.26-0.42 μM. Bofutrelvir has an additive antiviral effect when combined with Remdesivir (HY-104077) [1] .
Anti-IAV agent 1 (Compound (R)-1a) is an orally active anti-influenza A virus (IAV) agent with IC50s of 0.03 and 0.06 μM against IAV H1N1 and Oseltamivir-resistant IAV H1N1 strains, respectively [1].
FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4 WT, FGFR3, FGFR4 V550L, FGFR2 and FGFR1, respectively [1].
4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC50 value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity [1] .
PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) [1] .
PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) [1] .
Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) [1] .
Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) [1] .
CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells [1].
Tebanicline, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.
Antitumor agent-133 (compound 4d) is a bis-isatin derivative, with activities against Huh1 (IC50=17.13 μM) and Huh7 (IC50=8.27 μM). Antitumor agent-133 induces cell autophagy and inhibits tumor growth through regulation of LC3BII, ATG5 and p62 proteins [1].
ASCT2-IN-1 (compound 20k) is an ASCT2 inhibitor with IC50 values of 5.6 μM and 3.5 μM in cells A549 and HEK293, respectively. ASCT2-IN-1 induces cell apoptosis. ASCT2-IN-1 inhibits tumor growth [1].
Psychotridine is a natural alkaloid isolated from Psychotria colorata, reveals an analgesic activity in nervous system and an inhibitory efficacy towards platelet aggregation [1] .
Diacerein (Diacerhein), an orally active anthraquinone, reduces production of IL-1 converting enzyme then inhibits the activation of IL-1β by related downstream signaling. Diacerein is an anti-inflammatory and anti-rheumatic drug. Diacerein can relieve bronchospasm and control airway inflammation in asthmatic mice. Diacerein has the potential for slow acting drug in osteoarthritis (SYSADOA) research [1] .
PRE-084 hydrochloride is a highly selective σ1 receptor(S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway [1] .
Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders [1] .
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active [1] .
Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma [1] .
L-Glucose (L-(-)-Glucose) is a stereoisomer of D-Glucose (HY-B0389), which does not readily enter the brain. L-Glucose can promote food intake. L-glucose is combined with a fluorescence detector to produce a fluorescent probe that can be used to visualize and characterize cancer cells. L-Glucose also can be used in the research to enhance memory in mice[1] .
RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice[1].
ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice[1].
Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
Fmoc-leucine-d10 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
CYM2503 is a putative GalR2-positive allosteric modulator. CYM2503 increases the latency to first electrographic seizure and decreases the total time in seizure. CYM2503 also attenuates electroshock-induced seizures in mice. Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for the research of seizures and epilepsy [1].
Anti-inflammatory agent 22 (compound 14a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 22 inhibits LPS-induced TNF-α production with an IC50 value of 14.6 μM. Anti-inflammatory agent 22 has preventive effects on lymphedematous tissue via suppression of adipogenesis. Anti-inflammatory agent 22 suppresses limb lymphedema volume in mice[1].
Antibacterial agent 102 (compound 32) possesses potent in vitro and in vivo antibacterial activity, with MICs < 0.5 μg/mL in Staphylococcus aureus (S. aureus). Antibacterial agent 102 also moderately inhibits CYP3A4 with an IC50 value of 6.148 μM. Antibacterial agent 102 can reduce Methicillin-resistant Staphylococcus aureus (MRSA) load in thigh infected mice[1].
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM [1].
5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice[1].
Cabenoside D (compound 8) is a triterpenoid glycoside, which can be isolated from the methanol extract of lichen root. Cabenoside D shows anti-inflammatory activity and inhibits inflammation induced by 12-O-tetracylacyl hormone-13-acetate (TPA) in mice. Cabenoside D also inhibits TPA-induced Epstein-Barr virus (EBV) early antigen (EBV-EA) activation [1].
Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cell Apoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity Ki of 2.8 μM [1] .
Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab leads to muscle fiber hypertrophy and not hyperplasia in SCID mice. Stamulumab has the potential for Becker muscular dystrophy (BMD), facioscapulohumeral dystrophy (FSHD), and limb-girdle muscular dystrophy (LGMD) research [1] .
PRE-084 is a highly selective σ1 receptor(S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway [1] .
Anserine-d4 hydrochloride is the deuterium labeled Anserine (HY-113354). Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1] .
DH-376 is a potent diacylglycerol lipase inhibitor with pIC50 values of 8.6 and 8.9 for ABHD6 and DAGLα, respectively. DH-376 prevents fasting-induced refeeding of mice[1]. DH-376 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
BD-9136 is a highly selective BRD4 degrader. BD-9136 can inhibit tumor growth without adverse effects on mice. BD-9136 can be used for the research of cancer [1]. BD-9136 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
RASP-IN-1 (compound A) is a lipophili ccompound used for macular degeneration inhibition. RASP-IN-1 is biologically active in the retina of the rabbit's eye. Thirty minutes after IP treatment with 14C-RASP-IN-1 (10 mg/kg)，the Cmax amount of 14C-RASP-IN-1 in the posterior eye cup is 14.36 μg/g in mice model [1].
ERD-3111 (Compound 44) is an orally active PROTACERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer [1].
CD38 inhibitor 3 (compound 1) is a potent CD38 inhibitor (IC50=11 nM). CD38 inhibitor 3 can promote mitochondrial biogenesis, reduce lactate levels, and increase NAD+ content and Nrf2 expression. In a model of mitochondrial myopathy, CD38 inhibitor 3 increases muscle contraction/development and improves exercise tolerance in Pus1-/-mice[1].
(S)-4C3HPG ((S)-4-Carboxy-3-hydroxyphenylglycine) is an antagonist of metabotropic glutamate receptor 1a (mGluR 1a) and an agonist of GluR2. (S)-4C3HPG has the anticonvulsant activity and protects against audiogenic seizures in DBA/2 mice[1].
D359-0396 is an orally active NLRP3 inflammasome inhibitor. D359-0396 inhibits pyroptosis and IL-1β release in macrophages. D359-0396 also inhibits the oligomerization of NLRP3, ASC and the cleavage of GSDMD. D359-0396 alleviates EAE, and also improves survival after septic shock in mice[1].
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα H1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice[1].
Citric acid- 18O is 18O-labeled Citric acid (HY-N1428) Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice.
NKL 22 (compound 4b) is a potent and selective inhibitor of histone deacetylases (HDAC), with an IC50 of 199 and 69 nM for HDAC1 and HDAC3, respectively. NKL 22 exhibits selectivity over HDAC2/4/5/7/8 (IC50≥1.59 μM). NKL 22 ameliorates the disease phenotype and transcriptional abnormalities in Huntington's disease transgenic mice[1] .
T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα [1]. T0901317 activates FXR with an EC50 of 5 μM . T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively . T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice .
Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory [1].
Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation .
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice[1] .
TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1[1]. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques .
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) [1].
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice[1] .
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure [1] .
JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1(IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice[1]. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM .
U-69593 is a potent and selective κ1-opioid receptor agonist [1]. U-69593 attenuates addictive agent-induced behavioral sensitization in the rat . U-69593 reduces anxiety and enhances spontaneous alternation memory in mice . U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum .
ATX inhibitor 12 (compound 20) is an orally active and potent ATX (autotaxin) inhibitor, with an IC50 of 1.72 nM. ATX inhibitor 12 effectively alleviates lung structural damage with fewer fibrotic lesions at an oral dose of 60 mg/kg in C57Bl/6J mice. ATX inhibitor 12 can be uesd for idiopathic pulmonary fibrosis (IPF) research [1].
COX-2-IN-14 (compound 2a) is a potent and selective COX-2 (cyclooxygenase-2) inhibitor. COX-2-IN-14 shows effective binding at the active site of COX-2 co-crystal. COX-2-IN-14 exhibits a high level of in vivo anti-inflammatory activity, reducing ear edema and myeloperoxidase (MPO) activity in mice[1].
WWL123 analogue-1 is an analogue of WWL123. WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM [1] . WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice .
Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies [1].
Diprovocim-X (compound 35) is a potent TLR1/TLR2 (toll-like receptor 1/2) agonist, with EC50 values of 0.14 and 0.75 nM for hTLR1/TLR2 and mTLR1/TLR2, respectively. Diprovocim-X is a potent adjuvant in vivo in mice, and serves to stimulate the adaptive immune response [1].
PBI-6DNJ is an orally active and potent multivalent glycosidase inhibitor. PBI-6DNJ exhibits good inhibition activity against α-glucosidase from mice, with a Ki of 0.14 μM. PBI-6DNJ exhibits good hypoglycemic activity. PBI-6DNJ can be used for type 2 diabetes research [1].
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer [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].
(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice[1] .
HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research [1].
THR-β agonist 6 is an orally active, selective thyroid hormone receptor β (THR-β) agonist with EC50s of 0.03 μM and 0.22 μM for THR-β and THR-α, respectively. THR-β agonist 6 exhibits an xcellent liver-to-serum ratio of 93:1 in mice. THR-β agonist 6 has the potential for nonalcoholic steatohepatitis (NASH) research [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] .
(Rac)-Anemonin ((Rac)-Pulsatilla camphor) is the diastereoisomer of Anemonin (HY-N0278). Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases [1] .
JT002 is an orally active inhibitor of the NLRP3 inflammasome. JT002 reduces NLRP3-dependent proinflammatory cytokine (such as IL-1β, IL-1α, IL-18) production and pyroptosis. JT002 blocks NLRP3 inflammasome complex formation. JT002 reduces airway hyperresponsiveness and airway neutrophilia in mice[1].
RUNX-IN-2 (Compound Conjugate 3) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-2 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-2 inhibits tumor growth in PANC-1 xenograft mice. RUNX-IN-2 has high alkylation efficiency and specificity [1].
XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model [1].
ZHSI-1 is an EV71 (Enterovirus 71) inhibitor that inhibits EV71/CVA16 replication and virus-induced pyroptosis associated with viral pathogenesis. ZHSI-1 effectively prevents EV71 infection in neonatal and young mice in animal models. ZHSI-1 can be used to study viral infections such as hand, foot and mouth disease (HFMD) [1].
9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation. 9-PAHSA also improved carotid vascular calcification and attenuates cardiac hypertrophy and dysfunction in db/db mice. 9-PAHSA increases the viability of steatosis primary mouse hepatocytes (PMH). 9-PAHSA can be used in research on diabetes, inflammation, and cardiovascular disease [1] .
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model [1].
KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice[1] .
Eritoran tetrasodium (E5564) is a Toll-like receptor 4 (TLR4) antagonist. Eritoran tetrasodium protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran tetrasodium decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran tetrasodium inhibits pathogenesis of filovirus infection. Eritoran tetrasodium has anti-inflammatory activity [1] .
Citric acid-d4-1 is deuterated labeled Citric acid (HY-N1428) Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice.
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity [1]. MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
8-prenylnaringenin is a prenylflavonoid isolated from hop cones Humulus lupulus, with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice[1] .
Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction [1] .
(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice[1].
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice[1] .
Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) [1].
AP39 is a triphenylphosphonium derivatised anethole dithiolethione and mitochondria-targeting hydrogen sulfide (H2S) donor. AP39 increases intracellular H2S levels. AP39 exerts cytoprotective effects and maintains mitochondrial DNA integrity under oxidative stress conditions. AP39 protects against myocardial reperfusion injury in mice model and has the potential for Alzheimer's disease research [1] .
CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. CA77.1 is a derivative of AR7 (HY-101106) and can increase the expression of the lysosomal receptor LAMP2A in lysosomes. CA77.1 improves behavior and neuropathology in PS19 mice model and can be used for alzheimer's disease research [1].
TTBK1-IN-2 (compound 29) is a potent Tau-Tubulin kinase (TTBK1) inhibitor with IC50s of 0.24 and 4.22 µM, respectively. TTBK1-IN-2 reveals good brain penetration in vivo and is able to reduce TDP-43 phosphorylation not only in cell cultures but also in the spinal cord of transgenic TDP-43 mice[1].
Ethacrynic acid (Etacrynic acid sodium) sodium is a diuretic. Ethacrynic acid sodium is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid sodium is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid sodium also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid sodium has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice[1] .
MAO-B-IN-21 is an excellent MAO-B inhibitor with antioxidant activity and anti-Aβ aggregation activity. MAO-B-IN-21 also exhibits metal-ion chelating ability, anti-neuroinflammation (NO, TNF-α), neuroprotective activity and BBB permeability. MAO-B-IN-21 significantly improves the memory and cognitive impairment in Aβ1-42 induced Alzheimer's disease mice model [1].
JAK1-IN-12 is a selective inhibitor of JAK1, with IC50 of 0.0246 μM. And IC50s of 0.423 μM, 0.410 μM and 1.12 μM for JAK2, JAK3 and TYK2. JAK1-IN-12 promotes hair growth in mice. JAK1-IN-12 can be used for research of immune and inflammatory diseases [1].
Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM) [1] .
S-Propargylcysteine (SPRC), a structural analog of S-allyl cysteine (SAC), is a slow H2S-releasing compound. S-Propargylcysteine reduces Ca 2+ accumulation and inflammatory cytokines, inhibits STAT3, and elevates p53 and Bax. S-Propargylcysteine has anti-inflammatory activity and protects mice against acute pancreatitis. S-Propargylcysteine also has cardioprotective, neuroprotective acitivties [1] .
AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy [1].
CL4F8-6 is an ionizable cationic lipid with a pKa of 6.14. CL4F8-6 can be used in lipid nanoparticles (LNPs)-based mRNA therapeutics. CL4F8-6 LNPs carrying Cas9 mRNA and sgRNA could induce CRISPR-mediated gene knockdown in mice[1].
iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR) [1].
GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma [1] .
Lalistat 2 is an inhibitor of many lipases especially Lysosomal acid lipase (LAL, IC50 = 152 nM), which is a key enzyme that degrades neutral lipids at an acidic pH in lysosomes. Lalistat 2 is commonly used to investigate the cell-specific functions of LAL and LAL deficiency in vitro, as well as specifically measure LAL activity in human blood samples or cells [1] .
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities [1] .
Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research [1] .
DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone is orally active against HMGCR mutation and statin caused myopathy . DL-Mevalonolactone induces inflammation and oxidative stress response with decreased mitochondrial membrane potential (MMP) and induces mitochondrial swelling [2][4].
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis[1] .
S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 induces autophagy and inhibits QR2-mediated ROS production [1].
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively [1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy .
Thymidine 3',5'-disphosphate (Deoxythymidine 3′,5′-diphosphate; pdTp) is a selective small molecule inhibitor of staphylococcal nuclease and tudor domain containing 1(SND1, the miRNA regulatory complex RISC subunit) and inhibits SND1 activity. Thymidine 3',5'-disphosphate exhibits anti-tumor efficacy in vivo[1].
S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes [1] .
AAA-10 formic is an orally active gut bacterial bile salt hydrolases (BSH) inhibitor, with IC50s of 10 nM, 80 nM against B. theta rBSH and B. longum rBSH, respectively [1].
(+)-Butin is the R enantiomer of Butin. Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities [1].
Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is a histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect [1].
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant [1].
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer [1].
Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19 [1] .
Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway [1].
CRK12-IN-2 (compound 2) is an inhibitor of CRK12. CRK12-IN-2 shows potency against Trypanosoma congolense and Trypanosoma vivax with EC50 values of 3.2 and 0.08 nM. CRK12-IN-2 can be used for the research of animal trypanosomiasis [1].
Anti-infective agent 5 (compound 74) is an orally active inhibitor of Trypanosoma cruzi with an IC50 value of 0.10 μM. Anti-infective agent 5 effectively reduces parasite burden in vivo. Anti-infective agent 5 can be used for the research of infection [1].
Naproxcinod (Nitronaproxen) is the first in class of cyclooxygenase (COX)-inhibiting nitric oxide donators (CINODs). Naproxcinod shows analgesic and anti-inflammatory effects, it can be used for the research of osteoarthritis and inflammation [1] .
ALM301 is an orally active highly specific AKT inhibitor with IC50 values of 0.13 µM, 0.09 µM and 2.75 µM for AKT1, AKT2 and AKT3, respectively. ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro. ALM301 can inhibit cancer cell proliferation and tumor growth [1].
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model [1]. RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease [1].
Mavodelpar (REN001) is a selective PPARδ agonist. Mavodelpar suppresses glomerular injury and renal fibrosis. Mavodelpar can be used for the research of primary mitochondrial myopathies (PMM) and long-chain fatty acid oxidation disorders (LC-FAOD) [1]. Mavodelpar is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
AA-T3A-C12 is an anisamide ligand-tethered lipidoid (AA-lipidoid). AA-T3A-C12 mediates great RNA delivery and transfection of activated fibroblasts [1].
Thymidine 3',5'-diphosphate (Deoxythymidine 3′,5′-diphosphate) tetrasodium is a selective inhibitor of staphylococcal nuclease and tudor domain containing 1(SND1, the MicroRNA regulatory complex RISC subunit) and [3,5- 2H2] tyrosyl nuclease. Thymidine 3',5'-diphosphate tetrasodium has anti-tumor activity and can also be used as a catalyst in biochemical reactions [1] .
LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM [1] .
Z21090 (ZL40) is a potent inhibitor of PDE4 with the IC50 value of 37.4 nM and oral bioavailability. Z21090 plays an important role in alcohol-related diseases research [1].
ST-148 maleate is a potent and orally active DENV inhibitor. ST-148 maleate shows antiviral efficacy and low cell toxicity. ST-148 alters the interaction between lipid droplets and the C protein, thereby inhibiting viral replication. [1].
BN-82685 is a a quinone-based CDC25 inhibitor with IC50 of 201 nM, 117 nM, 109 nM, 160 nM, 249 nM, for CDC25C, CDC25C-cat, CDC25A, CDC25B2, CDC25B3, respectively. BN-82685 plays an important role in cancer research [1].
Anguinomycin A is an antibiotic that exhibits good inhibitory activity against G. boninense with an MIC value of 5 µg/disk. Anguinomycin A has antitumor activity [1] .
Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice[1] .
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys [1] .
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves [1].
Deacetylasperulosidic acid (DAA) is a major phytochemical constituent of Morinda citrifolia fruit. Deacetylasperulosidic acidhas antioxidant activity by increasing superoxide dismutase activity. Deacetylasperulosidic acid has anticlastogenic activity, suppressing the induction of chromosome aberrations in hamster ovary cells and mice[1]. Deacetylasperulosidic acid prevents 4-nitroquinoline 1-oxide (4NQO) induced DNA damage in vitro, suppresses IL-2 production along with the activation of natural killer cells .
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses [1] .
Azemiglitazone potassium (MSDC-0602K), a PPARγ-sparing thiazolidinedione (Ps-TZD), binds to PPARγ with the IC50 of 18.25 μM [1]. Azemiglitazone potassium modulates the mitochondrial pyruvate carrier (MPC). Azemiglitazone potassium can be used for the research of fatty liver including dysfunctional lipid metabolism, inflammation, and insulin resistance . Azemiglitazone potassium, an insulin sensitizer, improves insulinemia and fatty liver disease in mice, alone and in combination with Liraglutide .
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].
γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC50 of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice[1].
YW1128 (compound 3a) is a potent Wnt/β-Catenin inhibitor. YW1128 induces the proteasome degradation of β-catenin and subsequent inhibits the Wnt/β-catenin signaling in cells. YW1128 significantly decreases hepatic lipid accumulation. YW1128 improves glucose tolerance of high fat diet-fed mice without noticeable toxicity. YW1128 down regulates the genes involved in the glucose and fatty acid anabolism [1].
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction [1] .
Suvratoxumab (MEDI4893) is a long-acting, high-affinity human anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) [1] .
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability [1].
HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and ＞100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension [1].
(S)-CCG-1423 is an inhibitor of Rho signaling that blocks the nuclear import of MRTF-A. (S)-CCG-1423 reduces the nuclear accumulation of MRTF-A and improves glucose uptake and tolerance in insulin-resistance mice in vivo. (S)-CCG-1423 exhibits higher inhibition activity than the SR- and the R-isomers of CCG-1423 (HY-13991). (S)-CCG-1423 can be used for the research of cancer and diabetes [1].
2,7"-Phloroglucinol-6,6'-bieckol is an orally active dual α-amylase/α-glucosidase inhibitor with IC50 values of 6.94 μM and 23.35 μM respectively. 2,7"-Phloroglucinol-6, 6'-bieckol alleviates postprandial hyperglycemia in diabetic mice. 2,7"-Phloroglucinol-6,6'-bieckol can be used in diabetes research [1].
MorHap is a heroin hapten. MorHap conjugated to tetanus toxoid (TT), palm-CV2, and to monophosphoryl lipid A (MPLA)-containing liposomes partially blocks heroin-induced analgesia and hyperlocomotion in mice. MorHap designed conjugates also significantly inhibits HIV-1 binding to α4β7 receptors. MorHap can be used in research to develop vaccines related to heroin addiction and HIV-1 infection [1].
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 [1].
TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation [1] .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats [1] .
Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively [1]. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research [1] .
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a [1].
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 [1]. (Z)-Ligustilide inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans[1] .
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice[1] .
Medroxyprogesterone (17α-Hydroxy-6α-methylprogesterone) is a synthetic human variant of progesterone that is a progesterone receptor agonist with oral activity. Medroxyprogesterone can induce cell proliferation through the PI3K/Akt signaling pathway. Medroxyprogesterone has an inhibitory effect on atherosclerosis in mice. The progesterone agonist activity of Medroxyprogesterone is less effective than Medroxyprogesterone acetate (HY-B0469) [1] .
PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice[1] .
EGCG Octaacetate (AcEGCG) is a proagent of Green tea epigallocatechin-3-gallate (EGCG). EGCG Octaacetate decreases the proinflammatory mediator levels by down-regulating of PI3K/Akt/NFκB phosphorylation and p65 acetylation. EGCG Octaacetate reduces colitis-driven colon cancer in mice. EGCG octaacetate is the potential antibacterial compound for gram-positive bacteria (GPB) and gram-negative bacteria (GNB) [1] .
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer [1].
4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic agent. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mouse brain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice[1].
TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion [1] .
Cuprizone is a copper chelating agent that forms a deep blue copper ketone complex with copper (II). The copper ketone reaction can be used in colorimetric tests for the presence of trace copper. Cuprizone can be used to induce some schizophrenia-like behavior in mice. Cuprizone acts on copper enzymes, including SOD1, cytochrome oxidase, and DβH, thereby causing oxidative stress and increasing DA levels in certain brain regions such as the medial prefrontal cortex (PFC) [1].
BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research [1] .
Relatlimab (BMS-986016) is a human monoclonal antibody anti-LAG-3 antibody generated by immunization of transgenic mice bearing human immunoglobulin miniloci with recombinant LAG-3 protein. Relatlimab blocks LAG-3/MHC II interaction with an IC50 value of 0.67 nM and LAG-3/FGL1 interaction with an IC50 value of 0.019 nM. Relatlimab can be used in research of cancer [1].
Antitumor agent-81 (compound 5a) is a low cytotoxic P62-RNF168 agonist that promotes the interaction of P62 with RNF168. Antitumor agent-81 induces a decrease in RNF168-mediated H2A ubiquitination and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits mice xenograft tumor growth in a dose-dependent manner [1].
Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses [1] .
ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2 V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia [1].
(E/Z)-Locostatin ((E/Z)-UIC-1005) is a racemic of Locostatin. Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice[1] .
Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice[1] .
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice). ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 also shows good plasma exposure levels [1].
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice[1] .
NF-κB-IN-9 is a nuclear factor kappa B (NF-κB) targeting sonosensitizer (λex/λem=489/628 nm). NF-κB-IN-9 exhibits strong inhibition on NF-κB signaling due to its two resveratrol units in one molecule. NF-κB-IN-9 has anti-tumor activity and shows remarkable sonocytotoxicity against cancer cells. NF-κB-IN-9 has biosafety in eenograft mice model.
AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). AMPA receptor modulator-4 can cross the blood-brain barrier. AMPA receptor modulator-4 increases the cognition performance and improves working memory performance in mice[1].
UBP141 is a GluN2C/2D (NR2C/2D)-preferring receptor antagonist, with Kds of 2.8, 4.2, 14.2, and 19.3 μM for NMDA receptor subtypes: GluN2C, 2D, 2A, and 2B, respectively. UBP141 can induce potent motor impairment in WT mice[1] .
Israpafant (Y-24180) is a potent, selective and long-acting platelet activation factor (PAF) receptor antagonist with IC50s of 0.84 nM and 3.84 nM against PAF-induced human and rabbit platelet aggregation, respectively. Israpafant stimulates both extracellular Ca 2+ influx and intracellular Ca 2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice[1] .
CBP/p300-IN-21 (Compound 5d) is a selective CBP/p300 inhibitor (IC50: 0.07 and 1.755 μM for p300 and CBP). CBP/p300-IN-21 decreases H3K18Ac level. CBP/p300-IN-21 inhibits growth of 4T1 tumor growth in mice[1].
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits migration and invasion of A549 cells by reversing EMT, and induces cell apoptosis and autophagy. Sotetsuflavone inhibits HIF-1α, VEGF, angiostatin, MMP-9, and MMP-13 expression in A549 cells. Sotetsuflavone also protects mice against Crohn's disease (CD)-like colitis. Sotetsuflavone can be used for research of NSCLC [1] .
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC50=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research [1].
Brassinolide-d5 (Brassin lactone-d5) is the deuterated labeled Brassinolide (HY-N0273). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[1] .
Menthofuran- 13C2 is 13C labeled Menthol (HY-N1369). Menthol is an analgesic and TRPM8 modulator. TRPM8 is a cold temperature sensing ion channel, and Menthol can regulate TRPM8 to exert analgesic and anti-irritation mechanisms. Menthol stimulates cold receptors and produces a cooling sensation by inhibiting Ca ++ currents in neuronal cell membranes. Menthol also improves oral nicotine rejection in mice[1] .
Pro-905 is a phosphite peptide with antitumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to the tumor. Pro-905 effectively prevents incorporation of purine salvage substrates into nucleic acids and inhibits colony formation in human malignant peripheral nerve sheath tumors (MPNST) cells. Pro-905 inhibits purine salvage incorporation to nucleic acids and prevents cell growth. Pro-905 inhibits the growth of MPNST and enhances the anti-tumor efficacy of JHU395 (HY-124778) [1].
8-Hydroxyquinoline (8-Quinolinol) is a lipophilic metal chelator that can be used as a fungicide .8-Hydroxyquinoline shows the MIC range of 27.56-55.11 μM (4-8 μg/mL) against the clinical isolates of Neisseria gonorrhoeae. 8-Hydroxyquinoline can bind to copper form complexes and transport copper into cells. 8-Hydroxyquinoline increases in the number of micronucleated polychromatic erythrocytes and can also make hair depigmented in mice[1] .
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model [1]. EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells [1] .
MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice[1].
Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole-d3 is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1][2][3][4].
Forsythiaside A is an orally active phenylethanoid glycoside isolated from the dried fruits of Forsythia suspensa. Forsythiaside A is also an inhibitor of COX-2 and has anti-inflammatory, antioxidant and neuroprotective effects. Forsythiaside A prevents neuroinflammation and apoptosis caused by Aβ25-35 damage and may be used in Alzheimer's disease (AD) research. Forsythiaside A also activates the Nrf2/HO-1 signaling pathway and inhibits OVA-induced asthma in mice[1] .
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance [1].
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats [1] .
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM) [1]. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse . GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice .
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM [1] .
Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease [1]. Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD) . Omigapil (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance [1].
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells [1] .
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains [1] .
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles [1] .
CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice[1].
Yhhu-3792 enhances the self-renewal capability of neural stem cells (NSCs). Yhhu-3792 activates Notch signaling pathway and promotes the expression of Hes3 and Hes5. Yhhu-3792 expands the NSCs pool and promotes endogenous neurogenesis in the hippocampal dentate gyrus (DG) in mouse. Yhhu-3792 increases the spatial and episodic memory abilities of mice. Yhhu-3792 has the potential for the research of impairment of learning and memory associated DG dysfunction [1].
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer [1].
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity [1].
JZP-MA-11 is a positron emission tomography (PET) ligand targeting the endocannabinoid α/β-hydrolase domain 6 (ABHD6) enzyme. JZP-MA-11 selectively inhibits ABHD6 with an IC50 value of 126 nM. JZP-MA-11 can cross the blood-brain barrier (BBB). [18F]JZP-MA-11 has the potential for preclinical evaluation targeting the brain ABHD6 in mice and nonhuman primate (NHP) [1].
AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice. AR-C118925XX also inhibits ATP-induced tumor growth [1] .
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research [1].
BAY-747 is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model [1] .
MPP is a highly selective estrogen receptor alpha (ERα) antagonist. MPP reduces the ratio of p-ERα/ERα [1].
https://www.ncbi.nlm.nih.gov/pubmed/29799481
Labouesse MA, et al. Effects of selective estrogen receptor alpha and beta modulators on prepulse inhibition in male mice. Psychopharmacology (Berl). 2015 Aug;232(16):2981-94.
https://www.ncbi.nlm.nih.gov/pubmed/25893642
FR173657 is an orally active bradykinin B2 receptor antagonist (IC50: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease [1].
GK444 (Compound 15a) is a HDAC1/2 inhibitor (IC50: 100 and 92 nM for HDAC1/2 respectively). GK444 inhibits Caco-2 cells with IC50 of 4.1 μM. GK444 also reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts. GK444 inhibits Bleomycin (HY-108345)-induced lung fibrosis in mice[1].
SAR127303 is an orally active, selective, competitive monoacylglycerol lipase (MAGL) covalent inhibitor with IC50s of 3.8 nM and 29 nM for mouse and human MAGL, respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis [1].
FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice[1].
Yhhu-3792 hydrochloride enhances the self-renewal capability of neural stem cells (NSCs). Yhhu-3792 hydrochloride activates Notch signaling pathway and promotes the expression of Hes3 and Hes5. Yhhu-3792 hydrochloride expands the NSCs pool and promotes endogenous neurogenesis in the hippocampal dentate gyrus (DG) in mouse. Yhhu-3792 hydrochloride increases the spatial and episodic memory abilities of mice. Yhhu-3792 hydrochloride has the potential for the research of impairment of learning and memory associated DG dysfunction [1].
Ethacrynic acid (Standard) is the analytical standard of Ethacrynic acid. This product is intended for research and analytical applications. Ethacrynic acid (Etacrynic acid) is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice[1] .
SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC50 of 33 nM. SE-7552 is greater than 850-fold selectivity versus all other known HDAC isozymes. SE-7552 is capable of blocking multiple myeloma growth in vivo. SE-7552 acts as an anti-obesity agent in diet-induced obese mice[1] .
Angiotensin I- 13C5, 15N (human, mouse, rat) is the 13C and 15N labeled Angiotensin I (human, mouse, rat) (HY-P1032). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[1].
Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection [1] .
Nitrofurazone (Nitrofural) is a broad spectrum antibiotic that has oral activity. Nitrofurazone is a nitro-aromatic drug. Nitrofurazone is active against both Gram-positive and Gram-negative bacteria [1] .
L-Glutamic acid monosodium salt is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid monosodium salt has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid monosodium salt can be used in the study of neurological diseases [1] .
L-Glutamic acid is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid can be used in the study of neurological diseases [1] .
L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer [1] .
RR-11a is a synthetic enzyme inhibitor of Legumain (IC50=31-55 nM). RR-11a can be used for the research of cancer and acute myocardial infarction (AMI) [1] .
AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1[1].
Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression [1].
Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research [1].
Azemiglitazone (MSDC-0602) is an orally active thiazolidinedione (TZD) -like molecule, which binds to PPARγ with low binding and activating affinity. Azemiglitazone inhibits mitochondrial pyruvate carrier (MPC), which inhibits Alzheimer’s disease and diminishes nonalcoholic steatohepatitis (NASH) caused liver injury .
ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1). ELQ-300 inhibits growth of P. falciparum Dd2, Tm90-C2B, and D1 with IC50 values of 6.6, 4.6 and 160 nM, respectively. ELQ-300 can be used for the research of antimalarial [1] .
Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research [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] .
Melanin probe-1 is an 18F-picolinamides based PET probe. Melanin probe-1 can be used for PET imaging of malignant melanoma. Melanin probe-1 exhibits high tumor targeting efficiency, excellent tumor imaging contrasts, desirable biodistribution patterns, and good in vivo stability [1].
FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1(FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity [1].
ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1[1] .
AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39) [1].
PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity [1].
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML [1].
PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain [1].
Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca 2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca 2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca 2+ signaling in neuronal and nonneuronal cells [1] .
Ompenaclid (RGX-202) is an oral small-molecule SLC6A8 transporter inhibitor. Ompenaclid robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. Ompenaclid can be used for the research of cancer and duchenne muscular dystrophy [1] .
CRK12-IN-1 is a potent CRK12 inhibitor. CRK12-IN-1 is extremely potent against T.b. brucei and rapidly cytocidal, as well as equally potent against T. congolense and T. vivax (EC50 of 1.3 and 18 nM, respectively) [1].
Methyl isoeugenol (MIE) is a natural food flavour that can be isolated from Pimenta pseudocaryophyllus leaf. Methyl isoeugenol shows anxiolytic and antidepressant like effects. Methyl isoeugenol is orally active [1].
AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC50 of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro [1].
Zalutumumab is a high affinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC50s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer [1] .
hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy [1].
5-AIQ (5-Aminoisoquinolin-1-one) is a water-soluble PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver [1] .
Dehydrothio-p-toluidine (DHPT) is a chemical intermediate used in dyestuff production. Dehydrothio-p-toluidine shows inhalation toxicity in acute and subchronic conditions [1].
M4K2234 (compound 26b) is an ALK2 inhibitor. M4K2234 inhibits ALK2 and ALK5 with IC50s of 5 and 2144 nM, respectively. M4K2234 can be used as a chemical probe for ALK1 and ALK2 protein kinases. M4K2234 can be used for the research of cancer [1].
SARS-CoV-2 Mpro-IN-4 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 900 nM and 60 nM respectively. SARS-CoV-2 Mpro-IN-4 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-4 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 8.2 nM [1].
SARS-CoV-2 Mpro-IN-5 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM [1].
SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer [1].
SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL) [1].
KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis[1].
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively [1].
Andecaliximab is a recombinant chimeric IgG4 monoclonal antibody (mAb) targets matrix metalloproteinase 9 (MMP9). Andecaliximab shows the antifibrotic efficacy in idiopathic pulmonary fibrosis mouse models. Andecaliximab can be used for the research of gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF) [1] .
JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer [1].
α-Synuclein inhibitor 8 is an active inhibitor of α-Synuclein with an IC50 value of 2.5 µM. α-Synuclein inhibitor 8 has highly inhibition on the aggregation and disaggregation of α-Synuclein fibers. α-Synuclein inhibitor 8 reduces the formation of inclusions in neurons that can repairs damage neurons and improves Parkinson’s disease (PD)-like symptoms. α-Synuclein inhibitor 8 has high antioxidant activity and low cytotoxicity [1].
YM543 free base is a potent and orally active sodium-glucose cotransporter (SGLT) 2 inhibitor. YM543 free base reduces blood glucose levels. YM543 free base can be used in research of diabetes [1] .
L-Octanoylcarnitine hydrochloride is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine hydrochloride can be used for the research of breast cancer [1] .
Keliximab (SB-210396) is a chimeric human/macaque IgG1anti-CD4 monoclonal antibody with a Ki value of 1.0 nM for soluble CD4. Keliximab blocks T cell proliferation and inhibits IL-2 production. Keliximab can be used for cancer research [1] .
Crizanlizumab is an anti-P-selectin monoclonal antibody. Crizanlizumab binds to P-selectin and blocks its interaction with P-selectin glycoprotein ligand 1 (PSGL-1). Crizanlizumab prevents vaso-occlusive crises (VOCs) and can be used for research of sickle cell disease [1] .
Anti-hepatic fibrosis agent 2 (Compound 6k) is an orally active COL1A1 inhibitor. Anti-hepatic fibrosis agent 2 is an anti-fibrogenic agent targeting ewing sarcoma breakpoint region 1 (EWSR1) [1].
LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway [1].
PROTAC CDK9/CycT1Degrader-1 (compounds 10) is a potent inhibitor of CDK9. PROTAC CDK9/CycT1Degrader-1 can be used as a PROTAC target protein ligand for PROTAC synthesis. PROTAC CDK9/CycT1Degrader-1 shows strong anti-proliferative activity in solid tumors [1].
L-Octanoylcarnitine-d3 is the deuterium-labeled L-Octanoylcarnitine (HY-113161). L-Octanoylcarnitine-d3 is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine-d3 can be used for the research of breast cancer [1] .
Pancreatic lipase-IN-2 (compound 7r) is a potent inhibitor of pancreatic lipase (PL), with the IC50 value of 2.67 μM, that has anti-obesity effect [1].
5-LO/mPGES1-IN-1 (Compound 16) is a dual inhibitor of microsomal prostaglandin E2 synthase-1(mPGES-1) and 5-lipoxygenase (5-LO). IC50 values are 0.3 and 0.4 μM, respectively. 5-LO/mPGES1-IN-1 has anti-inflammatory activity [1].
Cbz-Gly-Pro-Ala-O-cinnamyl (compound 25) is a small peptide targeting BACE-1 and AChE with the IC50 values of 0.02 μM and 1 μM, respectively. Cbz-Gly-Pro-Ala-O-cinnamyl shows neuroprotective effect and can be used for study of Alzheimer’s disease [1].
Elamipretide TFA (MTP-131 TFA; RX-31 TFA; SS-31 TFA) is the TFA salt form of Elamipretide (HY-P0125). Elamipretide TFA is a mitochondria-targeting peptide, which ameliorates myocardial infarction, improves the renal function and protects neurons form inflammatory and oxidative stress injury [1] .
Suprafenacine is a cell permeable, tubulin-destabilizing molecule which bind microtubules at the colchicine-binding site and inhibit polymerization. Suprafenacine can induce G2/M cell cycle arrest and apoptosis, and can be used for cancer research [1].
URAT1 inhibitor 10 (Compound 23a) is a URAT1 inhibitor. URAT1 inhibitor 10 has oral efficacy and low cytotoxicity. URAT1 inhibitor 10 has high selectivity for OAT1[1].
Napyradiomycin B4 is a Napyradiomycin derivative, which inhibits the RANKL-induced MEK-ERK signaling pathway. Napyradiomycin B4 attenuates osteoclastogenesis and prevents alveolar bone destruction in experimental periodontitis [1].
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1(LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice[1].
DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice[1].
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease [1].
Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice[1]. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
C30(ω-hydroxy) Ceramide (d18:1/30:0), a sphingolipid, is an epidermis-specifically vital component of the water barrier in mammalian skin. C30(ω-hydroxy) Ceramide (d18:1/30:0) is expressed in epidermal keratinocytes and male germ cells during their differentiation and maturation. C30(ω-hydroxy) Ceramide (d18:1/30:0) deficiency in the epiderm of Elovl4 deletion or mutation mice[1] .
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight [1].
5-{8-[(3,4'- difluoro [1,1'- biphenyl]-4-yl) methoxy] - 2-methylimidazo [1,2-a] pyridin-3-yl}-n-methylpyridin-2-formamide (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome [1].
Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts [1].
Firivumab (CT-P22; CT120) is a human IgG1 monoclonal influenza A virus hemagglutinin (Anti-IAV HA) antibody. Firivumab is capable of neutralizing H1N1, H5N1, H6N1, H6N2, H8N4, H8N8, H9N2 and H12N7. Firivumab shows protection against H1N1 virus in mice[1] .
NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprotective activity. NMDAR/TRPM4-IN-2 prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss [1].
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries [1].
5-Heptadecylresorcinol (AR-C17), a phenolic lipid component, is also an orally active mitochondrial protector. 5-Heptadecylresorcinol improves mitochondrial function via sirtuin3 signaling pathway, thus alleviates endothelial cell damage and apoptosis. 5-Heptadecylresorcinol induces sirtuin3-mediated autophagy. 5-Heptadecylresorcinol reduces the atherosclerotic plaques in the aortic root region of mice heart. 5-Heptadecylresorcinol can be used for research of atherosclerosis prevention and obesity [1] .
E1231 is an orally active activator of Sirtuin 1(SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/-mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases [1].
E6446 dihydrochloride is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 dihydrochloride is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 dihydrochloride also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD) [1] .
DNL343 is a brain-penetrating activator of eukaryotic initiation factor 2B (eIF2B) that inhibits the abnormal integrated stress response (ISR). DNL343 inhibits ISR activity in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 has inhibitory potential in studies of vanishing white matter disease (VWMD) driven by eIF2B LOF and chronic ISR activation [1].
Chemerin-9, mouse (Chemerin148-156, mouse) is a C-terminal nonapeptide of chemerin. Chemerin-9, mouse is a ligand for ChemR23 (EC50 = 42 nM). Chemerin-9, mouse reduces basal lipolysis in primary mouse white adipocytes(IC50 = 3.3 nM). Chemerin-9, mouse enhances memory and relieves Aβ1-42-induced memory impairment in AD mice. Chemerin-9, mouse also inhibits atherogenesis [1] .
E6446 is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD) [1] .
PAT1inh-A0030 is a selective PAT1 (SLC26A6) inhibitor (IC50= 1.0 μM). PAT1inh-A0030 inhibits fluid absorption in the ileum of wild-type and cystic fibrosis (CF) mice (CftrdelF508/delF508) in a closed-loop model of intestinal fluid absorption. PAT1inh-A0030 can be used in the study of intestinal diseases related to CF [1].
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice[1] .
YK-4-279 blocks RNA Helicase A (RHA) binding with EWS-FLI1 (oncogenic protein). YK-4-279 induces apoptosis and shows anti-proliferation activities towards various cancer cells. YK-4-279 has a chiral center and it can be separated into two enantiomers. YK-4-279 can be used for the research of cancer [1] .
(E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer [1] .
Cefozopran (SCE-2787) is a semi-synthetic, parenteral, fourth-generation cephalosporin. Cefozopran, an antibiotic, has a broad spectrum of antibacterial activity, inhibiting most of the gram-negative and gram-positive organisms [1] .
Cefozopran (SCE-2787) hydrochloride is a semi-synthetic, parenteral, fourth-generation cephalosporin. Cefozopran hydrochloride, an antibiotic, has a broad spectrum of antibacterial activity, inhibiting most of the gram-negative and gram-positive organisms [1] .
Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity [1] .
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10 [1] .
Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity [1].
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues [1]. PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity [1].
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity [1].
PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer [1].
HE-S2 is an antibody-drug conjugate triggering a potent antitumor immune response. HE-S2 acts by blocking the PD-1/PD-L1 interaction and activating the Toll-like receptor 7/8 (TLR7/8) signaling pathway. HE-S2 has remarkable antitumor activity [1].
KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC50s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo [1].
DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.040, 0.15, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. DS17701585 can be used for cancer research [1].
DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
ZC0101 is a potent, orally active IDO1 and TrxR dual inhibitor with IC50 values of 0.084 μM and 7.98 μM, respectively. ZC0101 effectively induces apoptosis and ROS accumulation in cancer cells [1].
GB83 is a potent PAR2 antagonist. GB83 reverses neutrophil elastase‐induced synovitis and pain. GB83 blocks the effect of MET-1 supernatant on NG neurons [1].
AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer [1].
3'-Sialyllactose (3'-SL) is a prebiotic, maintains immune homeostasis and exerts anti-inflammatory and anti-arthritic effects. 3'-Sialyllactose is an ordinary carbohydrate with the lowest toxicity rating, it can be used for the research of inflammation [1] .
TA-1887 (JNJ-39933673) is a highly potent, selective and orally active SGLT2 inhibitor (IC50: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes [1] .
Teplizumab (MGA-031) is a Fc receptor non-binding anti-human CD3 monoclonal antibody. Teplizumab reduces the loss of beta-cell function. Teplizumab can be used in the research of type 1 diabetes [1] .
Zorubicin (Rubidazon) is a derivative of Daunorubicin (HY-13062A). Zorubicin interacts with topoisomerase II and inhibits DNA polymerases. Zorubicin can be used for the research of acute leukemias and sarcomas [1] .
3'-Sialyllactose (3'-SL) sodium is a prebiotic, maintains immune homeostasis and exerts anti-inflammatory and anti-arthritic effects. 3'-Sialyllactose sodium is an ordinary carbohydrate with the lowest toxicity rating, it can be used for the research of inflammation [1] .
LY5 is a STAT3 inhibitor with an IC50 value of 0.5 μM. LY5 induces apoptosis and inhibits STAT3 phosphorylation. LY5 shows antitumor activity in vivo, it can be used for the research of cancer [1].
ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti-mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner [1].
Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia [1].
HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis [1].
c-Met-IN-22 (compound 51am) is an orally active inhibitor against c-Met with an IC50 value of 2.54 nM. c-Met-IN-22 has antiproliferative and antitumor activities. c-Met-IN-22 induces cell apoptosis[1].
Tubulin inhibitor 40 (compound 45) is a tubulin inhibitor with IC50 of 1.2 μM. Tubulin inhibitor 40 shows selective cytotoxicity towards cancer cells. Tubulin inhibitor 40 processes antitumor activity [1].
Valnemulin is an orally active broad-spectrum antibiotic against Gram-negative and Gram-positive bacteria, anaerobic bacteria, Mycoplasma, and Spirochetes. Valnemulin ameliorates enteric diseases, acute polyarthritis and enzootic pneumonia in pigs [1]. Valnemulin exhibits anti-inflammatory efficacy against lipopolysaccharide (HY-D1056)-induced lung injury .
LTA4H-IN-4 (compound 3) is an orally active LTA4H inhibitor. The IC50 value of LTA4H-IN-4 for hERG is 156 μM. LTA4H-IN-4 can be used in inflammation related studies [1].
F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders [1].
Tivozanib hydrate (AV-951 hydrate; KRN951 hydrate) is the hydrate form of Tivozanib (HY-10977). Tivozanib hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrate exhibits antitumor efficacy [1].
4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitory activities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects [1] .
BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice[1] .
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice[1].
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice[1].
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties [1]. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats . β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression .
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice[1].
YM-244769 dihydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 dihydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 dihydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 dihydrochloride can also increase urine volume and urinary excretion of electrolytes in mice[1] .
JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively [1]. Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607 .
7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice[1].
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice[1].
HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety [1].
GPR40 agonist 5 (compound I-14) is an orally active and potent GPR40 (G protein coupled receptor 40) agonist, with an EC50 of 47 nM. GPR40 agonist 5 decreases the levels of blood glucose and improves the glucose tolerance. GPR40 agonist 5 has sufficient effectiveness for the control of hyperglycemia state in type 2 diabetic mice[1]. GPR40 agonist 5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
YM-244769 is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice[1] .
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].
non-alcoholic fatty liver disease [1] .
YM-244769 hydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice[1] .
9AzNue5Ac, 9-azido-9-deoxy-N-acetylneuraminic acid, is a click chemistry reagent and a Neu5Ac analogue with the substitution of 9-hydroxyl group with an azide. 9AzNue5Ac could be metabolized and incorporated into sialoglycans in living cells and mice. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity [1].
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model [1] .
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1] .
FD1024 is PIM inhibitor (IC50s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice[1].
URAT1&XO inhibitor 2 (Compound BDEO) is a dual inhibitor of xanthine oxidase and URAT1, with IC50 of 3.3 μM for xanthine oxidase. URAT1&XO inhibitor 2 blocks uptake of uric acid in HEK293 cells expressing URAT1, with a Ki value of 0.145 μM. URAT1&XO inhibitor 2 decreases serum urate level and uric acid excretion in hyperuricemic mice. URAT1&XO inhibitor 2 can be used for research of hyperuricemia [1].
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research [1] .
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts [1].
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) [1].
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator [1] . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS [1] .
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1(LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells [1].
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model [1] .
(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist [1]. (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively . (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice .
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice[1] .
NIR-H2O2 is a cell-permeable near-infrared (NIR) fluorescent turn-on sensor. NIR-H2O2 has both absorption and emission in the NIR region. NIR-H2O2 responds to H2O2 with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-H2O2 is capable of imaging endogenously produced H2O2 in living cells and mice[1].
CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis [1] .
T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream) [1].
Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice[1].
NMDAR/TRPM4-IN-2 free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 free base shows neuroprotective activity. NMDAR/TRPM4-IN-2 free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss [1].
SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity [1]. SBI-581 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model [1] .
NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel [1].
Tat-beclin 1 scrambled is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus [1].
Tat-beclin 1 scrambled TFA is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus [1].
PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD [1].
(S,R,S)-MI-1061 is the isomer of MI-1061(HY-125858). (S,R,S)-MI-1061 can used to synthesize Antibody-Drug Conjugates (ADCs). MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity [1].
Fluphenazine (dihydrochloride) (Standard) is the analytical standard of Fluphenazine (dihydrochloride). This product is intended for research and analytical applications. Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1] .
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice was 75.4% [1].
Famciclovir (BRL 42810) is an orally active nucleoside analogue. Famciclovir is an antiviral agent with potent activities against HBV, HSV and VZV. Famciclovir can be used for the research of herpesvirus infection [1].
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization [1] .
NIBR189 is an EBI2 (Epstein-Barr virus-induced gene 2) antagonist. NIBR189 inhibits human and mouse EBI2 with IC50s of 11 and 16 nM, respectively. NIBR189 can be used for the research of autoimmune diseases [1].
CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes [1] .
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1[1] . GSK-J4 induces endoplasmic reticulum stress-related apoptosis .
K 01-162 (K162) inhibits the fibril formation of Aβ peptides and eliminates their neurotoxicity. K 01-162 binds with Aβ42 peptide with an EC50 value of 80 nM. K 01-162 binds directly to AβO with a KD value of 19 μM. K 01-162 is capable of penetrating the brain and can be used for the research of Alzheimer’s disease [1] .
Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest [1] .
BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma [1] .
Valinomycin is a potassium-specific ionophore, the valinomycin-K + complex can be incorporated into biological bilayer membranes with the hydrophobic surface of valinomycin, destroys the normal K + gradient across the membrane, and as a result kills the cells, incorporating into liposomes can significantly reduces the cytotoxicity and enhances the targeting effect. Valinomycin exhibits antibiotic, antifungal, antiviral, antitumor and insecticidal efficacy, thus can be used for relevant research [1] .
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1[1] .
MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis[1].
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM [1].
LeuRS-IN-1 is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively [1]. LeuRS-IN-1 inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM) .
LeuRS-IN-1 hydrochloride is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 hydrochloride has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively [1]. LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM) .
FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease [1] .
Alirocumab (REGN 727) is a human monoclonal antibody inhibitor of PCSK9. Alirocumab is a monoclonal antibody. Alirocumab has anti-inflammatory, antiangiogenic and antioxidant effects. Alirocumab can be used in the study of hypercholesterolemia [1] .
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis[1].
HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity [1].
TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model [1].
COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks [1].
BF844 mitigate hearing loss associated with USH3 (usher syndrome type III) mutation CLRN1 (clarin-1) N48K. BF844 induces CLRN1N48K transportes to the plasma membrane. BF844 shows significantly preserves hearing in vivo [1].
YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity [1].
DHODH-IN-22 is a potent, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value of 0.3 nM. DHODH-IN-22 can be used for researching acute myelogenous leukemia (AML) [1].
Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest [1] .
Cefroxadine (CGP 9000) is an orally active cephalosporin antibiotic. Cefroxadine is more effective than cephalexin against Escherichia coli and Klebsiella pneumoniae with MIC values of 3.13 and 1.56 μg/mL respectively with a concentration of 10 6 μg/mL. Cefroxadine can be used for the research of infection [1].
AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research [1].
RyR2 stabilizer-1 (compound 12a) is a potent RyR2 stabilizer and SERCA2a activator with EC50s of 2.7 μM for RyR2 and 383 nM for SERCA2. RyR2 stabilizer-1 inhibits Ca 2+ leakage from the SR RyR2 while promoting SERCA2 to pump Ca 2+ back to SR, which make RyR2 stabilizer-1 possible to prevent cardiac arrhythmias [1].
CARM1/HDAC2-IN-1 (compound CH-1) is a dual inhibitor against CARM1 and HDAC2, with IC50 values of 3.71 nM and 4.07 nM, respectively. CARM1/HDAC2-IN-1 possesses antitumor activity [1].
Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC50 of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis [1].
SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis[1].
CSF1R-IN-23 (Compound 7dri) is a selective inhibitor for colony-stimulating factor-1 receptor (CSF1R), with IC50 of 36.1 nM. CSF1R-IN-23 serves as antineuroinflammatory agent in mouse model. CSF1R-IN-23 is blood brain barrier (BBB) permeable [1].
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner [1]. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester proagent of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice[1].
D-5-Hydroxytryptophan (D-5-HTP) is the D-isomer of 5-HTP and can be isolated from DL-5-hydroxytryptophan by continuous separation. Compared with intraperitoneal administration of L-5-Hydroxytryptophan, which can induce dose-dependent backward walking behavior in mice, D-5-Hydroxytryptophan has no significant effect on mouse behavior and is a negative control. D-5-Hydroxytryptophan is also a 5-HT ligand, capable of binding to the 5-HT site with affinity in the micromolar range [1] .
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression [1].
Emodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction [1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice[1] .
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator [1] . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase [1] .
Piperacillin sodium is a semisynthetic broad-spectrum β-lactam antibiotic which exhibits potent bactericidal activity against Gram-negative bacteria as well as select Gram-positive strains through penicillin-binding proteins. Piperacillin is most commonly used in combination with the β-lactamase inhibitor Tazobactam [1] .
Garenoxacin (BMS284756) Mesylate hydrate is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms [1].
Garenoxacin (BMS284756) is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms [1].
Cetrimonium bromide (CTAB), a quaternary ammonium, is an orally active cationic surfaetant. Cetrimonium bromide has toxicity and anticancer effect. Cetrimonium bromide inhibits cell migration and invasion through modulating the canonical and non-canonical TGF-β signaling pathways. Cetrimonium bromide can be used for DNA extraction [1] .
V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells [1].
N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation [1] .
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1(AdipoR1;Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) [1] .
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo [1].
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model [1].
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase [1] .
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase [1] .
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer [1].
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase [1] .
SPHINX is a selective SRPK1 inhibitor with an IC50 value of 0.58 μM. SPHINX effectively reduces Choroidal Neovascularization (CNV) in vivo. SPHINX can be used for the research of (age-related macular degenaration) AMD [1].
FDGlcU can be used as a fluorescent probe for non-invasively image with a high level of fluorescent activity. FDGlcU is non-fluorescent when the fluorescein is conjugated with two mono-glucuronides (Ex/Em=480/514 nm) [1].
Nimustine is a nitrosourea alkylating agent. Nimustine induces cell apoptosis, and activates DNA damage response and MAPK signaling. Nimustine shows anti-cancer effects, it can be used for the research of cancer [1] .
(R)-ZG197 is a highly selective Staphylococcus aureus Caseinolytic protease P (SaClpP) activator with an EC50 of 1.5 μM. (R)-ZG197 also activates Homo sapiens ClpP (HsClpP) with an EC50 of 31.4 μM [1].
Feralolide is a dihydroisocoumarin isolated from the methanolic extract of aloe vera resin. Feralolide is also a dual inhibitor of AChE and BuChE, with IC50s of 55 μg/mL and 52 μg/mL respectively. Feralolide has antioxidant activity and inhibits 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2′-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS). Feralolide could be used in research into cognitive disorders such as Alzheimer's disease, potentially restoring and enhancing memory [1].
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs [1].
Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response [1] .
CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases [1] .
CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases [1] .
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model [1].
1,11b-Dihydro-11b-hydroxymedicarpin (11b-Hydroxy-11b,1-dihydromedicarpin) is a pterocarpan from Ononis viscosa subsp. breviflora is a Medicarpin derivative [1]. Medicarpin, a natural pterocarpan, heals cortical bone defect by activation of Notch and Wnt canonical signaling pathways . Medicarpin prevents arthritis in post-menopausal conditions by arresting the expansion of TH17 cells and pro-inflammatory cytokines. Medicarpin down-regulates pro-inflammatory cytokines like TNF-α, IL-6 and IL-17A, while up-regulates anti-inflammatory cytokine IL-10 in arthritis (CIA) model of mice .
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice[1].
PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC50=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice[1].
ADS032 is a dual inhibitor of NLRP1 and NLRP3 that can rapidly, reversibly and stably inhibit inflammasome formation. ADS032 can reduce NLPR1 and NLRP3 activation of human macrophages and bronchial epithelial cells to secrete and mature IL-1β and TNF-α, and reduce NLRP3-induced ASC speck formation. ADS032 protected mice against the deadly influenza A virus, reducing inflammation in the lungs and improving survival. ADS032 inhibits Nigericin (HY-127019)-induced IL-1β secretion with IC50s of 94.6 μM (No wash out) and 354 μM (Wash out) respectively [1].
Ketoprofen (RP-19583) is a non-steroidal anti-inflammatory agent. Ketoprofen can inhibits the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity [1] .
Penicillamine (D-(-)-Penicillamine) is a penicillin metabolic degradation product, can be used as a heavy metal chelator. Penicillamine reduces free copper and reduces oxidative stress. Penicillamine has effect of seizures through nitric oxide/NMDA pathways. Penicillamine is a potential immune modulator. Penicillamine can be used for the research of Wilson disease, rheumatoid arthritis, and cystinuria [1] .
Flunisolide is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation [1] .
Smurf1-IN-A01 is a Smurf1 inhibitor. Smurf1-IN-A01 has anticancer activity and can be used for the research of osteoporosis and age-related macular degeneration [1] .
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1(mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity [1]. (Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease [1] .
Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease [1] .
IP2 is an immunomodulatory agent. IP2 increases PTP (Pioneer Translation Product)-derived antigen presentation in cancer cells. IP2 shows non-cytotoxic for cancer cells. IP2 induces tumor growth defects in mouse [1].
EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers [1].
Ketoprofen (RP-19583) lysinate is a non-steroidal anti-inflammatory agent. Ketoprofen lysinate can inhibit the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity [1] .
Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation [1] .
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability [1].
BChE-IN-14 (compound 19c) is a selective butyrylcholinesterase (BChE) inhibitor with IC50s of 0.23 and 0.011 μM for eqBChE and hBChE, respectively. BChE-IN-14 shows good blood brain barrier permeation and primary cell safety. BChE-IN-14 is able to restore cognitive impairment in vivo, it can be used for the research of Alzheimer’s disease [1].
cyclo(RLsKDK) (BK-1361) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) has potential applications in inflammatory diseases and cancer [1].
cyclo(RLsKDK) (TFA) (BK-1361 (TFA)) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) (TFA) has potential applications in inflammatory diseases and cancer [1].
VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC50 value of 155 nM. VU6004256 has the potential for the research of schizophrenia [1].
δ-Theraphotoxin-Hm1a toxin is a selective Nav1.1 activator. δ-Theraphotoxin-Hm1a toxin elicits pain and touch sensitivity. δ-Theraphotoxin-Hm1a toxin can be used for the research of irritable bowel syndrome [1].
Anticancer agent 195 (Compound 10) is an inhibitor for ELF3-MED23 PPI with Ki of 0.68 μM. Anticancer agent 195 induces apoptosis and exhibits antitumor activity [1].
Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria [1] .
Nafamostat, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat has anticancer and antivirus effect. Nafamostat induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1(TNFR1). Nafamostat can be used in the development of the pathological thickening of the arterial wall [1]3] .
Nafamostat mesylate (FUT-175), an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat mesylate has anticancer and antivirus effect. Nafamostat mesylate induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1(TNFR1). Nafamostat mesylate can be used in the development of the pathological thickening of the arterial wall [1]3] .
Nafamostat hydrochloride, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat hydrochloride has anticancer and antivirus effect. Nafamostat hydrochloride induces apoptosis by up-regulating the expression of tumor necrosis factor receptor-1(TNFR1). Nafamostat hydrochloride can be used in the development of the pathological thickening of the arterial wall [1]3] .
GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 value of 0.4 μM. GSK4112 can be used as a chemical tool to probe the function of Rev-erbα in transcriptional repression, regulation of circadian biology, and metabolic pathways [1].
Diallyl Trisulfide is an orally active anticancer agent that can be isolated from garlic. Diallyl Trisulfide has the ability to induce apoptosis and exhibits anticancer, anti-inflammatory, antioxidant, and antibacterial activities. Diallyl Trisulfide can be used to study a variety of cancers, including liver, colon and prostate cancer [1] .
Isoallolithocholic acid (3β-Hydroxy-5α-cholanic acid), a derivative of Lithocholic acid (HY-10219), is a T cell regulator. Isoallolithocholic acid enhances regulatory T cells (Tregs) differentiation [1].
GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth [1].
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) [1].
BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM [1].
α-Glucosidase-IN-16 is a potent and orally active α-glucosidase inhibitor with an IC50 value of 3.28 μM. α-Glucosidase-IN-16 can reduce the level of blood glucose in Streptozotocin-induced diabetic rats. Antidiabetic activity [1].
Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19 [1] .
Pafuramidine (maleate) (DB289 (maleate)) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine (maleate) (DB289 (maleate)) is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria [1] .
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice[1] .
RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitory activity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice[1].
Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
CHR-6494 is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer [1].
ML604440 is a specific and cell-permeable Proteasome β1i (LMP2) subunit inhibitor. ML604440 can be used in experimental colitis, EAE and autoimmune disease research. ML604440 shows synergistic effects and advantageous when combined with LMP7 inhibitor [1] .
CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer [1] .
ML179 (SR-1309) is a inverse LRH1 (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].
GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity [1].
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer [1].
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer [1] .
KGP591 is a tubulin polymerization inhibitor (IC50 0.57 µM). KGP591 induces significant G2/M stagnation, inhibits cell migration, disrupts microtubule structure and cell morphology in MDA-MB-231 cells. KGP591 shows antitumor activity in orthotopic model of kidney cancer (RENCA) [1].
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM [1]. Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
Benzbromarone is an orally active anti-gout agent. Benzbromarone has anti-infammatory, anti-oxidative stress and nephroprotective effects. Benzbromarone can be used for the research of hyperuricemia and gout [1] .
HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites [1].
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment [1] .
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment [1] .
TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), shows excellent selectivity over indoleamine-2,3-dioxygenase (IDO), with an IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo [1].
R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research [1].
Peramivir is an novel cyclopentane neuraminidase inhibitor of influenza virus. Peramivir has antiviral activity and anti-cytokines stom effects. Peramivir can be used for the research of COVID-19 [1] .
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease [1].
Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research [1] .
SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC50 is 4.2 nM and Ki is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer [1] .
GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo[1].
Benzosceptrin C is an inhibitor for PD-L1, which promotes programmed cell death ligand (PD-L1) degradation in a lysosomal pathway, enhances the cytotoxicity of T-cells and exhibits antitumor activity [1].
T-2 Toxin (T-2 Mycotoxin) is a toxic trichothecene mycotoxin produced by various Fusarium species in feedstuffs and cereal grains, LD50 values of T-2 Toxin in mice and rats are 5.2 and 1.5 mg/kg BW a,respectively [1]. T-2 Toxin (T-2 Mycotoxin) can be transformed into a variety of metabolite, the typical metabolites of T-2 toxin in animals are HT-2 toxin and T-2-triol, which are hydrolysates [1]. T-2 Toxin (T-2 Mycotoxin) is an inhibitor of protein synthesis resulting from binding peptidyltransferase, which is an integral part of the 60s ribosomal subunit. T-2 Toxin (T-2 Mycotoxin) inhibits the synthesis of DNA and RNA, interferes with the metabolism of membrane phospholipids, and increases the level of liver lipid peroxides [1]. T-2 Toxin (T-2 Mycotoxin) induces apoptosis in the immune system, gastrointestinal tissues, and fetal tissues .
Pinostrobin is a flavonoid with anti-cancer, antioxidant, antiviral and neuroprotective activities. Pinostrobin has oral activity. Pinostrobin is a potent PCSK9 inhibitor that inhibits the catalytic activity of PCSK9. Pinostrobin can be used in the research of viral infections, cancer, leukemia, cardiovascular and cerebrovascular diseases, cirrhosis, inflammation and neurological diseases [1] .
Hedgehog IN-6 (Compound Q29) is a Hedgehog (Hh) inhibitor that can be used in cancer research. Hedgehog IN-6 inhibits the hedgehog (Hh) pathway by binding to the cysteine-rich domain (CRD) of Smoothened (Smo) and blocking its cholesterization [1].
WYJ-2 is a selective agonist for toll-like receptor 2/1(TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC) [1].
Peimine (Verticine; Dihydroisoimperialine) is an orally active natural product. Peimine has anti-inflammatory, analgesic and cough relieving effects. Peimine can be used in cancer and inflammation related research [1] .
PD-1/PD-L1-IN-27 is a potent PD-1/PD-L1 inhibitor with an IC50 value of 134 nM. PD-1/PD-L1-IN-27 shows antitumor effects with low T cell cytotoxicity. PD-1/PD-L1-IN-27 has the ability to activate CD8 + T cells and reduces T cell exhaustion [1].
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research [1].
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research [1] .
EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also enhances autophagy by inhibiting Na +/H +-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma [1] .
EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na +/H +-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma [1] .
Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis [1] .
Anethole is a type of orally active aromatic compound that is widely found in nature and used as a flavoring agent. Anethole possesses anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, anesthetic, estrogenic, central nervous system depressant, hypnotic, insecticidal, and gastroprotective effects. Anethole can be used in the study of oxidative stress-related skin diseases and prostate cancer [1] .
LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections [1].
Antitumor photosensitizer-5 (Ru2) is a photosensitizer which effectively target tumor mitochondria with an IC50 of 0.3 μM for phototoxicity to A549 cells. Under 460 nm light irradiation, antitumor photosensitizer-5 induces the generation of reactive oxygen species and NADH depletion, causes mitochondrial damage and activation of caspase-3, inducing apoptosis and suppressing cell migration. Antitumor photosensitizer-5 has the potential to prevent the growth of malignant tumors, therefore, shows the potential to be applied to photodynamic therapy [1].
IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research [1].
MF59 (GMP) is a GMP grade MF59. MF59 is a immunologic adjuvant. MF59 significantly influnces immunogenicity of influenza vaccines. MF59 reduces the viral load in the lungs of challenged mice[1].
Medical fluorophore 33 is a novel quinoline-isoquinoline salt. Medical fluorophore 33 exhibits a strong fluorescent signal, good microsomal stability and high biocompatibility in vivo. Medical fluorophore 33 has antitumor activity in colorectal cancer mice[1].
NIR-Thiol dinitrobenzenesulfonate has both absorption and emission in the NIR region. NIR-Thiol dinitrobenzenesulfonate responds to thiol with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-Thiol dinitrobenzenesulfonate is capable of imaging endogenously produced thiol in living cells and mice[1].
NFL-NH2 is a mitochondrial-targeted near-infrared ratiometric fluorescent probe. NFL-NH2 can rapidly detect NO levels associated with the inflammatory damage degree in rheumatoid arthritis (RA) mice models by ratiometric fluorescence imaging. The excitation wavelength and emission wavelength are 650 nm and 780 nm, respectively [1].
FITC-labeled Tominersen (sodium) is the Tominersen labeled with FITC. Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen improves survival and reduces brain atrophy in mice. Tominersen can be used for the research of Huntington’s disease (HD).
Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies [1].
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity [1]. MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
IR-Crizotinib is a NF-κB-inducing kinase (NIK) inhibitor that crosses the blood-brain barrier and fluorescently localizes intracranial glioblastoma (GBM) in mice (IC50=3.381 μM). IR-Crizotinib is conjugated from the near-infrared dye IR-786 and the NF-κB-inducing kinase (NIK) inhibitor Crizotinib. IR-Crizotinib can effectively inhibit the growth and invasion of glioma in vitro and in vivo and can be used in cancer research [1].
NIR-H2O2 is a cell-permeable near-infrared (NIR) fluorescent turn-on sensor. NIR-H2O2 has both absorption and emission in the NIR region. NIR-H2O2 responds to H2O2 with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-H2O2 is capable of imaging endogenously produced H2O2 in living cells and mice[1].
FDGlcU can be used as a fluorescent probe for non-invasively image with a high level of fluorescent activity. FDGlcU is non-fluorescent when the fluorescein is conjugated with two mono-glucuronides (Ex/Em=480/514 nm) [1].
Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research [1] .
Lysophosphatidylcholines is an orally active lysolipid and a component of oxidized low density lipoprotein (LDL). Lysophosphatidylcholines induces cell injury, the production of IL-1β and apoptosis. Lysophosphatidylcholines has a proactive effect on sepsis [1] .
Choline tosylate is a nucleophilic compound that inhibits phospholipase A2 and phospholipase C. Choline tosylate inhibits tumor growth in mice by inhibiting the formation of diacylglycerol (DAG) [1] .
Type II collagen II is a protein used to treat osteoarthritis. Type II collagen shows significant efficacy in improving the pain and inflammation of collagen induced arthritis in mice[1].
HEPPS (EPPS) is a buffering agent with the useful pH range from 7.3 ~ 8.7. HEPPS reduces Aβ-aggregate-induced memory deficits and rescues cognitive deficits in mice. EPPS is orally active and penetrates the blood-brain barrier [1].
MF59 (GMP) is a GMP grade MF59. MF59 is a immunologic adjuvant. MF59 significantly influnces immunogenicity of influenza vaccines. MF59 reduces the viral load in the lungs of challenged mice[1].
DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice[1] .
Zymosan A (Zymosan A from Saccharomyces cerevisiae) is a TLR2 agonist, that targeting TLRs can prevent and suppress IR-induced intestinal injury. Zymosan A exhibits a significant radioprotective effect, and protects IR-induced intestinal injury in mice. Zymosan A promotes the regeneration of intestinal stem cells (ISCs), after IR injury [1].
C12-200 is an ionizable cationic lipid and auxiliary lipid. C12-200 is commonly used for mRNA delivery. Administration of human erythropoietin (EPO) mRNA or factor VII siRNA increased and decreased serum factor VII levels, respectively, in LNPs mice containing C12-200 [1] .
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice[1] .
CL4F8-6 is an ionizable cationic lipid with a pKa of 6.14. CL4F8-6 can be used in lipid nanoparticles (LNPs)-based mRNA therapeutics. CL4F8-6 LNPs carrying Cas9 mRNA and sgRNA could induce CRISPR-mediated gene knockdown in mice[1].
AA-T3A-C12 is an anisamide ligand-tethered lipidoid (AA-lipidoid). AA-T3A-C12 mediates great RNA delivery and transfection of activated fibroblasts [1].
Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
Clovibactin TFA is the TFA salt form of Clovibactin (HY-P10027). Clovibactin TFA is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors [1].
Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1mice[1] .
Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1mice[1] .
Cd1a is a β-toxin derived from the African spider Ceratogyrus darlingi. Cd1a can regulate calcium ion channels. Cd1a inhibits human calcium ion channels (Cav2.2)(IC502.6 μM) and mouse sodium ion channels (Nav1.7).Cd1a can be used in the development of peripheral pain treatment drugs [1].
YPLP is a yeast-derived peptide Tyr-Pro-Leu-Pro, which exhibits activity in anti fatigue mechanisms through the nuclear factor erythroid-2-related factor 2 (Nrf2)- and AMP-activated protein kinase (AMPK) pathway. YPLP is orally active [1].
xStAx-VHLL is a PROTAC β-catenin degrader that manifests strong inhibition of Wnt signaling and sustains degradation of β-catenin in cancer cells and the intestinal organoids derived from wild-type and APC –/–mice. xStAx-VHLL can be used as a promising anticancer agent [1].
P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity [1].
KK-103 is a precursor of leucine-enkephalin (Leu-ENK) overcomes high proteolytic instability of Leu-ENK via markedly increased plasma stability in mice that has antinociceptive effect [1].
Endokinin C is a peptide component of endokinin. Endokinin C works as a neurotransmitter or modulator in the pain system. Pretreatment with endokinin C prevents induction of scratching behavior and thermal hyperalgesia of endokinin A/B in mice[1].
[Pro3]-GIP (Mouse) is a GIP receptor antagonist (IC50: 2.6 μM). [Pro3]-GIP (Mouse) improves glucose tolerance and insulin sensitivity in ob/ob mice. [Pro3]-GIP (Mouse) can be used for research of type 2 diabetes [1] .
Glp-Amyloid-β (3-40) Peptide (human) (AβpE3-40) is a minor amounts of pyroglutamate-modified Aβ isolated from from 24-month-old Amyloid precursor protein (APP) transgenic Mice[1].
DiaPep277 is a 24 amino acid peptide derived from positions 437-460 in HSP60. DiaPep277 arrests the progression of β-cell destruction in NOD mice. DiaPep277 has an immune modulatory effect on diabetogenic T cells in animal models of diabetes [1] .
IRBP (1-20), human contains a major epitope for the H-2 b haplotype. IRBP (1-20), human induces experimental autoimmune uveoretinitis (EAU) in H-2 bmice[1] .
J5 peptide is an MBP inhibitor that competitively inhibits the binding of MBP85-99 to HLA-DR2. J5 peptide alleviates PLP139-151/MBP85-99-induced experimental autoimmune encephalomyelitis (EAE) in mice. J5 peptide can be used in research on inflammatory and immune diseases [1].
IRBP (1-20), human TFA contains a major epitope for the H-2 b haplotype. IRBP (1-20), human TFA induces experimental autoimmune uveoretinitis (EAU) in H-2 bmice[1] .
L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC50: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test [1] .
G6PI 325-339 (human) hydrochloride is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) hydrochloride primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) hydrochloride induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms [1].
G6PI 325-339 (human) is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms [1].
Neuropeptide S(Rat) TFA is a potent endogenous neuropeptide S receptor (NSPR) agonist (EC50=3.2 nM). Neuropeptide S(Rat) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Rat) TFA also reduces anxiety-like behavior in mice.
retro-inverso TAT-Beclin 1 D-amino acid is has higher activity and resistance to proteolytic degradation in vivo compared to L-amino acids peptide. TAT-Beclin 1 can induce autophagy in peripheral tissues in adult mice as well as in the central nervous system of neonatal mice[1] .
Neuropeptide S(Mouse) TFA is a potent endogenous neuropeptide S receptor (NPSR) agonist (EC50=3 nM). Neuropeptide S(Mouse) TFA induces mobilization of intracellular Ca 2+. Neuropeptide S(Mouse) TFA increases locomotor activity and wakefulness in mice. Neuropeptide S(Mouse) TFA also reduces anxiety-like behavior in mice.
Nv-CATH is an antibacterial peptide of frog origin. Nv-CATH has broad-spectrum antibacterial activity against gram-positive and gram-negative bacteria. Nv-CATH significantly protects mice from fatal infections caused by Staphylococcus aureus. Nv-CATH protects mice from bacterial infection through antimicrobial immunoregulatory duality [1].
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
Microcystin-RR (Cyanoviridin RR) is a potent and orally active protein phosphatase inhibitor. Microcystin-RR induces Apoptosis and ER stress in mice liver [1] .
OVA Peptide (323-339) represents a T and B cell epitope of Ovalbumin (Ova), which is important in the generation and development of immediate hypersensitivity responses in BALB/c mice.
Tyrosylhistidine is a dipeptide consisting of tyrosine and histidine (Tyr-His). Tyrosylhistidine is an orally active antihypertensive peptide. Tyrosylhistidine reduces blood pressure in mice in a model of spontaneous hypertension [1].
R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice[1].
mLR12 is a Trem1 inhibitory peptide. mLR12 decreases aortic rupture rate in BAPN-induced Thoracic aortic aneurysm and dissection (TAAD) mice model [1].
YVAD-CHO is an interleukin-1β converting enzyme (ICE, caspase 1) inhibitor that can partially delay motoneurone death in lesioned facial nerve mice[1].
MOG (92–106), mouse, rat is a biological active peptide. (This is amino acids 92 to 106 fragment of the myelin oligodendrocyte glycoprotein (MOG) from mouse/rat. Mice with MOG (92–106)-induced experimental autoimmune encephalomyelitis develop extensive B cell reactivity against secondary myelin antigens. Despite the fact that this MOG peptide induces only weak T cell responses, MOG-induced autoimmunity is very severe. This peptide is encephalitogenic in SJL mice, DA rats, and rhesus monkeys.)
Collagen Type II Fragment is an anti-inflammatory peptide that potently inhibits collagen-induced arthritis (CIA) in mice. Collagen Type II Fragment can be used for research on inflammation and immunity [1].
Teduglutide is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide is associated with trophic effects on gut mucosa. Teduglutide can be used for the research of short bowel syndrome (SBS) and Crohn's disease (CD) .
SAHM1, a peptide mimetic of a dominant negative form of mastermind-like (MAML), inhibits canonical Notch transcription complex formation. SAHM1 can be used for the research of allergic airway inflammation in mice[1] .
BAM(8-22), a proteolytically cleaved product of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner [1].
CTP is a cardiac targeting peptide. CTP transduces cardiomyocytes in vitro. CTP leads to efficient and specific transduction of heart tissue in mice model. CTP can be used to deliver therapeutic peptides, proteins and nucleic acid specifically to the heart [1].
pTH (2-34) (human) (80 μg/kg) slightly increases serum osteocalcin levels and alkaline phosphatase activity of bone extract (markers of bone formation) in mice. pTH (2-34) is not as effective as pTH (1-34) [1].
PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA is associated with trophic effects on gut mucosa. Teduglutide TFA can be used for the research of short bowel syndrome (SBS) and Crohn's disease (CD) .
BAM(8-22) TFA, a proteolytically cleaved product of proenkephalin A, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1, and induces scratching in mice in an Mrgpr-dependent manner [1].
Kp7-6, a Fas mimetic peptide, is a Fas/FasL antagonist. Kp7-6 protects cells from Fas-mediated apoptosis, and protects mice from Fas-mediated hepatic injury [1] .
IA9 (human TREM-2 182-190) is a TREM-2 inhibitor , and can diminish release of proinflammatory cytokines and dramatically suppressed joint inflammation and damage in collagen-Induced Arthritis (CIA) mice model [1].
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice[1] .
Splenopentin diacetate is a synthetic immunomodulating pentapeptide corresponding to the residues 32-36 of the splenic hormone splenin. Splenopentin diacetate influences both early T and B cell differentiation, to increase the number of antibody-forming cells in mice after gamma irradiation [1] .
TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice. TAT-M2NX can be used to study ischemic neuronal damage [1].
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia [1] .
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice[1] .
Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa [1].
IA9 TFA (human TREM-2 182-190 TFA) is a TREM-2 inhibitor , and can diminish release of proinflammatory cytokines and dramatically suppressed joint inflammation and damage in collagen-Induced Arthritis (CIA) mice model [1].
w-Conotoxin SVIB is a peptide toxin, it can be isolated from Conus venoms. w-Conotoxin SVIB inhibits twitch response with an IC50 value of 37 nM. w-Conotoxin SVIB induces respiratory distress and it can be lethal to mice at a high concentration [1] .
CP7-FP13-2 is a peptide with antivirulence factor and antibacterial activity. CP7-FP13-2 inhibits the formation of Staphylococcus aureus biofilm and has good antibacterial efficacy in mice[1].
Sakura-6 is a SERT-nnos interaction promoter that significantly increases the SERT-nnos complex, but reduces the level of SERT on the cell surface. Acute injection of Sakura-6 into the dorsal raphe nucleus (DRN) causes depression-like behavior in mice[1].
lota-conotoxin RXIA is an agonist of voltage-gated
sodium channels (Nav1.2,1.6, 1.7). Iota-conotoxin RXIA
can induce repetitive action potential and seizure in motor axons of frogs
after intracranial injection in mice[1].
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa [1].
MR 409 is a selected growth hormone-releasing hormone (GHRH) agonist. MR 409 has remarkable neuroprotective effects through enhancing endogenous neurogenesis in cerebral ischemic mice. MR 409 also inhibits the in vivo growth of lung cancer [1] .
TAT-CIRP is a a small peptide, refers to Trans-trans-activating (Tat)-cold-inducible RNA binding protein. TAT-CIRP is an inhibitor of myeloid differentiation protein 2 (MD2). TAT-CIRP exhibits robust neuroprotection against ischemic and hemorrhagic stroke in mice[1].
NN1177 (NNC9204-1177) TFA is a long-acting GLP-1/glucagon receptor co-agonist. NN1177 TFA can induce a dose-dependent body weight loss in diet-induced obese (DIO) mice[1] .
ELAAWCRWGFLLALLPPGIAG (P5) is derived from rat HER2/neu protein with 21 amino acid length (aa 5-25). ELAAWCRWGFLLALLPPGIAG can induce cytotoxic T lymphocyte (CTL) responses in mice bearing HER2-positive tumours [1].
cpm-1285 induces apoptosis by functionally blocking intracellular Bcl-2 and related death antagonists. cpm-1285 shows strong binding potency to Bcl-2 with an IC50 value of 130 nM. cpm-1285 reduces tumor burden in mice[1].
BigLEN(mouse) TFA is a GPR171 agonist. BigLEN(mouse) TFA is a proSAAS-derived neuropeptide. BigLEN(mouse) TFA regulates food intake in mice. BigLEN(mouse) inhibits the release of glutamate onto parvocellular neurons of the paraventricular nucleus in a process dependent upon activation of postsynaptic G proteins.
T-peptide, a Tuftsin analog, can be used for the research of human immunodeficiency virus (HIV) infection. T-peptide prevents cellular immunosuppression and improves survival rate in septic mice. T-peptide also can inhibit the growth of residual tumor cells after surgical resection [1] .
Cyclic MKEY is a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, which protects against atherosclerosis and aortic aneurysm formation by mediating inflammation. Cyclic MKEY also protects against stroke-induced brain injury in mice[1] .
RG33 Peptide is a diabetes inhibitor that significantly improves glucose clearance in insulin-resistant mice. RG33 Peptide effectively solubilizes lipid vesicles and promotes cholesterol efflux in cultured macrophages. RG33 Peptide is used in research into type 2 diabetes (T2D) [1].
A8SGLP-1 is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 reduces blood glucose in db/db mice without affecting its function [1].
Z-Leu-Leu-Leu-fluoromethyl ketone (Z-LLL-FMK) is a cysteine protease inhibitor. Z-Leu-Leu-Leu-fluoromethyl ketone inhibits SARS infection. Z-Leu-Leu-Leu-fluoromethyl ketone also protects mice against a T. crassiceps challenge [1] .
GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice[1] .
ELAAWCRWGFLLALLPPGIAG TFA (P5) is derived from rat HER2/neu protein with 21 amino acid length (aa 5-25). ELAAWCRWGFLLALLPPGIAG TFA can induce cytotoxic T lymphocyte (CTL) responses in mice bearing HER2-positive tumours [1].
β-Amyloid (1-16) rat is a β-amyloid peptide (Abeta), a metal-binding domain fragment of amyloid. Three amino acid substitutions in β-Amyloid (1-16) rat that differ from humans render rats and mice less susceptible to AD-like neurodegeneration [1].
Cyclic MKEY TFA is a synthetic cyclic peptide inhibitor of CXCL4-CCL5 heterodimer formation, which protects against atherosclerosis and aortic aneurysm formation by mediating inflammation. Cyclic MKEY TFA also protects against stroke-induced brain injury in mice[1] .
IGRP(206-214) is a biological active peptide. (This peptide corresponds to residues 206–214 of murine islet-specific glucose-6-phosphatase catalytic subunit–related protein (IGRP). This peptide is T cells specific for proinsulin and IGRP induces diabetes in non-obese diabetic (NOD) mice.)
A8SGLP-1 TFA is an orally active GLP-1 analogue that the alanine at position 8 substituted with serine. A8SGLP-1 TFA reduces blood glucose in db/db mice without affecting its function [1].
Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice[1].
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research [1] .
GLP-1(32-36)amide TFA, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. GLP-1(32-36)amide TFA could inhibit weight gain and modulate whole body glucose metabolism in diabetic mice[1] .
Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis [1] .
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC), a cyclic RGD peptide which has high affinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors [1].
TAT-Gap19, a Cx mimetic peptide, is a specific connexin43 hemichannel (Cx43 HC) inhibitor. TAT-Gap19 does not inhibits the corresponding Cx43 GJCs. TAT-Gap19 traverses the blood-brain barrier and alleviate liver fibrosis in mice[1] .
Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe −/− Irs 2+/−mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation .
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research [1] .
TAT-Gap19 TFA, a Cx mimetic peptide, is a specific connexin43 hemichannel (Cx43 HC) inhibitor. TAT-Gap19 TFA does not inhibits the corresponding Cx43 GJCs. TAT-Gap19 TFA traverses the blood-brain barrier and alleviate liver fibrosis in mice[1] .
Urumin has antiviral activity against the human influenza A virus. Urumin inhibits the growth of PR8 influenza virus (IC50: 3.8 μM). Urumin targets the conserved stalk of H1 hemagglutini, and is effective at neutralizing drug-resistant H1 influenza viruses. Urumin protects naive mice from lethal influenza infection [1].
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1(PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis [1] .
Cytochrome c-pigeon (88-104) (PCC 88-104) has full stimulatory activity for pigeon cytochrome c-primed T cells from B10.A mice. The I-E k-restricted T cell response to Cytochrome c pigeon (pcyt c) is specific for the COOH-terminal sequence 88-104 [1] .
Bevonescein (ALM-488) is a novel, intravenously-administrated fluorescein-conjugated peptide that binds nerve-associated connective tissue, labels peripheral nerves under real-time fluorescence imaging (FL) in living mice and human ex vivo nerve tissue. Bevonescein is a peptide-linked tracer which fluorescently labeled both intact and degenerated nerves [1] .
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats [1] .
PKCd (8-17) is a biological active peptide. (This peptide is derived from the V1 domain of protein kinase C (PKC)d. It inhibits phorbol 12-myristate 13-acetate (PMA)-induced PKCd translocation and activation. Inhibition of PKCd reduces ischemia damage in cardiac and cerebral cells, induces proliferation of fibroblasts, and inhibits graft coronary artery disease in mice.)
γ-Glutamylvaline is an activator of CaSR with anti-inflammatory activity. γ-Glutamylvaline inhibits TNF-α-induced proinflammatory cytokine production and increases Wnt5a expression. γ-Glutamylvaline activates calcium-sensing receptor pathways in adipocytes of 3T3-L1mice and prevents low-grade chronic inflammation [1].
GIP (3-42), human acts as a glucose-dependent insulinotropic polypeptide (GIP) receptor antagonist, moderating the insulin secreting and metabolic actions of GIP in vivo [1].
PLP (178-191) is a biological active peptide. (This is amino acids 178 to 191 fragment of the proteolipid protein (PLP), an immunodominant encephalitogenic epitope in SJL mice, one of two major encephalitogenic epitopes. PLP peptide 178 to 191 was compared with another encephalitogenic peptide, 139 to 151. The day of onset of disease induced by PLP 178 to 191 was earlier, but the incidence, severity, and histologic features were indistinguishable.)
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) [1].
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice[1] .
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice[1] .
Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) [1].
Alloferon 1 is an antiviral and antitumoral peptide. Alloferon 1 stimulates natural cytotoxicity of human peripheral blood lymphocytes. Alloferon 1 also induces IFN synthesis, and enhances antiviral and antitumor resistance in mice. Alloferon 1 also shows anti-inflammatory activity in λ-carrageenan-induced paw edema model. Alloferon 1 can be isolated from the blood of the blow fly Calliphora vicina (Diptera) [1] .
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC50:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses [1] .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats [1] .
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice[1] .
γ-Fibrinogen377-395 is a fibrinogen-derived inhibitory peptide, as well as fibrinogen epitope. γ-Fibrinogen377-395 blocks microglia activation and inhibits fibrin-Mac-1 interactions in vitro, and suppresses experimental autoimmune encephalomyelitis (EAE) in micein vivo. γ-Fibrinogen377-395 can be used for research in multiple sclerosis (MS), and other neuroinflammatory diseases associated with blood-brain barrier disruption and microglia activation [1].
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats [1] .
γ-Fibrinogen377-395 TFA is a fibrinogen-derived inhibitory peptide, as well as fibrinogen epitope. γ-Fibrinogen377-395 TFA blocks microglia activation and inhibits fibrin-Mac-1 interactions in vitro, and suppresses experimental autoimmune encephalomyelitis (EAE) in micein vivo. γ-Fibrinogen377-395 TFA can be used for research in multiple sclerosis (MS), and other neuroinflammatory diseases associated with blood-brain barrier disruption and microglia activation [1].
Angiotensin I- 13C5, 15N (human, mouse, rat) is the 13C and 15N labeled Angiotensin I (human, mouse, rat) (HY-P1032). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[1].
Elamipretide TFA (MTP-131 TFA; RX-31 TFA; SS-31 TFA) is the TFA salt form of Elamipretide (HY-P0125). Elamipretide TFA is a mitochondria-targeting peptide, which ameliorates myocardial infarction, improves the renal function and protects neurons form inflammatory and oxidative stress injury [1] .
Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries [1].
Chemerin-9, mouse (Chemerin148-156, mouse) is a C-terminal nonapeptide of chemerin. Chemerin-9, mouse is a ligand for ChemR23 (EC50 = 42 nM). Chemerin-9, mouse reduces basal lipolysis in primary mouse white adipocytes(IC50 = 3.3 nM). Chemerin-9, mouse enhances memory and relieves Aβ1-42-induced memory impairment in AD mice. Chemerin-9, mouse also inhibits atherogenesis [1] .
Tat-beclin 1 scrambled is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus [1].
Tat-beclin 1 scrambled TFA is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus [1].
GAD65 (524-543) is a biological active peptide. (This is amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). It is one of the first fragments of this islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. This peptide is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with p524–543 increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells.)
Valinomycin is a potassium-specific ionophore, the valinomycin-K + complex can be incorporated into biological bilayer membranes with the hydrophobic surface of valinomycin, destroys the normal K + gradient across the membrane, and as a result kills the cells, incorporating into liposomes can significantly reduces the cytotoxicity and enhances the targeting effect. Valinomycin exhibits antibiotic, antifungal, antiviral, antitumor and insecticidal efficacy, thus can be used for relevant research [1] .
D-5-Hydroxytryptophan (D-5-HTP) is the D-isomer of 5-HTP and can be isolated from DL-5-hydroxytryptophan by continuous separation. Compared with intraperitoneal administration of L-5-Hydroxytryptophan, which can induce dose-dependent backward walking behavior in mice, D-5-Hydroxytryptophan has no significant effect on mouse behavior and is a negative control. D-5-Hydroxytryptophan is also a 5-HT ligand, capable of binding to the 5-HT site with affinity in the micromolar range [1] .
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease [1] .
Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease [1] .
cyclo(RLsKDK) (BK-1361) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) has potential applications in inflammatory diseases and cancer [1].
cyclo(RLsKDK) (TFA) (BK-1361 (TFA)) is a specific inhibitor of metalloproteinase ADAM8 with an IC50 value of 182 nM. cyclo(RLsKDK) (TFA) has potential applications in inflammatory diseases and cancer [1].
δ-Theraphotoxin-Hm1a toxin is a selective Nav1.1 activator. δ-Theraphotoxin-Hm1a toxin elicits pain and touch sensitivity. δ-Theraphotoxin-Hm1a toxin can be used for the research of irritable bowel syndrome [1].
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice[1] .
Influenza NP (311-325) is a biological active peptide. (This peptide is amino acids 311 to 325 fragment of the influenza virus nucleoprotein (NP). This bona fide MHC class II restricted epitope from influenza virus was used to study the host immunoresponse during the infection. This peptide elicits the strongest gamma interferon (IFN-gamma) production in the intracellular cytokine assays. It does not stimulate CD8 T-cells in mice.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
Pabinafusp alfa (JR-141) is a transferrin receptor-targeting antibody consisting of Iduronate 2-sulfatase (HY-P76399) and an anti-human transferrin receptor antibody. Pabinafusp alfa is blood-brain permeable and prevents heparan sulfate (HS) deposition in the central nervous system of mucopolysaccharidosis II (MPS II) mice. Pabinafusp alfa improves learning and prevents central nervous system neuronal damage in mice[1].
Tulisokibart (PRA023) is a humanized IgG1-κ monoclonal antibody targeting to TNFSF15/TL1A. Tulisokibart can be used to study a variety of inflammatory/fibrotic diseases, such as Crohn's Disease (CD) .
Topsalysin is a PSA-activated protoxin, a pore-forming protein (synthetic proaerolysin) fusion protein with human prostate-specific antigen. Topsalysin has tumor suppression effect in mice modle [1].
Foralumab (NI-0401) is a potent, orally active human monoclonal antibody targeting the CD3. Foralumab modulates immune responses by human cells in NSG mice that were reconstituted with human hematopoietic stem cells [1].
Bavunalimab (Anti-Human CTLA4xLAG3) is a bispecific human anti-CTLA-4/LAG-3 monoclonal antibody. Bavunalimab activates T cells in NSG mice. Bavunalimab can be used for the research of cancer [1].
Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease [1].
Efineptakin alfa (NT-17) is a long-acting recombinant human IL-7. Efineptakin alfa supports the proliferation and survival CD4 + and CD8 + cells in both human and mice. Efineptakin alfa can be used for glioblastoma research [1].
Ontuxizumab (MORAb-004) is a humanized IgG1/κ anti-endosialin (TEM-1 or CD248) monoclonal antibody with antitumor effects. Ontuxizumab can be used for the research of cancer [1].
Duvakitug is a humanized IgG1-λ2 monoclonal antibody targeting to TNFSF15/TL1A. Duvakitug' main expression system is CHOK1SV cells endogenously expressing glutamine synthetase (GS). Duvakitug can be used in the study of Crohn's Disease (CD) .
Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research [1].
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) [1].
Lutikizumab (ABT-981) is an anti-IL-1α and IL-1β dual variable domain immunoglobulin. Lutikizumab binds and inhibits IL-1α and IL-1β. Lutikizumab can be used for the research of osteoarthritis [1].
Mapatumumab (HGS-ETR1) is a fully human IgG1 agonistic monoclonal antibody that targets tumor necrosis factor-related apoptosis-inducing ligand receptor 1(TRAIL-R1). Mapatumumab can be used for the research of cancer [1].
Pavurutamab (AMG-701) is a bispecific T cell engager molecule that anti-CD3 and anti-B cell maturation antigens (BCMA). Pavurutamab has an extended half-life based on Pacanalotamab (HY-P99798). The Fc of Pavurutamab is coupled to molecules to improve pharmacokinetic parameters. Pavurutamab has potential applications in immune regulation and multiple myeloma (MM) [1] .
Evinacumab (REGN1500) is a human anti-ANGPTL3 (angiopoietin-like protein 3) monoclonal antibody (IgG4 class antibody). Evinacumab reduces plasma lipids in dyslipidemic mice by blocking ANGPTL3. Evinacumab can be used in studies of homozygous familial hypercholesterolaemia (HoFH), refractory hypercholesterolaemia (both familial and non-familial) and severe hypertriglyceridaemia [1].
Asfotase alfa (ENB-0040) is a bone-targeted genetically engineered glycoprotein. Asfotase alfa increases the survival rate, bone mineralization and bone length and prevents mineralization defects of the feet, rib cage, lower limbs, jaw bones in Akp2 −/− knockout mice. Asfotase alfa can be used for the research of perinatal, infantile, and juvenile-onset hypophosphatasia (HPP) [1].
Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab leads to muscle fiber hypertrophy and not hyperplasia in SCID mice. Stamulumab has the potential for Becker muscular dystrophy (BMD), facioscapulohumeral dystrophy (FSHD), and limb-girdle muscular dystrophy (LGMD) research [1] .
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease [1].
Marstacimab (PF-06741086) is an anti-tissue factor pathway inhibitor (TFPI) monoclonal antibody. Marstacimab can be used for the research of hemophilia [1] .
Suvratoxumab (MEDI4893) is a long-acting, high-affinity human anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) [1] .
Relatlimab (BMS-986016) is a human monoclonal antibody anti-LAG-3 antibody generated by immunization of transgenic mice bearing human immunoglobulin miniloci with recombinant LAG-3 protein. Relatlimab blocks LAG-3/MHC II interaction with an IC50 value of 0.67 nM and LAG-3/FGL1 interaction with an IC50 value of 0.019 nM. Relatlimab can be used in research of cancer [1].
Zalutumumab is a high affinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC50s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer [1] .
Prezalumab (AMG 557) is a humanized IgG2 monoclonal antibody targets ICOSL and BAFF. Prezalumab demonstrates beneficial activities on the arthritis of systemic lupus erythematosus. Prezalumab can be used for the research of sjogren's syndrome cutaneous lupus erythematosus, psoriasis and systemic lupus erythematosus (SLE) [1].
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively [1].
Andecaliximab is a recombinant chimeric IgG4 monoclonal antibody (mAb) targets matrix metalloproteinase 9 (MMP9). Andecaliximab shows the antifibrotic efficacy in idiopathic pulmonary fibrosis mouse models. Andecaliximab can be used for the research of gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF) [1] .
Keliximab (SB-210396) is a chimeric human/macaque IgG1anti-CD4 monoclonal antibody with a Ki value of 1.0 nM for soluble CD4. Keliximab blocks T cell proliferation and inhibits IL-2 production. Keliximab can be used for cancer research [1] .
Crizanlizumab is an anti-P-selectin monoclonal antibody. Crizanlizumab binds to P-selectin and blocks its interaction with P-selectin glycoprotein ligand 1 (PSGL-1). Crizanlizumab prevents vaso-occlusive crises (VOCs) and can be used for research of sickle cell disease [1] .
Firivumab (CT-P22; CT120) is a human IgG1 monoclonal influenza A virus hemagglutinin (Anti-IAV HA) antibody. Firivumab is capable of neutralizing H1N1, H5N1, H6N1, H6N2, H8N4, H8N8, H9N2 and H12N7. Firivumab shows protection against H1N1 virus in mice[1] .
CTX-2026 is a fully human antibody that binds to CD277. CTX-2026 shows an anti-tumor effect on ovarian tumor models. CTX-2026 can be used for the research of cancer [1].
Teplizumab (MGA-031) is a Fc receptor non-binding anti-human CD3 monoclonal antibody. Teplizumab reduces the loss of beta-cell function. Teplizumab can be used in the research of type 1 diabetes [1] .
Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia [1].
Alirocumab (REGN 727) is a human monoclonal antibody inhibitor of PCSK9. Alirocumab is a monoclonal antibody. Alirocumab has anti-inflammatory, antiangiogenic and antioxidant effects. Alirocumab can be used in the study of hypercholesterolemia [1] .
Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19 [1] .
Landogrozumab (LY2495655) is an humanized anti-myostatin monoclonal antibody. Landogrozumab effectively improves muscle volume, hand grip strength and function. Landogrozumab can be used for the research of muscle wasting disease [1].
3,3-Dimethyl-1-butanol (DMB) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-Dimethyl-1-butanol inhibits the signaling pathway of p65 NF-κB and TGF-β1/Smad3. 3,3-Dimethyl-1-butanol has potential applications in cardiovascular disease (CVD) [1] .
Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is an orally active mycotoxin produced by Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1] .
(±)-Pantothenic acid ((±)-Pantothenate), a B-vitamin, is an essential vitamin required for the biosynthesis of coenzyme A (CoA) in mammalian cells. Pantothenic acid has protective activity against valproic acid (VPA)-induced neural tube defects (NTD) in CD-1mice[1].
Spilanthol is an orally active analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial and insecticidal compound.pilanthol can induce cAMP to inhibit negative regulation of urinary concentration mechanism. Spilanthol can be use as diuretic research [1] .
Borapetoside E can be isolated from T. crispa. Borapetoside E improves hyperglycemia, insulin resistance, hepatic steatosis, hyperlipidemia, and oxygen consumption in obese mice. Borapetoside E also inhibits SREBPs expression in the liver and adipose tissue [1].
Estradiol benzoate (β-Estradiol 3-benzoate) is a HBx protein inhibitor and inhibits androgen and hepatitis B virus (HBV) transcription, replication. Estradiol benzoate shows antifertility effects, anti- Toxoplasma gondii activity and can improve memory behavior of Ovariectomy (Ovx) female mice[1] .
L-Sepiapterin (Sepiapterin) is a precursor of the endothelial nitric oxide synthase (eNOS) cofactor tetrahydrobiopterin (BH4). L-Sepiapterin improves endothelial dysfunction in small mesenteric arteries from db/db mice, and induces angiogenesis. L-Sepiapterin inhibits cell proliferation and migration of ovarian cancer cells via down-regulation of p70 S6K-dependent VEGFR-2 expression [1] .
Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction [1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .
Pulchinenoside A is a natural triterpenoid saponin that enhances synaptic plasticity in the adult mouse hippocampus and facilitates spatial memory in adult mice.
D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell. D-panthenol exhibits nephroprotective effect in AKI, promotes tissue repair and regeneration.
Dibutyl maleate, the diester of the Maleic Acid, can be used as an intermediate of pharmaceutical synthesis. Dibutyl maleate can enhance contact sensitization to Fluorescein isothiocyanate in mice[1].
Juncusol, a phenanthrenoid found in Juncus setchuenensis, possesses anxiolytic effect. Juncusol is associated with metabolic changes in cortical serotonin/dopamine levels in Mice[1].
Tilifodiolide ((-)-Tilifodiolide) is a lactone, which can be isolated from the roots of Salvia tiliaefolia. Tilifodiolide has anti-inflammatory activity in mice model [1].
Mahanimbine is an orally active alkaloid from Murraya koenigii. Mahanimbine inhibits progression of high-fat diet (HFD)-induced metabolic complications in mice[1].
9,10-Dihydroxystearic acid is an oxidation product of oleic acid. 9,10-Dihydroxystearic acid can improve glucose tolerance and insulin sensitivity in KKAy mice[1].
Phenazoviridin is a free radical scavenger. Phenazoviridin shows strong inhibitory activity against lipid peroxidation in rat brain homogenate and exhibits antihypoxic activity in mice[1].
3-Methylhistamine dihydrochloride is a degradation product of histamine. 3-Methylhistamine dihydrochloride, a methylated product of histamine, is associated with immune response and shows upregulation in the vaccinated mice[1] .
Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice[1].
Wilfortrine is a bioactive sesquiterpene alkaloid. Wilfortrine exhibits immunosuppresive effects. Wilfortrine also can inhibit leukaemia cell growth in mice and shows anti-HIV activity [1].
Feruloyl tyramine, an amide compound, can be isolated from ethanol extract of hemp seed. Feruloyl tyramine injected into the lateral ventricle caused hypothermia and dyskinesia in mice[1].
SY-640 is an Acetamide derivative and has potent hepatoprotective effect. SY-640 reduces Propionibacterium acnes and Lipopolysaccharide-induced liver injury in mice[1] .
Neoechinulin A is an isoprenyl indole alkaloid that exhibits scavenging, neurotrophic factor-like, and anti-apoptotic activities. Neoechinulin A induces memory improvements and antidepressant-like effects in mice[1] .
Glycyrin is a PPAR-γ ligand of licorice. Glycyrin can decrease the blood glucose levels of genetically diabetic mice. Glycyrin also shows antibacterial activity [1] .
Pseudoginsenoside F11 (Ginsenoside A1), a component of Panax quinquefolium (American ginseng), has been demonstrated to antagonize the learning and memory deficits induced by scopolamine, morphine and methamphetamine in mice.
Cytochalasin C is a cell-permeable fungal toxin and induces the formation of nuclear rodlets. Cytochalasin C is 10 times less toxic in mice than is cytochalasin D [1] .
Uvaol, a triterpene present in olives and virgin olive oil, possesses anti-inflammatory properties and antioxidant effects. Uvaol attenuates pleuritis and eosinophilic inflammation in ovalbumin-induced allergy in mice[1].
Aurodox is an antibiotic obtained from a streptomyces variant, Aurodox can against a number of gram-positive bacteria. Aurodox shows a very low toxicity in mice and promoted poultry growth [1].
Rubicordifolin is a natural product that can be isolated from Rubia cordifolia. Rubicordifolin inhibits the growth of sarcoma ascites in mice. Rubicordifolin has significant cytotoxic activity both in vitro and in vivo [1].
Digitoxose (D-(+)-Digitoxose), a natural product, specifically and competitively inhibits glucose-stimulated insulin release from islets in lean and obese mice. Digitoxose can be used in diabetes research [1].
Isocampneoside I is an acylated phenethyl oligosaccharide that can be isolated from Cistanche deserticola (Orobanchaceae). Isocampneoside I inhibits D-galactose-induced cytotoxicity and protects primary hepatocytes in mice[1].
Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α [1].
Neocurdione is a hepatoprotective sesquiterpene isolated from Curcuma zedoaria rhizome. Neocurdione exerts potent effect on D-galactosamine- (D-Gain) and lipopolysaccharide- (LPS) induced acute liver injury in mice[1].
Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside is a orally active phenolic compound that can be isolated from the Geranium species. Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside has anti-inflammatory activities and has potential application in edema and aortic endothelium-dependent relaxation injury [1].
β-Maaliene can be isolated from the fresh leaves of Vitex densiflora (Maaliene) and is the main component in the isolate. β-Maaliene can significantly reduce the exercise capacity of mice at certain doses [1].
Pterosin A is an orally active anti-diabetic agent. Pterosin A promotes glucose uptake, increases serum insulin, and improves hyperglycemia and glucose intolerance in diabetic mice. Pterosin A can be isolated from Pteridium aquilinum[1] .
Bruceantin(NSC165563) is first isolated from Brucea javanica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.
Plantamajoside is a phenylpropanoid glycoside isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside has protective effects on LPS-induced acute lung injury (ALI) mice model. Plantamajoside has the potential for the treatment of pulmonary inflammation [1].
Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application [1].
Eucommiol is a natural product that can be isolated from the roasted leaves of E. ulmoides. Eucommiol inhibits growth of Molt 4B cells. Eucommiol reduces spontaneous activity and increases the sleep ratio in mice[1] .
Volvaltrate B is an anticancer agent, iridoid, can be obtained from the root of valerian (Valeriana officinalis). Volvaltrate B is effective against ovarian tumors in female mice. Volvaltrate B has the potential to study cancer [1] .
Lividomycin A is a broad-spectrum aminoglycoside antibiotic. Lividomycin A shows antimicrobial activity. Lividomycin A shows a positive protecting effect for the experimental infections in mice with several bacteria such as S. aureus, P. aeruginosa, Klebsiella pneumoniae and Escherichia coli[1].
(E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice[1].
Kadsurin, a natural compound from the stems of Kadsura heteroclita (Schizandraceae), results in significant decreases of CCL4- induced lipid-peroxidation products, such as thiobarbituric acid reactive substances (TBA-RS), conjugated dienes and fluorescent products in the liver of mice[1].
Andrographiside is a labdane diterpenoid glucoside that can be isolated from the leaves of Andrographis paniculata Nees. Andrographiside has antihepatotoxic and antioxidative effects. Andrographiside shows protective effects on mice with hepatotoxicity induced by carbon tetrachloride or tert-butylhydroperoxide (tBHP) [1].
Bruceine E is a quassinoid from seeds of Brucea javanica (L.) Merr, exhibiting hypoglycemia effect [1]. Bruceine E exhibits blood glucose lowering effect in both nondiabetic mice and Streptozotocin (STZ)-induced diabetic rats at lower dose .
Cupressuflavone is a natural product that can be found in Cupressus macrocarpa. Cupressuflavone exhibits anti-inflammatory and antiulcerogenic activities. Cupressuflavone also show protective effects against CCl4-induced hepato- and nephrotoxicity in mice[1] .
Gymnoside I (compound 1) is a glycosidoxybenzyl 2-isobutylmalic acid. Gymnoside I shows antiallergic activity in passive cutaneous allergic reaction (PCA) in mice. Gymnoside I can be used in research to treat asthma, neurasthenia and chronic hepatitis [1].
Hedragonic acid is an oleane-type triterpenoid compound, which can be isolated from the stems and roots of the southern snake vine. Hedragonic acid is a ligand and agonist for FXR. Hedragonic acid protected mice from liver damage caused by acetaminophen overdose and reduced liver inflammation [1].
Chebulanin, a polyphenol acid, exerts its anti-inflammatory and anti-arthritic effects via inhibiting NF-κB and MAPK activation in collagen-induced arthritis mice. Chebulanin inhibits the nuclear translocation of p38 and p65 in LPS-stimulated macrophages [1].
γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).
Platycoside E is a platycodigenin-type saponin isolated from the root of Platycodon grandiflorum with haemolytic activity and adjuvant potential. Platycoside E promotes the production of the sera OVA-specific IgG2a and IgG2b antibody in the ovalbumin (OVA)-immunized mice[1].
FR-901235 is a new type of immunoactive substance produced by an imperfect fungus, Paecilomyces carneus F-4882. FR-901235 partially restored the impaired delayed-type hypersensitivity to sheep red blood cells in tumor-bearing mice[1].
8-Epidiosbulbin E acetate, a furanoid, is abundant in Dioscorea bulbifera L.. 8-Epidiosbulbin E acetate exhibits broad-spectrum plasmid-curing activity against multidrug-resistant (MDR) bacteria. 8-Epidiosbulbin E acetate induces liver injury in mice[1] .
Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice[1].
Strictosidinic acid, an orally active glycoside indole monoterpene alkaloid isolated from Psychotria myriantha leaves, inhibits precursor enzymes of 5-HT biosynthesis and reduces the 5-HT levels. Strictosidinic acid has peripheral analgesic and antipyretic activities in mice[1] .
Cinnamtannin A2, a tetrameric procyanidin, can increases GLP-1 and insulin secretion in mice. Cinnamtannin A2 could upregulate the expression of corticotrophin releasing hormone. Cinnamtannin A2 exhibits antioxidant, anti-diabetic and nephroprotective effect [1] .
Flaccidoside II inhibits proliferation and induces apoptosis in Malignant peripheral nerve sheath tumors (MPNSTs) cell lines. Flaccidoside II ameliorates collagen-induced arthritis in mice. Flaccidoside II is an active triterpenoid saponin constituent from Anemone flaccida rhizome [1] .
Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning [1] .
Hyptadienic acid is a triterpene acid that can be isolated from the leaves of Perilla frutescens. Hyptadienic acid inhibits 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice with an ID50 value of 0.13 mg/ear. Hyptadienic acid can be used for the research of inflammation [1].
Verazine ((-)-Verazine) is an anti-Fungal Agent that can be found in the dried roots and rhizoma of Veratrum maackii Regel. Verazine causes DNA damage in the cerebellum and cerebral cortex of mice in a dose-dependent manner. Verazine can be used in the study of fungal infections and neurological diseases [1] .
Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades [1].
Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD) [1] .
Demethyleneberberine chloride is a natural mitochondria-targeted antioxidant. Demethyleneberberine chloride alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine chloride could serve as a AMPK activator for researching non-alcoholic fatty liver disease (NAFLD) [1] .
Fulvotomentoside B is a saponin isolated from Lactobacillus flavus. Fulvotomentoside compounds can significantly reduce serum glutamate pyruvate transaminase (SGPT) and triacylglycerol (GT) levels in mice poisoned by CCl4, d-galactosamine (d-gal) and acetaminophen, and significantly alleviate liver pathology. damage [1].
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase[1].
Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1] .
Celosin I, an oleanane-type triterpenoid saponin isolated from the seeds of Celosia argentea L, could be used as chemical markers for the quality control of C. argentea seeds. Celosin I exhibits significant hepatoprotective effect on carbon tetrachloride-induced and N,N-dimethylformamide-induced hepatotoxicity in mice[1] .
Tridocosahexaenoylglycerol (TG-DHA) is an orally active dietary supplement that improves autoimmune encephalomyelitis in mice. Tridocosahexaenoylglycerol shows beneficial effects on neurodegenerative diseases and also improves macular function in diabetic retinopathy. Tridocosahexaenoylglycerol can be used for research on neurological diseases, inflammatory immune diseases, and metabolic diseases [1] .
YC-001 is an inverse agonist and antagonist of rod opsin. YC-001 reversibly binds rod opsin and stabilizes the rod opsin structure. YC-001 protects mice from bright light-induced retinal degeneration. YC-001 has the potential for the research of retinal degeneration [1].
3β-Hydroxylanosta-8,24-dien-21-al is a lanostane-type triterpene. 3β-Hydroxylanosta-8,24-dien-21-al can inhibit the tumor promotion, reducing the percentage of mice bearing papillomas [1].
D-Mannose is a C-2 superpolymer of glucose that occurs naturally in many plants and fruits. D-Mannose has anti-inflammatory and antitumor activity. D-Mannose plays an important role in immune regulation [1] .
NADH-IN-1 has NADH:ubiquinone oxidoreductase inhibitory activity with an IC50 value of 27 μM. NADH-IN-1 can effectively stimulate glucose uptake in vitro. NADH-IN-1 is readily metabolised by the liver. NADH-IN-1 can be used for researching diabetes [1].
5-Methoxycanthin-6-one is an orally active inhibitor of Leishmania strains. 5-Methoxycanthin-6-one shows cytotoxicity with an IC50 of 5.44 μg/mL against Ailanthus altissima cells [1] .
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice[1] .
Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[1] .
Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases [1] .
Albofungin (Antibiotic P-42-1) is isolated from the culture filtrate of Actinomyces tumemacerans strain INMI.P-42. Albofungin shows highly active on a wide variety of gram-positive bacteria and fungi. Albofungin shows cytotoxic to HeLa cell cultures and exhibited antitumor activity on EHRLICH ascites tumor in mice.
7-Deoxy-trans-dihydronarciclasine, an alkaloid, is a tobacco mosaic virus (TMV) inhibitor (IC50: 1.80 μM). 7-Deoxy-trans-dihydronarciclasine is an anti-neuroinflammatory agent. 7-Deoxy-trans-dihydronarciclasine decreases the Aβ and APP levels in the cerebral cortex of Tg2576 mice[1] .
7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro [1].
Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice[1] .
AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity [1] . AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway .
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice[1] .
Suffruticosol A is a neuroprotective agent that restores scopolamine-induced cellular neurodegenerative damage. Suffruticosol A ameliorates hippocampal cholinergic deficits and partially enhances BDNF signaling. Suffruticosol A has neuromodulatory effects in a Scopolamine (HY-N0296)-induced model, restoring memory and cognitive performance in mice. Suffruticosol A can be isolated from seeds of P. lactiflora [1].
CMPF can be found in trace constituent of urine and blood. CMPF is a biomarker of type 2 diabetes. CMPF can act on the β cell and induces impaired mitochondrial function. CMPF decreases glucose-induced ATP accumulation, and induces oxidative stress. CMPF reverses hepatic lipid accumulation and improves insulin sensitivity in obese mice[1] .
Stevisalioside A (Compound 2) can be isolated from Stevia serrata roots. Stevisalioside A is an orally active antidiabetic agent. Stevisaliosides A inhibits PTP1B (IC50: 526.8 μM). Stevisalioside A reduces blood glucose levels and the postprandial peak in oral glucose and insulin tolerance tests in Streptozotocin (HY-13753) induced hyperglycemic mice[1].
Benzyl alcohol (Standard) is the analytical standard of Benzyl alcohol. This product is intended for research and analytical applications. Benzyl alcohol is an aromatic alcohol, a colorless liquid with a mild aromatic odor. Benzyl alcohol is an inhibitor of P450 enzyme. Benzyl alcohol mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice[1] .
Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM [1] . Apocynin improves acute lung inflammation in Carrageenan (HY-125474)-induced pleurisy mice model . Apocynin can also be used for cancer research . Apocynin reverses the aging process in mesenchymal stem cells to promote osteogenesis and increases bone mass .
13-Oxo-9E,11E-octadecadienoic acid, an isomer of 9-oxo-ODA, is a potent PPARα activator derived from tomato juice. 13-Oxo-9E,11E-octadecadienoic acid decreases plasma and hepatic triglyceride in obese diabetic mice[1].
Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature [1].
Corydalmine (L-Corydalmine) inhibits spore germination of some plant pathogenic as well as saprophytic fungi [1]. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity . Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway .
Taxamairin B is a potent anti-inflammatory agent. Taxamairin B decreases proinflammatory cytokines (TNF-α, IL-1β and IL-6) expression and the production of NO and ROS in LPS-induced RAW264.7 cells. Taxamairin B exhibits significant
protective effects in LPS-induced acute lung injury in mice[1] .
Isozaluzanin C (Dehydrozaluzanin c-derivative) is an anti-inflammatory agent that can be isolated from Saussurea lappa and has immunomodulatory effects. Isozaluzanin C improves tissue damage (lung, kidney, and liver) and excessive inflammation in mice induced by LPS (HY-D1056) or CRKP infection. Isozaluzanin C can be used in the study of bacterial infections and sepsi [1] .
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity [1]. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice .
NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser 70 and c-Myc at Thr 58 and Ser 62 through activation of both ERK1/2 and PKCα[1]. NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
3-tert-Butyl-4-methoxyphenol is a PROTAC linker, belongs to alkyl/ether class, with insecticidal activity. 3-tert-Butyl-4-methoxyphenol also induced increased activities of glutathione (GSH) S-transferase and epoxide hydrolase in the liver and forestomach tissues of A/HeJ mice, regulating the carcinogen metabolism system [1] .
Fortunellin, is a flavonoid, that can be isolated from the fruits of Fortunella margarita (kumquat). Fortunellin exhibits little toxicity to mice and suppresses inflammation and ROS generation in H9C2 cells induced by LPS. Fortunellin protects against fructose-induced inflammation and oxidative stress by enhancing AMPK/Nrf2 pathway. Fortunellin can be used for diabetic cardiomyopathy research [1].
Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells [1].
7-aminocephalosporanic acid (7-ACA) is a HSP90β inhibitor and an antibiotic. 7-Aminocephalosporanic acid is the core chemical structure of the synthesis of cephalosporin antibiotics and an effective β-lactamase inhibitor [1] .
Rubusoside is a diterpene glycoside that is also a sweetener and solubilizer with anti-angiogenic, anti-cancer, anti-obesity, anti-allergic and anti-asthmatic effects. Rubusoside attenuates airway hyperresponsiveness and reduces inflammatory cells in bronchoalveolar lavage fluid (BALF), reducing OVA (HY-W250978)-induced airway inflammation. Rubusoside also prevents palmitic acid-induced lipotoxicity in pancreatic INS-1 cells, reduces the transport of human glucose transporters GLUT-1 and fructose GLUT-5, and inhibits NF-κB and α-amylase (α-amylase) [1] .
Psychotridine is a natural alkaloid isolated from Psychotria colorata, reveals an analgesic activity in nervous system and an inhibitory efficacy towards platelet aggregation [1] .
Diacerein (Diacerhein), an orally active anthraquinone, reduces production of IL-1 converting enzyme then inhibits the activation of IL-1β by related downstream signaling. Diacerein is an anti-inflammatory and anti-rheumatic drug. Diacerein can relieve bronchospasm and control airway inflammation in asthmatic mice. Diacerein has the potential for slow acting drug in osteoarthritis (SYSADOA) research [1] .
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active [1] .
Cabenoside D (compound 8) is a triterpenoid glycoside, which can be isolated from the methanol extract of lichen root. Cabenoside D shows anti-inflammatory activity and inhibits inflammation induced by 12-O-tetracylacyl hormone-13-acetate (TPA) in mice. Cabenoside D also inhibits TPA-induced Epstein-Barr virus (EBV) early antigen (EBV-EA) activation [1].
Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory [1].
Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation .
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure [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] .
9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation. 9-PAHSA also improved carotid vascular calcification and attenuates cardiac hypertrophy and dysfunction in db/db mice. 9-PAHSA increases the viability of steatosis primary mouse hepatocytes (PMH). 9-PAHSA can be used in research on diabetes, inflammation, and cardiovascular disease [1] .
8-prenylnaringenin is a prenylflavonoid isolated from hop cones Humulus lupulus, with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice[1] .
Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research [1] .
DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone is orally active against HMGCR mutation and statin caused myopathy . DL-Mevalonolactone induces inflammation and oxidative stress response with decreased mitochondrial membrane potential (MMP) and induces mitochondrial swelling [2][4].
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis[1] .
(+)-Butin is the R enantiomer of Butin. Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities [1].
Deacetylasperulosidic acid (DAA) is a major phytochemical constituent of Morinda citrifolia fruit. Deacetylasperulosidic acidhas antioxidant activity by increasing superoxide dismutase activity. Deacetylasperulosidic acid has anticlastogenic activity, suppressing the induction of chromosome aberrations in hamster ovary cells and mice[1]. Deacetylasperulosidic acid prevents 4-nitroquinoline 1-oxide (4NQO) induced DNA damage in vitro, suppresses IL-2 production along with the activation of natural killer cells .
2,7"-Phloroglucinol-6,6'-bieckol is an orally active dual α-amylase/α-glucosidase inhibitor with IC50 values of 6.94 μM and 23.35 μM respectively. 2,7"-Phloroglucinol-6, 6'-bieckol alleviates postprandial hyperglycemia in diabetic mice. 2,7"-Phloroglucinol-6,6'-bieckol can be used in diabetes research [1].
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 [1]. (Z)-Ligustilide inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans[1] .
Forsythiaside A is an orally active phenylethanoid glycoside isolated from the dried fruits of Forsythia suspensa. Forsythiaside A is also an inhibitor of COX-2 and has anti-inflammatory, antioxidant and neuroprotective effects. Forsythiaside A prevents neuroinflammation and apoptosis caused by Aβ25-35 damage and may be used in Alzheimer's disease (AD) research. Forsythiaside A also activates the Nrf2/HO-1 signaling pathway and inhibits OVA-induced asthma in mice[1] .
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains [1] .
L-Glutamic acid monosodium salt is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid monosodium salt has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid monosodium salt can be used in the study of neurological diseases [1] .
L-Glutamic acid is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid can be used in the study of neurological diseases [1] .
L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer [1] .
Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research [1] .
Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca 2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca 2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca 2+ signaling in neuronal and nonneuronal cells [1] .
Ompenaclid (RGX-202) is an oral small-molecule SLC6A8 transporter inhibitor. Ompenaclid robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. Ompenaclid can be used for the research of cancer and duchenne muscular dystrophy [1] .
Methyl isoeugenol (MIE) is a natural food flavour that can be isolated from Pimenta pseudocaryophyllus leaf. Methyl isoeugenol shows anxiolytic and antidepressant like effects. Methyl isoeugenol is orally active [1].
L-Octanoylcarnitine hydrochloride is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine hydrochloride can be used for the research of breast cancer [1] .
Napyradiomycin B4 is a Napyradiomycin derivative, which inhibits the RANKL-induced MEK-ERK signaling pathway. Napyradiomycin B4 attenuates osteoclastogenesis and prevents alveolar bone destruction in experimental periodontitis [1].
C30(ω-hydroxy) Ceramide (d18:1/30:0), a sphingolipid, is an epidermis-specifically vital component of the water barrier in mammalian skin. C30(ω-hydroxy) Ceramide (d18:1/30:0) is expressed in epidermal keratinocytes and male germ cells during their differentiation and maturation. C30(ω-hydroxy) Ceramide (d18:1/30:0) deficiency in the epiderm of Elovl4 deletion or mutation mice[1] .
5-Heptadecylresorcinol (AR-C17), a phenolic lipid component, is also an orally active mitochondrial protector. 5-Heptadecylresorcinol improves mitochondrial function via sirtuin3 signaling pathway, thus alleviates endothelial cell damage and apoptosis. 5-Heptadecylresorcinol induces sirtuin3-mediated autophagy. 5-Heptadecylresorcinol reduces the atherosclerotic plaques in the aortic root region of mice heart. 5-Heptadecylresorcinol can be used for research of atherosclerosis prevention and obesity [1] .
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10 [1] .
3'-Sialyllactose (3'-SL) is a prebiotic, maintains immune homeostasis and exerts anti-inflammatory and anti-arthritic effects. 3'-Sialyllactose is an ordinary carbohydrate with the lowest toxicity rating, it can be used for the research of inflammation [1] .
Valnemulin is an orally active broad-spectrum antibiotic against Gram-negative and Gram-positive bacteria, anaerobic bacteria, Mycoplasma, and Spirochetes. Valnemulin ameliorates enteric diseases, acute polyarthritis and enzootic pneumonia in pigs [1]. Valnemulin exhibits anti-inflammatory efficacy against lipopolysaccharide (HY-D1056)-induced lung injury .
4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitory activities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects [1] .
9AzNue5Ac, 9-azido-9-deoxy-N-acetylneuraminic acid, is a click chemistry reagent and a Neu5Ac analogue with the substitution of 9-hydroxyl group with an azide. 9AzNue5Ac could be metabolized and incorporated into sialoglycans in living cells and mice. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity [1].
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model [1] .
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator [1] . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model [1] .
Valinomycin is a potassium-specific ionophore, the valinomycin-K + complex can be incorporated into biological bilayer membranes with the hydrophobic surface of valinomycin, destroys the normal K + gradient across the membrane, and as a result kills the cells, incorporating into liposomes can significantly reduces the cytotoxicity and enhances the targeting effect. Valinomycin exhibits antibiotic, antifungal, antiviral, antitumor and insecticidal efficacy, thus can be used for relevant research [1] .
Emodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction [1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects . Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice .
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator [1] . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1(AdipoR1;Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) [1] .
Feralolide is a dihydroisocoumarin isolated from the methanolic extract of aloe vera resin. Feralolide is also a dual inhibitor of AChE and BuChE, with IC50s of 55 μg/mL and 52 μg/mL respectively. Feralolide has antioxidant activity and inhibits 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2′-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS). Feralolide could be used in research into cognitive disorders such as Alzheimer's disease, potentially restoring and enhancing memory [1].
1,11b-Dihydro-11b-hydroxymedicarpin (11b-Hydroxy-11b,1-dihydromedicarpin) is a pterocarpan from Ononis viscosa subsp. breviflora is a Medicarpin derivative [1]. Medicarpin, a natural pterocarpan, heals cortical bone defect by activation of Notch and Wnt canonical signaling pathways . Medicarpin prevents arthritis in post-menopausal conditions by arresting the expansion of TH17 cells and pro-inflammatory cytokines. Medicarpin down-regulates pro-inflammatory cytokines like TNF-α, IL-6 and IL-17A, while up-regulates anti-inflammatory cytokine IL-10 in arthritis (CIA) model of mice .
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice[1].
Penicillamine (D-(-)-Penicillamine) is a penicillin metabolic degradation product, can be used as a heavy metal chelator. Penicillamine reduces free copper and reduces oxidative stress. Penicillamine has effect of seizures through nitric oxide/NMDA pathways. Penicillamine is a potential immune modulator. Penicillamine can be used for the research of Wilson disease, rheumatoid arthritis, and cystinuria [1] .
Diallyl Trisulfide is an orally active anticancer agent that can be isolated from garlic. Diallyl Trisulfide has the ability to induce apoptosis and exhibits anticancer, anti-inflammatory, antioxidant, and antibacterial activities. Diallyl Trisulfide can be used to study a variety of cancers, including liver, colon and prostate cancer [1] .
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM [1]. Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
Benzosceptrin C is an inhibitor for PD-L1, which promotes programmed cell death ligand (PD-L1) degradation in a lysosomal pathway, enhances the cytotoxicity of T-cells and exhibits antitumor activity [1].
T-2 Toxin (T-2 Mycotoxin) is a toxic trichothecene mycotoxin produced by various Fusarium species in feedstuffs and cereal grains, LD50 values of T-2 Toxin in mice and rats are 5.2 and 1.5 mg/kg BW a,respectively [1]. T-2 Toxin (T-2 Mycotoxin) can be transformed into a variety of metabolite, the typical metabolites of T-2 toxin in animals are HT-2 toxin and T-2-triol, which are hydrolysates [1]. T-2 Toxin (T-2 Mycotoxin) is an inhibitor of protein synthesis resulting from binding peptidyltransferase, which is an integral part of the 60s ribosomal subunit. T-2 Toxin (T-2 Mycotoxin) inhibits the synthesis of DNA and RNA, interferes with the metabolism of membrane phospholipids, and increases the level of liver lipid peroxides [1]. T-2 Toxin (T-2 Mycotoxin) induces apoptosis in the immune system, gastrointestinal tissues, and fetal tissues .
Pinostrobin is a flavonoid with anti-cancer, antioxidant, antiviral and neuroprotective activities. Pinostrobin has oral activity. Pinostrobin is a potent PCSK9 inhibitor that inhibits the catalytic activity of PCSK9. Pinostrobin can be used in the research of viral infections, cancer, leukemia, cardiovascular and cerebrovascular diseases, cirrhosis, inflammation and neurological diseases [1] .
Peimine (Verticine; Dihydroisoimperialine) is an orally active natural product. Peimine has anti-inflammatory, analgesic and cough relieving effects. Peimine can be used in cancer and inflammation related research [1] .
Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis [1] .
Anethole is a type of orally active aromatic compound that is widely found in nature and used as a flavoring agent. Anethole possesses anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, anesthetic, estrogenic, central nervous system depressant, hypnotic, insecticidal, and gastroprotective effects. Anethole can be used in the study of oxidative stress-related skin diseases and prostate cancer [1] .
The CD1B protein is a key antigen-presenting molecule that binds self- and non-self lipid and glycolipid antigens and presents them to T-cell receptors on natural killer T cells. As a B2M (beta-2-microglobulin) heterodimer, CD1B is crucially involved in immune surveillance and responses. CD1B Protein, Human (HEK293, Fc) is the recombinant human-derived CD1B protein, expressed by HEK293 , with C-hFc labeled tag. The total length of CD1B Protein, Human (HEK293, Fc) is 286 a.a., with molecular weight of 60-90 kDa.
The CD1A protein is a key antigen-presenting molecule that binds self and non-self lipid and glycolipid antigens and presents them to T cell receptors on natural killer T cells. CD1A, as a B2M (beta-2-microglobulin) heterodimer, plays a central role in immune surveillance and regulation. CD1A Protein, Human (HEK293, His) is the recombinant human-derived CD1A protein, expressed by HEK293 , with C-His labeled tag. The total length of CD1A Protein, Human (HEK293, His) is 282 a.a., with molecular weight of 48-53 kDa.
The CD1D protein, a key antigen-presenting molecule, binds self and non-self glycolipids, presenting them to T-cell receptors on natural killer T-cells. Partnering with B2M, it centrally orchestrates immune responses, and its interactions with MHC II emphasize its significance in the intricate network of immune system regulation. CD1D Protein, Human (HEK293, His) is the recombinant human-derived CD1D protein, expressed by HEK293, with C-His labeled tag. The total length of CD1D Protein, Human (HEK293, His) is 301 a.a., with molecular weight of 45-50 kDa.
CD1D protein, in partnership with B2M, functions as an antigen-presenting protein, binding self and non-self glycolipids. It presents these molecules to T-cell receptors on natural killer T-cells, playing a pivotal role in immune responses. CD1D also interacts with MHC II and CD74, contributing to the coordination of the adaptive immune system. CD1D Protein, Mouse (HEK293, His) is the recombinant mouse-derived CD1D protein, expressed by HEK293 , with C-His labeled tag. The total length of CD1D Protein, Mouse (HEK293, His) is 305 a.a., with molecular weight of 45-50 kDa.
CD1D protein, in partnership with B2M, functions as an antigen-presenting protein, binding self and non-self glycolipids. It presents these molecules to T-cell receptors on natural killer T-cells, playing a pivotal role in immune responses. CD1D also interacts with MHC II and CD74, contributing to the coordination of the adaptive immune system. CD1D Protein, Mouse (HEK293, His-Fc) is the recombinant mouse-derived CD1D protein, expressed by HEK293 , with C-hFc, C-His labeled tag. The total length of CD1D Protein, Mouse (HEK293, His-Fc) is 305 a.a., with molecular weight of ~60.4 kDa.
CD1D protein, in partnership with B2M, functions as an antigen-presenting protein, binding self and non-self glycolipids. It presents these molecules to T-cell receptors on natural killer T-cells, playing a pivotal role in immune responses. CD1D also interacts with MHC II and CD74, contributing to the coordination of the adaptive immune system. CD1D1-B2M Heterodimer Protein, Mouse (HEK293, His) is a recombinant protein dimer complex containing mouse-derived CD1D1-B2M Heterodimer protein, expressed by HEK293, with C-His labeled tag. CD1D1-B2M Heterodimer Protein, Mouse (HEK293, His), has molecular weight of ~33.7 & 11.7 KDa, respectively.
The CD1D2 protein plays a crucial role as an antigen-presenting molecule, binding self and non-self glycolipids and presenting them to T-cell receptors on natural killer T-cells. In partnership with B2M, it mediates immune responses, and its interactions with MHC II and CD74 highlight its significance in the complex network of immune system regulation. CD1D2-B2M Heterodimer Protein, Mouse (HEK293, His) is a recombinant protein dimer complex containing mouse-derived CD1D2-B2M Heterodimer protein, expressed by HEK293, with C-His labeled tag. CD1D2-B2M Heterodimer Protein, Mouse (HEK293, His), has molecular weight of ~33.7 & 11.7 KDa, respectively.
CD1B belongs to family 1 of the transmembrane glycoprotein CD1 family and plays a critical role in immune surveillance and response. As a key antigen-presenting molecule, CD1B protein has shown the ability to bind both self and non-self-lipid and glycolipid antigens. CD1B is a potential prognostic biomarker associated with tumor mutation burden and promotes antitumor immunity in lung adenocarcinoma. CD1B-B2M Heterodimer Protein, Rhesus Macaque (HEK293, His) is a recombinant protein dimer complex containing Rhesus Macaque-derived CD1B-B2M Heterodimer protein, expressed by HEK293 , with C-His labeled tag. CD1B-B2M Heterodimer Protein, Rhesus Macaque (HEK293, His), has molecular weight of ~38-45 & 12 KDa.
CD1C belongs to Group 1 of the transmembrane glycoprotein CD1 family. CD1C protein, as a key antigen-presenting molecule, has shown the ability to bind both self and non-self lipid and glycolipid antigens, mediating host defense against tuberculosis. CD1C is associated with breast cancer prognosis and immune invasion. CD1C-B2M Heterodimer Protein, Rhesus Macaque (HEK293, His) is a recombinant protein dimer complex containing Rhesus Macaque-derived CD1C-B2M Heterodimer protein, expressed by HEK293 , with C-His labeled tag. CD1C-B2M Heterodimer Protein, Rhesus Macaque (HEK293, His), has molecular weight of ~44.7 (33.1+ 11.6) KDa.
The CD1D protein, a key antigen-presenting molecule, binds self and non-self glycolipids, presenting them to T-cell receptors on natural killer T-cells. Partnering with B2M, it centrally orchestrates immune responses, and its interactions with MHC II emphasize its significance in the intricate network of immune system regulation. CD1D-B2M Heterodimer Protein, Human (HEK293, His) is a recombinant protein dimer complex containing human-derived CD1D-B2M Heterodimer protein, expressed by HEK293, with C-His labeled tag. CD1D-B2M Heterodimer Protein, Human (HEK293, His), has molecular weight of ~48 & 12 kDa, respectively.
The CCND1 protein is a regulatory component of the cyclin D1-CDK4 complex that coordinates phosphorylation and RB family inhibition to regulate the G(1)/S transition. This promotes the dissociation of E2F from the RB/E2F complex and promotes the transcription of E2F target genes critical for G(1) phase progression. CCND1 Protein, Human (His) is the recombinant human-derived CCND1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of CCND1 Protein, Human (His) is 295 a.a., with molecular weight of ~37.7 kDa.
TREM-2 Protein is an immune receptor expressed on immune and non-immune cells. It is an anti-inflammatory molecule and considered a marker for microglia activation. CD1E-B2M Heterodimer Protein, Cynomolgus (HEK293, His) is a recombinant protein dimer complex containing cynomolgus-derived CD1E-B2M Heterodimer protein, expressed by HEK293 , with N-His labeled tag. CD1E-B2M Heterodimer Protein, Cynomolgus (HEK293, His), has molecular weight of ~37.8 & 13.6 kDa, respectively.
Phenytoin-d10 is the deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[1][2].
DPPC-d9 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
DPPC-d62 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
DPPC-d9-1 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
Phenytoin- 15N2, 13C is the 13C and 15N labeled Phenytoin[1]. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[2][3].
Cytidine-5'-triphosphate- 13C,d1 (Cytidine triphosphate- 13C,d1 dilithium; 5'-CTP- 13C,d1) dilithium is deuterium and 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Oxolinic acid-d5 is the deuterium labeled Oxolinic acid. Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice[1][2][3].
Anserine-d4 is the deuterium labeled Anserine. Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1][2].
Citric acid- 13C3 is the 13C labeled Citric acid[1]. Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[2][3][4].
Paynantheine-d3 is a deuterium labeled Paynantheine. Paynantheine is an alkaloid that can be isolated from Mitragyna speciosa. Paynantheine can decrease alcohol intake in mice[1] .
Speciogynine-d3 is a deuterium labeled Speciogynine. Speciogynine is an alkaloid that can be isolated from Mitragyna speciosa. Speciogynine can decrease alcohol intake in mice[1] .
D-Glucose- 13C,d-1 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
Ac-rC Phosphoramidite- 13C,d1 is deuterium and 13C-labeled Ac-rC Phosphoramidite (HY-W042357). Ac-rC Phosphoramidite is used for the oligoribonucleotide phosphorodithioate modification (PS2-RNA).
Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) [1]. GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury [1] .
Odevixibat-d5 is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis [1].
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
Odevixibat- 13C6 is 13C labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis [1].
Paquinimod-d5 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice[1] .
Paquinimod-d5-1 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice[1] .
Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
Fmoc-leucine-d10 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
Anserine-d4 hydrochloride is the deuterium labeled Anserine (HY-113354). Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1] .
Citric acid- 18O is 18O-labeled Citric acid (HY-N1428) Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice.
Citric acid-d4-1 is deuterated labeled Citric acid (HY-N1428) Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice.
Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19 [1] .
Brassinolide-d5 (Brassin lactone-d5) is the deuterated labeled Brassinolide (HY-N0273). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[1] .
Menthofuran- 13C2 is 13C labeled Menthol (HY-N1369). Menthol is an analgesic and TRPM8 modulator. TRPM8 is a cold temperature sensing ion channel, and Menthol can regulate TRPM8 to exert analgesic and anti-irritation mechanisms. Menthol stimulates cold receptors and produces a cooling sensation by inhibiting Ca ++ currents in neuronal cell membranes. Menthol also improves oral nicotine rejection in mice[1] .
Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole-d3 is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1][2][3][4].
Angiotensin I- 13C5, 15N (human, mouse, rat) is the 13C and 15N labeled Angiotensin I (human, mouse, rat) (HY-P1032). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[1].
L-Octanoylcarnitine-d3 is the deuterium-labeled L-Octanoylcarnitine (HY-113161). L-Octanoylcarnitine-d3 is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine-d3 can be used for the research of breast cancer [1] .
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice[1] .
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1] .
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice[1] .
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis [1] . Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
S-Propargylcysteine (SPRC), a structural analog of S-allyl cysteine (SAC), is a slow H2S-releasing compound. S-Propargylcysteine reduces Ca 2+ accumulation and inflammatory cytokines, inhibits STAT3, and elevates p53 and Bax. S-Propargylcysteine has anti-inflammatory activity and protects mice against acute pancreatitis. S-Propargylcysteine also has cardioprotective, neuroprotective acitivties [1] .
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues [1]. PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
DH-376 is a potent diacylglycerol lipase inhibitor with pIC50 values of 8.6 and 8.9 for ABHD6 and DAGLα, respectively. DH-376 prevents fasting-induced refeeding of mice[1]. DH-376 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
9AzNue5Ac, 9-azido-9-deoxy-N-acetylneuraminic acid, is a click chemistry reagent and a Neu5Ac analogue with the substitution of 9-hydroxyl group with an azide. 9AzNue5Ac could be metabolized and incorporated into sialoglycans in living cells and mice. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity [1].
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