Search Result
Results for "
tissue selectivity
" in MedChemExpress (MCE) Product Catalog:
5
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-12023
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GTx-007
4 Publications Verification
S-4
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Androgen Receptor
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Cancer
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GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity .
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-
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- HY-117658
-
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MAP3K
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Cardiovascular Disease
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GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 μM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue .
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- HY-105318
-
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Androgen Receptor
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Metabolic Disease
Endocrinology
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LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction .
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- HY-U00178
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-
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- HY-14210
-
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Phosphatase
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Inflammation/Immunology
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TNAP-IN-1 (Compound 1) is a selective tissue-nonspecific alkaline phosphatase (TNAP) inhibitor, with an IC50 of 0.19 μM. TNAP-IN-1 can be used for the research of soft tissue calcification .
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- HY-135732
-
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Androgen Receptor
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Cancer
|
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SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity .
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- HY-119433
-
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J867
|
Progesterone Receptor
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Endocrinology
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Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human .
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-
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- HY-U00216
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-
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- HY-N9141
-
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5-HT Receptor
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Neurological Disease
|
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Nantenine is a serotonergic receptor antagonist. Nantenine selectively inhibits the contractile response of tissues to serotonin. Nantenine can be isolated from Nandina domestica .
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- HY-139852
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Phosphatase
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Cancer
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PLAP-IN-1 is a potent (IC50 = 32 nM) and selective PLAP inhibitor, with no detectable inhibition of tissue non-specific alkaline phosphatase (TNAP) activity.
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- HY-78144
-
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IAP
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Inflammation/Immunology
|
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4-Methylsalicylic acid is a salicylic acid. 4-Methylsalicylic acid derivative is a selective tissue-nonspecific alkaline phosphatase (TNAP) and intestinal alkaline phosphatase (IAP) inhibitor .
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- HY-130013
-
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Fluorescent Dye
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Others
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HKYellow-AM (6/12-mixture) is a yellow fluorescent probe that can detect ONOO- in living cells and tissues with high selectivity and sensitivity without cytotoxicity .
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- HY-119649
-
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IKI220
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Parasite
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Infection
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Flonicamid (IKI220) is a novel systemic insecticide with selective activity against hemipterous pests. The main insecticidal mechanism of flonicamid is starvation based on the inhibition of stylet penetration to plant tissues .
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-
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- HY-13273
-
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MK-2866; GTX-024; Enobosarm
|
Androgen Receptor
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Others
Cancer
|
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Ostarine (MK-2866) is a selective androgen receptor modulator (SARMs) that regulates cardiomyocyte function, improves bone healing, regulates uterine function, and influences muscle tissue metabolism .
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- HY-13556A
-
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LY353381 hydrochloride; SERM III hydrochloride
|
Estrogen Receptor/ERR
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Cancer
|
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Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
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- HY-115768A
-
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Poly-p-methoxyphenethylmethylamine (trimer)
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Phospholipase
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Others
|
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Compound 48/80 (trimer) is a trimer of Compound 48/80 (HY-115768). Compound 48/80 is widely used in animal and tissue models as a "selective" mast cell activator .
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- HY-126969
-
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PPAR
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Metabolic Disease
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C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
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- HY-N2304A
-
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Opioid Receptor
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Inflammation/Immunology
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Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioid receptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract .
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- HY-W062700
-
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JAK
|
Neurological Disease
|
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STS-E412 is a selective activator of tissue-protective EPO receptor (including EPOR and CD131). STS-E412 can be used for research of neurodegenerative diseases and organ protection .
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- HY-161835
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-
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- HY-N0457A
-
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(-)-Chicoric acid; trans-Caffeoyltartaric acid
|
HIV Integrase
HIV
Endogenous Metabolite
|
Infection
Cancer
|
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L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture .
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- HY-114056
-
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Others
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Cancer
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AS115 is a potent and selective KIAA1363 inactivator with IC50 value of 150 nM. KIAA1363 is a 2-acetyl monoacylglycerol ether (MAGE) hydrolase that is upregulated in aggressive cancers of various tissues .
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- HY-13738A
-
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Keoxifene hydrochloride; LY156758; LY139481 hydrochloride
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Estrogen Receptor/ERR
Autophagy
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Endocrinology
Cancer
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Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue .
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- HY-P10216
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Biochemical Assay Reagents
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Neurological Disease
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CAQK peptide selectively binds to injured mouse brain. CAQK peptide selectively targets demyelinating areas and it is absent from healthy tissue. The CAQK peptide target is a proteoglycan complex upregulated in brain injuries and is used for drug delivery. CAQK peptide can penetrate the blood-brain barrier .
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- HY-163146
-
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Fluorescent Dye
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Cancer
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TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
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- HY-131006
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Monoamine Transporter
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Neurological Disease
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FFN200 dihydrochloride, a fluorescent substrate of VMAT2, selectively trace monoamine exocytosis in both neuronal cell culture and brain tissue. The fluorescence excitation and emission maxima of FFN200 are determined to be 352 and 451 nm, respectively .
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- HY-P1473
-
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Amylin (8-37) (mouse, rat)
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Amylin Receptor
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Metabolic Disease
|
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Amylin (8-37), rat is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Amylin (8-37), rat is a weak amylin receptor (AMY) antagonist.
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- HY-134194
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KL201
1 Publications Verification
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Cryptochrome
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Metabolic Disease
|
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KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues .
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- HY-120017
-
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MD-370503
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Monoamine Oxidase
|
Neurological Disease
|
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Befloxatone (MD-370503) is an orally active, selective and reversible inhibitor of Monoamine Oxidase A (MAO-A) (IC50=4 nM). Befloxatone increases the tissue level of monoamine, striatal dopamine and cortical norepinephrine. Befloxatone has antidepressant potential .
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- HY-156820
-
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Epigenetic Reader Domain
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Cancer
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HLDA-221 is a heterobifunctional small molecules called Regulated Induced Proximity Targeting Chimeras (RIPTACs). HLDA-221 elicits a stable ternary complex between a target protein selectively expressed in cancer tissue and a pan-expressed protein essential for cell survival, thus leading to cell death selectively in cells expressing the target protein .
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- HY-163684
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Complement System
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Inflammation/Immunology
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Zoracopan is a selective complement factor D (CFD) inhibitor. When administered systemically (orally or intravenously), Zoracopan accumulates and is sustained-released in ocular tissues, primarily in the choroid-retinal pigment epithelium (C-RPE) and/or iridociliary body (I-CB) .
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- HY-P1407
-
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VRPR
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MALT1
Influenza Virus
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Infection
Cancer
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Z-VRPR-FMK (TFA) (VRPR), a tetrapeptide, is a selective and irreversible MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1) inhibitor. Z-VRPR-FMK (TFA) can protect against influenza A virus (IAV) infection .
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- HY-151425
-
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Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
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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 .
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- HY-12960
-
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FLT3-IN-1
|
FLT3
c-Kit
Apoptosis
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Cancer
|
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SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .
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- HY-172687
-
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Liposome
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Cardiovascular Disease
|
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DSPE-PEG2000-CSTSMLKAC is a PEG compound which composed of DSPE and a peptide (CSTSMLKAC). CSTSMLKAC is capable of mediating selective homing of phage to ischemic heart tissue. DSPE-PEG2000-CSTSMLKAC can be used for drug delivery .
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- HY-172686
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Liposome
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Cardiovascular Disease
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DSPE-PEG1000-CSTSMLKAC is a PEG compound which composed of DSPE and a peptide (CSTSMLKAC). CSTSMLKAC is capable of mediating selective homing of phage to ischemic heart tissue. DSPE-PEG1000-CSTSMLKAC can be used for drug delivery .
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- HY-120290
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Histone Acetyltransferase
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Cancer
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PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity .
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- HY-172688
-
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Liposome
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Cardiovascular Disease
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DSPE-PEG5000-CSTSMLKAC is a PEG compound which composed of DSPE and a peptide (CSTSMLKAC). CSTSMLKAC is capable of mediating selective homing of phage to ischemic heart tissue. DSPE-PEG5000-CSTSMLKAC can be used for drug delivery .
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- HY-119649R
-
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Parasite
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Infection
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Flonicamid (Standard) is the analytical standard of Flonicamid. This product is intended for research and analytical applications. Flonicamid (IKI220) is a novel systemic insecticide with selective activity against hemipterous pests. The main insecticidal mechanism of flonicamid is starvation based on the inhibition of stylet penetration to plant tissues .
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- HY-147374
-
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Epigenetic Reader Domain
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Metabolic Disease
Inflammation/Immunology
|
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Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases .
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- HY-B1614
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-
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- HY-115768
-
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Poly-p-methoxyphenethylmethylamine
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Phospholipase
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Neurological Disease
Cancer
|
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Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways .
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- HY-NP002D
-
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Biochemical Assay Reagents
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Others
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Bovine Serum Albumin (Biotinylated) is a biotinylated bovine serum albumin that selectively binds to different vascular subsets in lymphoid tissue. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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- HY-150970
-
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Pyroptosis
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Cancer
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ICy-OH, an iodinated photosensitizer, is an effective anticancer agent. ICy-OH can be used not only for deep tissue imaging (λex=640 nm，λem=690-740 nm) but also to selectively induce cell death in pancreatic cancer cells via cell pyroptosis pathway .
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- HY-13738AR
-
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Keoxifene (hydrochloride)(Standard); LY156758(Standard); LY139481 (hydrochloride) (Standard)
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Estrogen Receptor/ERR
Autophagy
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Endocrinology
Cancer
|
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Raloxifene (hydrochloride) (Standard) is the analytical standard of Raloxifene (hydrochloride). This product is intended for research and analytical applications. Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue .
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- HY-19665
-
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LY303870
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
|
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Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis .
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- HY-100186
-
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Androgen Receptor
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Cardiovascular Disease
Others
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
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GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness .
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-
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- HY-137976
-
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Penequinine hydrochloride
|
mAChR
NF-κB
Apoptosis
Autophagy
Akt
GSK-3
ERK
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Penehyclidine (Penequinine) hydrochloride, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation .
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-
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- HY-N0457AR
-
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HIV Integrase
HIV
Endogenous Metabolite
|
Infection
Cancer
|
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L-Chicoric Acid (Standard) is the analytical standard of L-Chicoric Acid. This product is intended for research and analytical applications. L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture .
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-
-
- HY-W020468
-
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DuP 996
|
Potassium Channel
TRP Channel
|
Neurological Disease
|
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Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue .
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- HY-120110
-
-
- HY-142119
-
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mAChR
NF-κB
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Inflammation/Immunology
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Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation .
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- HY-101176
-
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Melatonin Receptor
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Cancer
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2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1 over MT2 . 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues .
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- HY-155684
-
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PROTACs
VEGFR
PDGFR
Ephrin Receptor
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Cancer
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SA-PA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues .
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- HY-D1275
-
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Fluorescent Dye
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Others
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CAY10731 (compound 3) is a highly selective fluorescent probe for detection of hydrogen sulfide (H2S). CAY10731 is used to monitor exo- and endogenous H2S in both cancer and normal cells. CAY10731 is applied for imaging of H2S in living tissues at variable depths and in nematodes .
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- HY-144126
-
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LPL Receptor
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Inflammation/Immunology
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S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS) .
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- HY-135747
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GR-7
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Bacterial
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Infection
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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 .
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- HY-131340
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion .
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- HY-103336
-
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T1117
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GPR55
Cannabinoid Receptor
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Cardiovascular Disease
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Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoid CB1 receptor antagonist AM251 (HY-15443), is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm) .
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- HY-103195
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NKY80
2 Publications Verification
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Adenylate Cyclase
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Metabolic Disease
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NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues .
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- HY-B1614R
-
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Adrenergic Receptor
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Metabolic Disease
Inflammation/Immunology
Endocrinology
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Clenbuterol (hydrochloride) (Standard) is the analytical standard of Clenbuterol (hydrochloride). This product is intended for research and analytical applications. Clenbuterol (NAB-365) hydrochloride, a selective β2-adrenergic agonist, enhances skeletal muscle strength and hypertrophy. Clenbuterol hydrochloride induces growth factor mRNA, activates astrocytes, and protects rat brain tissue against ischemic damage .
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- HY-155685
-
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PROTACs
VEGFR
Ephrin Receptor
Apoptosis
|
Cancer
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SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase .
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- HY-131891
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mAChR
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Neurological Disease
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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 .
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- HY-W753375R
-
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Fungal
Succinate Dehydrogenase
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Infection
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Clenbuterol (hydrochloride) (Standard) is the analytical standard of Clenbuterol (hydrochloride). This product is intended for research and analytical applications. Clenbuterol (NAB-365) hydrochloride, a selective β2-adrenergic agonist, enhances skeletal muscle strength and hypertrophy. Clenbuterol hydrochloride induces growth factor mRNA, activates astrocytes, and protects rat brain tissue against ischemic damage .
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- HY-119649S
-
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IKI220-15N18O
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Isotope-Labeled Compounds
Parasite
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Infection
|
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Flonicamid- 15N,18O (IKI220- 15N,18O) is 15N labeled Flonicamid. Flonicamid (IKI220) is a novel systemic insecticide with selective activity against hemipterous pests. The main insecticidal mechanism of flonicamid is starvation based on the inhibition of stylet penetration to plant tissues .
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- HY-167689
-
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Adrenergic Receptor
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Neurological Disease
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Parethoxycaine hydrochloride is an anesthetic with nerve conduction blocking activity. Parethoxycaine hydrochloride exhibits non-selective inhibitory effects on responses to various stimulants in rat vas deferens and guinea pig ileum muscles. Parethoxycaine hydrochloride has an enhanced effect on the action of norepinephrine, and its methyl bromide derivative also exhibits the same properties on the action of norepinephrine and potassium ions. Derivatives of parethoxycaine hydrochloride have significant effects on calcium dose-response curves, displaying different tissue and stimulant selectivities. The mechanism of action of Parethoxycaine hydrochloride involves the regulation of calcium transport processes .
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- HY-131334
-
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AMPK
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Metabolic Disease
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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 .
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- HY-111056
-
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Ser/Thr Protease
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Cancer
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UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM. UK122 shows no or little inhibition of tissue-type PA (tPA), plasmin, thrombin, and trypsin (all IC50>100 μM). UK122, 4-oxazolidinone analogue, is an anticancer agent and inhibits cancer cell migration and invasion .
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- HY-131881
-
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mAChR
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Neurological Disease
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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 .
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- HY-D0053
-
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6-Carboxy-X-rhodamine
|
Fluorescent Dye
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Others
|
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6-ROX is a selective fluorescent probe and potential inhibitor of COX-2. 6-ROX binds to the active site of COX-2 and inhibits its conversion of arachidonic acid into prostaglandins. 6-ROX is often used in the field of optical imaging related to tumors and inflammation, and helps detect diseased tissues with high expression of COX-2 .
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- HY-171248
-
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Anaplastic lymphoma kinase (ALK)
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Cardiovascular Disease
Endocrinology
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CDD-1115 is a potent, selective inhibitor of BMPR2 with IC50 of 1.8 nM, Kiapp of 6.2 nM. CDD-1115 inhibits bone morphogenetic protein (BMP)-mediated gene expression. BMP controls cellular processes across many tissue types, including the kidney, skeletal muscle, heart, and reproductive organs. BMP induces ectopic bone formation .
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- HY-171249
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TGF-β Receptor
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Cardiovascular Disease
Endocrinology
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CDD-1431 is a low-nanomolar selective kinase inhibitors of BMPR2, with Kiapp value of 20.6 nM. CDD-1431 suppresses BRE-reporter activity, with an IC50 of 4.87 μM. BMP controls cellular processes across many tissue types, including the kidney, skeletal muscle, heart, and reproductive organs. BMP induces ectopic bone formation .
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- HY-10656
-
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Urotensin Receptor
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Inflammation/Immunology
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SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells .
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- HY-137561A
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PLN-74809 hydrochloride
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Integrin
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Inflammation/Immunology
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Bexotegrast hydrochloride (PLN-74809 hydrochloride) is a small molecule dual selective inhibitor with activity targeting αVβ1 and αVβ6. Bexotegrast hydrochloride is used for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). Bexotegrast hydrochloride inhibits the activation of TGF-β1 by blocking the function of these integrins, thereby preventing the growth of fibrous tissue in the lungs and bile ducts .
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- HY-10569
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ACT-128800
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LPL Receptor
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Inflammation/Immunology
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Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-105017
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ATL 313; DE 112
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Adenosine Receptor
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Infection
Inflammation/Immunology
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Evodenoson is a selective agonist of the A2A adenosine receptor. Evodenoson’s primary actions include reducing inflammatory responses, decreasing intestinal fluid secretion, edema, tissue damage, and neutrophil infiltration induced by Clostridium difficile toxin A. Evodenoson’s protective effect is achieved by reducing myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, and by lowering the production of tumor necrosis factor-alpha (TNF-α) .
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- HY-19409
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Calcium Channel
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Neurological Disease
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AJG049 is a novel antagonist of the Ca 2+ channel with an IC50 value of 79 nM. AJG049 can be used to reduce the contraction of intestinal smooth muscle .
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- HY-16923A
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BIII-890 hydrochloride; BIII-890 CL
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Sodium Channel
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Neurological Disease
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Crobenetine hydrochloride (BIII-890 hydrochloride) is the hydrochloride form of Crobenetine (HY-16923). Crobenetine hydrochloride is a selective inhibitor for Na + channel. Crobenetine hydrochloride displaces 3HBTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, exhibits only low binding affinity for other receptors and ion channels. Crobenetine hydrochloride protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
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- HY-115924
-
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CDK
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Cancer
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CDK1-IN-1 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent .
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- HY-19674
-
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SSR182289A free base
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Thrombin
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Cardiovascular Disease
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SSR182289 (SSR182289A free base) is a selective and potent orally active thrombin inhibitor. SSR182289 competitively and selectivity inhibits human thrombin (Ki=0.031 μM). SSR182289 demonstrates anticoagulant activity in vitro (thrombin time EC100=96 nM) and inhibits tissue factor-induced thrombin generation (IC50=0.15 μM) in human plasma. SSR182289 inhibits thrombin-induced aggregation of human platelets (IC50=32 nM), but has no effect on aggregation induced by other platelet agonists .
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- HY-116450
-
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Dopamine Receptor
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Neurological Disease
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TISCH is a potent and selective iodinated ligand with high affinity and selectivity for CNS D1 dopamine receptors. TISCH showed a Kd value of 0.205 nM in rat striatal tissue, indicating its effectiveness in biological activity. TISCH is able to easily cross the blood-brain barrier and show distribution in specific areas with D1 receptor density. TISCH is considered to be useful as a pharmacological tool for characterizing D1 dopamine receptors. When labeled with I-123, TISCH has the potential to be used as an in vivo imaging agent for CNS D1 dopamine receptors .
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- HY-116771
-
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Adrenergic Receptor
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Metabolic Disease
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CL316243 free acid is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors. CL316243 free acid is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 free acid has the potential for the treatment obesity, diabetes and urge urinary incontinence .
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- HY-153114
-
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FXR
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Inflammation/Immunology
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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 .
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- HY-116771A
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Adrenergic Receptor
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Metabolic Disease
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CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors .CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate . CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence .
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- HY-15606
-
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NSP-989
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Progesterone Receptor
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Endocrinology
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Tanaproget is an orally effective, selective nonsteroidal progesterone receptor (PR) agonist targeting human PR with an IC50 of 1.7 nM. Tanaproget promotes the interaction between PR receptors and coactivators (such as SRC-1), thereby inhibiting the secretion of matrix metalloproteinases (MMP-3/MMP-7) and reducing endometrial tissue invasion and angiogenesis. Tanaproget can be used for contraception and endometriosis inhibition research .
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- HY-116908
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5-HT Receptor
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Neurological Disease
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SB-272183 is a selective 5-HT1A, 5-HT1B and 5-HT1D receptor antagonist. In addition, SB-272183 is also a potent and selective ligand for 5-HT1A, 5-HT1B and 5-HT1D receptors in human recombinant and native tissues with pKi values of 8.0, 8.1 and 8.7, respectively. SB-272183 can be used in antidepressant research .
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- HY-16923
-
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BIII-890; BIII-890 CL free acid
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Sodium Channel
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Neurological Disease
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Crobenetine (BIII-890), a benzomorphan derivative, is a potent, selective, and highly use-dependent Na + channel blocker. Crobenetine displaces [3H]BTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, yet exhibits only low binding affinity for other receptors and ion channels. Crobenetine protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
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- HY-136675
-
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Fluorescent Dye
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Others
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ASMI is a ratiometric, two-photon excited fluorescent probe, composed of a highly two-photon active and biocompatible merocyanine fluorophore and an acrylate moiety as a thiol reactive site. ASMI is able to selectively detect and monitor mitochondrial Cys with rapid responsiveness, imaging living cells and intact tissues with high contrast and brightness at a depth of 150 μm. The two-photon action cross section (Φσmax) of ASMI is 65.2 GM, corresponding to an excitation wavelength (λex) of 740 nm.
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- HY-P5421
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Proton Pump
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Others
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Caloxin 1B1 is a biological active peptide. (Caloxin 1b1 is obtained by screening for binding to extracellular domain 1 of PMCA4, which inhibited PMCA extracellularly, selectively, and had a higher affinity for PMCA4 than PMCA1. Because caloxin 1b1 had been selected to bind to an extracellular domain of PMCA, it could be added directly to cells and tissues to examine its effects on smooth muscle and endothelium.)
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- HY-111952
-
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CID 16016685
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Endogenous Metabolite
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Others
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SR-4995 (CID 16016685) is a highly effective and selective ligand for α-β-hydrolase domain-containing 5 (ABHD5), facilitating the activation of adipose triglyceride lipase (ATGL) by displacing ABHD5 from its inhibitory regulators, perilipin-1 (PLIN1) and PLIN5. It directly interacts with ABHD5, inhibiting its association with PLIN1, and promotes lipolysis in adipocytes and muscle tissues while circumventing PKA-dependent signaling pathways.
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- HY-150701
-
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Glucocorticoid Receptor
Mineralocorticoid Receptor
11β-HSD
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Metabolic Disease
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INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research .
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- HY-169179
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PROTACs
STAT
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Cancer
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AK-1690 is a potent and selective STAT6 PROTAC degrader. AK-1690 reduces the levels of STAT6 protein in cells (DC50=1 nM) and depletes STAT6 protein in mouse tissues. AK-1690 can be used for the research of cancer. (Pink: ligand for target protein STAT6 (HY-169182); Black: linker (HY-W459522); Blue: ligand for E3 ligase (HY-131318) .
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- HY-18572S
-
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2,4-Dichlorophenoxyacetic acid-13C6
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Isotope-Labeled Compounds
DNA/RNA Synthesis
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Others
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2,4-D- 13C6 is the 13C-labeled 2,4-D. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[1].
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- HY-18572S1
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DNA/RNA Synthesis
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Others
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2,4-D-d3 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].
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- HY-18572S2
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DNA/RNA Synthesis
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Others
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2,4-D-d5 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].
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- HY-B0639
-
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WR2721
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MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
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Cancer
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Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action .
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- HY-13508
-
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Histamine Receptor
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Inflammation/Immunology
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JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory .
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- HY-P1821
-
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MHP4-14
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PKC
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Neurological Disease
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Myelin Basic Protein (MHP4-14), a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca 2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts .
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- HY-B0639A
-
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WR2721 trihydrate
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MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
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Cancer
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Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action .
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- HY-138454
-
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Mercaptoethylguanidine hemisulfate
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NO Synthase
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Inflammation/Immunology
|
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MEG (Mercaptoethylguanidine) hemisulfate is a potent and selective inhibitor of the inducible NO synthase (iNOS), with EC50s of 11.5, 110, and 60 μM for iNOS, ecNOS, and bNOS respectively in tissue homogenates. MEG hemisulfate is also a potent scavenger of peroxynitrite and inhibits peroxynitrite-induced oxidative processes. MEG hemisulfate has a protective effect in many experimental models of inflammation, including ischemia/reperfusion injury, periodontitis, hemorrhagic shock, inflammatory bowel disease, and endotoxic and septic shock .
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- HY-103455
-
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Estrogen Receptor/ERR
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Others
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ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.
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- HY-P1821A
-
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MHP4-14 TFA
|
PKC
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Neurological Disease
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Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein TFA is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca 2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts .
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- HY-B0561
-
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SC9420
|
Mineralocorticoid Receptor
Androgen Receptor
Autophagy
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
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Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (Ang II)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type II diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
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-
- HY-16936
-
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LRRK2
|
Neurological Disease
|
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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 .
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- HY-10569S
-
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ACT-128800-d4
|
Isotope-Labeled Compounds
LPL Receptor
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Others
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|
Ponesimod-d4 (ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-145801
-
|
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NF-κB
|
Inflammation/Immunology
|
|
XT2 is a potent, orally active, and selective inhibitor of NF-κB-inducing kinase (NIK) with an IC50 of 9.1 nM. XT2 suppresses CCl4-induced upregulation of ALT, a key biomarker of acute liver injury. XT2 also decreases immune cell infiltration into the injured liver tissue. XT2 has the potential for the research of liver inflammatory diseases . XT2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-W338446
-
|
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Tau Protein
|
Neurological Disease
|
|
BF-170 is a selective tau fibril binding agent with an EC50 of 221 nM. It exhibits good blood-brain barrier permeability, and after intravenous injection in mice, the concentration in brain tissue reaches 9.1% ID/g within 2 minutes (with a brain clearance rate of 0.25% ID/g after 30 minutes). BF-170 can be used as a probe for tau protein pathology imaging in Alzheimer's disease (AD). It plays an important role in early-stage AD research and holds potential for imaging studies of tau-related neurodegenerative diseases .
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-
- HY-P10420
-
|
|
CD47
Interleukin Related
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Cancer
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|
RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumor cells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumor cells. RS17 can be used to study the mechanism of anti-tumor response and immune escape .
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-
- HY-10569S1
-
|
ACT-128800-d7
|
Isotope-Labeled Compounds
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Others
|
|
Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
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- HY-125961
-
|
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Others
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Cancer
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|
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) .
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- HY-162902
-
|
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TGF-β Receptor
|
Cardiovascular Disease
|
|
ALK5-IN-82 is a potent and selective inhibitor against activin receptor-like kinase 5 (ALK5) with an IC50 value of 9.1 nM. ALK5-IN-82 inhibits the protein expression of α-smooth muscle actin (α-SMA), collagen I and tissue inhibitor of metalloproteinase 1 (TIMP-1)/matrix metalloproteinase 13 (MMP-13) in transforming growth factor-β-induced human umbilical vein endothelial cells. ALK5-IN-82 is promising for research of cardiac fibrosis .
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-
- HY-P99575
-
|
AMG-757
|
Notch
|
Inflammation/Immunology
Cancer
|
|
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
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-
- HY-150057
-
|
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Cannabinoid Receptor
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Others
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CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .
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-
- HY-Y1147
-
|
Maleic acid diethyl ester
|
Biochemical Assay Reagents
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Others
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|
Diethyl maleate (DEM) is an orally available, effective glutathione (GSH) depletor that crosses the blood-brain barrier. Diethyl maleate covalently binds irreversibly to GSH via glutathione S-transferase with an in vitro IC50 of 0.1-0.5 mM. Diethyl maleate selectively depletes GSH in liver, lung, and brain tissues, exacerbating oxidative stress and enhancing hyperbaric oxygen toxicity. Diethyl maleate promotes precursor amino acid uptake and in turn promotes GSH synthesis by upregulating the activity of the cystine-glutamate transporter XO -. Diethyl maleate can be used to study redox homeostasis and GSH protection mechanisms in oxidative stress-related diseases such as hyperbaric oxygen injury and metabolic diseases[1][2][3].
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-
- HY-N13866
-
|
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Others
|
Cancer
|
|
Cucumarioside A2-2 is a triterpene glycoside with antitumor activity. Cucumarioside A2-2 can induce mouse macrophage polarization toward the M1 phenotype. Cucumarioside A2-2 pretreated macrophages can effectively and selectively target and kill multiple types of cancer cells. Cucumarioside A2-2-induced M1 macrophages can effectively target and penetrate tumor tissues and improve the survival rate of mice in an allogeneic model. Exogenous activation of Cucumarioside A2-2 provides a useful model for the subsequent development of antitumor cell immunosuppression .
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-
- HY-W205529
-
|
|
Fluorescent Dye
|
Neurological Disease
|
|
RO 16-6491 Free base is a selective, reversible inhibitor of monoamine oxidase type B (MAO-B), exhibiting high affinity and specificity for binding sites in human frontal cortex mitochondria and platelet membranes. RO 16-6491 demonstrates a fast dissociation of bound radioactivity at 20 degrees C, indicating its dynamic binding properties. RO 16-6491 also acts as a substrate for MAO-B, suggesting that its oxidation may produce a stable intermediate responsible for its potent inhibitory effects. RO 16-6491 serves as an excellent radioligand probe for investigating the regional tissue distribution of MAO-B in various physiological and pathological states.
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-
- HY-161449
-
|
|
11β-HSD
|
Metabolic Disease
|
|
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC50 of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC50 value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1). JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1 .
|
-
- HY-117991
-
|
|
VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
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-
- HY-P99459
-
|
BG 9924; TT-47
|
TNF Receptor
|
Inflammation/Immunology
|
|
Baminercept (BG 9924) is an anti-lymphotoxin β receptor (LTβR) IgG fusion protein (LTβR-Ig). Baminercept selectively binds to the LTβR ligand LTα/β heterotrimer and LIGHT, block the LTβR signaling pathway, and inhibits the expression of chemokines such as CXCL13. Baminercept also regulates peripheral blood B cell and T cell subsets, reduces the transcription of IFN-induced genes. Thereby Baminercept inhibits the formation of high endothelial venules and reticular structures in lymphoid tissues, and affects immune cell migration. Baminercept can be used for the study of autoimmune diseases such as primary Sj?gren's syndrome (pSS) and rheumatoid arthritis (RA) .
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- HY-N2909
-
|
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Others
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Neurological Disease
Inflammation/Immunology
|
|
Aurantiamide is a non-covalent, orally active, blood-brain-permeable GRPR selective antagonist with anti-inflammatory and neuroprotective effects. Aurantiamide reduces inflammation and oxidative stress in renal tissue by inhibiting GRPR-mediated renal necrosis pathways (such as RIPK3/MLKL signaling) and NF-κB inflammatory pathways, exerting anti-acute kidney injury and endothelial function activities. Aurantiamide also inhibits the M1 polarization of microglia and inhibits NLRP3 activation, thereby improving AD mouse models. Aurantiamide has in vivo inhibitory efficacy in acute kidney injury models such as ischemia/reperfusion, sepsis, and hypertension models .
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-
- HY-P3849
-
|
LMN-NKA
|
Neurokinin Receptor
|
Neurological Disease
|
|
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues .
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![[Lys5,MeLeu9,Nle10]Neurokinin A(4-10)](//file.medchemexpress.eu/product_pic/hy-p3849.gif)
- HY-116330
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Calcium Channel
TRP Channel
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Neurological Disease
Inflammation/Immunology
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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 and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. 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 .
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- HY-108596
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Potassium Channel
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Inflammation/Immunology
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BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM) .
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- HY-N3945
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O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
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Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
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Inflammation/Immunology
Cancer
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Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
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- HY-170824
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PROTACs
Epigenetic Reader Domain
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Cancer
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SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827) .
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Product Name |
Type |
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- HY-130013
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Fluorescent Dyes/Probes
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HKYellow-AM (6/12-mixture) is a yellow fluorescent probe that can detect ONOO- in living cells and tissues with high selectivity and sensitivity without cytotoxicity .
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- HY-D1275
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Fluorescent Dyes/Probes
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CAY10731 (compound 3) is a highly selective fluorescent probe for detection of hydrogen sulfide (H2S). CAY10731 is used to monitor exo- and endogenous H2S in both cancer and normal cells. CAY10731 is applied for imaging of H2S in living tissues at variable depths and in nematodes .
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- HY-D0053
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6-Carboxy-X-rhodamine
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Oligonucleotide Labeling
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6-ROX is a selective fluorescent probe and potential inhibitor of COX-2. 6-ROX binds to the active site of COX-2 and inhibits its conversion of arachidonic acid into prostaglandins. 6-ROX is often used in the field of optical imaging related to tumors and inflammation, and helps detect diseased tissues with high expression of COX-2 .
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Product Name |
Type |
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- HY-Y1147
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Maleic acid diethyl ester
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Biochemical Assay Reagents
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Diethyl maleate (DEM) is an orally available, effective glutathione (GSH) depletor that crosses the blood-brain barrier. Diethyl maleate covalently binds irreversibly to GSH via glutathione S-transferase with an in vitro IC50 of 0.1-0.5 mM. Diethyl maleate selectively depletes GSH in liver, lung, and brain tissues, exacerbating oxidative stress and enhancing hyperbaric oxygen toxicity. Diethyl maleate promotes precursor amino acid uptake and in turn promotes GSH synthesis by upregulating the activity of the cystine-glutamate transporter XO -. Diethyl maleate can be used to study redox homeostasis and GSH protection mechanisms in oxidative stress-related diseases such as hyperbaric oxygen injury and metabolic diseases[1][2][3].
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- HY-172687
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Drug Delivery
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DSPE-PEG2000-CSTSMLKAC is a PEG compound which composed of DSPE and a peptide (CSTSMLKAC). CSTSMLKAC is capable of mediating selective homing of phage to ischemic heart tissue. DSPE-PEG2000-CSTSMLKAC can be used for drug delivery .
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- HY-172686
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Drug Delivery
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DSPE-PEG1000-CSTSMLKAC is a PEG compound which composed of DSPE and a peptide (CSTSMLKAC). CSTSMLKAC is capable of mediating selective homing of phage to ischemic heart tissue. DSPE-PEG1000-CSTSMLKAC can be used for drug delivery .
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- HY-172688
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Drug Delivery
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DSPE-PEG5000-CSTSMLKAC is a PEG compound which composed of DSPE and a peptide (CSTSMLKAC). CSTSMLKAC is capable of mediating selective homing of phage to ischemic heart tissue. DSPE-PEG5000-CSTSMLKAC can be used for drug delivery .
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- HY-NP002D
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Native Proteins
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Bovine Serum Albumin (Biotinylated) is a biotinylated bovine serum albumin that selectively binds to different vascular subsets in lymphoid tissue. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules .
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Product Name |
Target |
Research Area |
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- HY-P10216
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Biochemical Assay Reagents
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Neurological Disease
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CAQK peptide selectively binds to injured mouse brain. CAQK peptide selectively targets demyelinating areas and it is absent from healthy tissue. The CAQK peptide target is a proteoglycan complex upregulated in brain injuries and is used for drug delivery. CAQK peptide can penetrate the blood-brain barrier .
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- HY-P1473
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Amylin (8-37) (mouse, rat)
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Amylin Receptor
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Metabolic Disease
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Amylin (8-37), rat is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Amylin (8-37), rat is a weak amylin receptor (AMY) antagonist.
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- HY-P1407
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VRPR
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MALT1
Influenza Virus
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Infection
Cancer
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Z-VRPR-FMK (TFA) (VRPR), a tetrapeptide, is a selective and irreversible MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1) inhibitor. Z-VRPR-FMK (TFA) can protect against influenza A virus (IAV) infection .
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- HY-P1821
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MHP4-14
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PKC
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Neurological Disease
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Myelin Basic Protein (MHP4-14), a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca 2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts .
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- HY-P1821A
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MHP4-14 TFA
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PKC
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Neurological Disease
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Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein TFA is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca 2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts .
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- HY-P10420
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CD47
Interleukin Related
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Cancer
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RS17 is an anti-tumor peptide designed to bind specifically to the CD47 molecule and block the interaction between CD47 and its ligand, SIRPα, on the surface membrane of macrophages. The main regulatory mechanism of RS17 is to prevent CD47 from transmitting selective phagocytosis signals to SIRPα by binding to CD47, so that macrophages do not recognize tumor cells as their own tissue, but phagocytose them as foreign substances, thereby inhibiting immune escape of tumor cells. RS17 can be used to study the mechanism of anti-tumor response and immune escape .
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- HY-P3849
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LMN-NKA
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Neurokinin Receptor
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Neurological Disease
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[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues .
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- HY-P5421
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Proton Pump
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Others
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Caloxin 1B1 is a biological active peptide. (Caloxin 1b1 is obtained by screening for binding to extracellular domain 1 of PMCA4, which inhibited PMCA extracellularly, selectively, and had a higher affinity for PMCA4 than PMCA1. Because caloxin 1b1 had been selected to bind to an extracellular domain of PMCA, it could be added directly to cells and tissues to examine its effects on smooth muscle and endothelium.)
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Product Name |
Target |
Research Area |
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- HY-P99575
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AMG-757
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Notch
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Inflammation/Immunology
Cancer
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Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
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- HY-P99459
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BG 9924; TT-47
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TNF Receptor
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Inflammation/Immunology
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Baminercept (BG 9924) is an anti-lymphotoxin β receptor (LTβR) IgG fusion protein (LTβR-Ig). Baminercept selectively binds to the LTβR ligand LTα/β heterotrimer and LIGHT, block the LTβR signaling pathway, and inhibits the expression of chemokines such as CXCL13. Baminercept also regulates peripheral blood B cell and T cell subsets, reduces the transcription of IFN-induced genes. Thereby Baminercept inhibits the formation of high endothelial venules and reticular structures in lymphoid tissues, and affects immune cell migration. Baminercept can be used for the study of autoimmune diseases such as primary Sj?gren's syndrome (pSS) and rheumatoid arthritis (RA) .
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Product Name |
Category |
Target |
Chemical Structure |
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- HY-N0457A
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- HY-13738A
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- HY-B1614
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- HY-13738AR
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- HY-N2909
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- HY-N9141
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- HY-N0457AR
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- HY-B1614R
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Structural Classification
Natural Products
Source classification
Endogenous metabolite
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Adrenergic Receptor
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Clenbuterol (hydrochloride) (Standard) is the analytical standard of Clenbuterol (hydrochloride). This product is intended for research and analytical applications. Clenbuterol (NAB-365) hydrochloride, a selective β2-adrenergic agonist, enhances skeletal muscle strength and hypertrophy. Clenbuterol hydrochloride induces growth factor mRNA, activates astrocytes, and protects rat brain tissue against ischemic damage .
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- HY-N13866
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Triterpenes
Structural Classification
Animals
Terpenoids
Source classification
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Others
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Cucumarioside A2-2 is a triterpene glycoside with antitumor activity. Cucumarioside A2-2 can induce mouse macrophage polarization toward the M1 phenotype. Cucumarioside A2-2 pretreated macrophages can effectively and selectively target and kill multiple types of cancer cells. Cucumarioside A2-2-induced M1 macrophages can effectively target and penetrate tumor tissues and improve the survival rate of mice in an allogeneic model. Exogenous activation of Cucumarioside A2-2 provides a useful model for the subsequent development of antitumor cell immunosuppression .
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- HY-116330
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- HY-N3945
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O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
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Infection
Alkaloids
Structural Classification
other families
Classification of Application Fields
Source classification
Plants
Isoquinoline Alkaloids
Glaucium flavum
Inflammation/Immunology
Disease Research Fields
Papaveraceae
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Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
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Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-18572S
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2,4-D- 13C6 is the 13C-labeled 2,4-D. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[1].
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- HY-18572S2
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2,4-D-d5 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].
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- HY-10569S1
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Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
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- HY-119649S
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Flonicamid- 15N,18O (IKI220- 15N,18O) is 15N labeled Flonicamid. Flonicamid (IKI220) is a novel systemic insecticide with selective activity against hemipterous pests. The main insecticidal mechanism of flonicamid is starvation based on the inhibition of stylet penetration to plant tissues .
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- HY-18572S1
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2,4-D-d3 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].
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- HY-10569S
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Ponesimod-d4 (ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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![[Lys5,MeLeu9,Nle10]Neurokinin A(4-10)](http://file.medchemexpress.eu/product_pic/hy-p3849.gif)
