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Results for "

DiD

" in MedChemExpress (MCE) Product Catalog:

49

Inhibitors & Agonists

2

Fluorescent Dye

6

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-D1028
    DiD perchlorate
    Maximum Cited Publications
    15 Publications Verification

    		 Fluorescent Dye Others
    DiD is a long-chain carbocyanine dye. Carbocyanine dyes are widely used as Di to label cells, organelles, liposomes, viruses and lipoproteins .
    DiD perchlorate
  • HY-D0086
    DIDS sodium salt
    10+ Cited Publications

    MDL101114ZA

    		 VDAC RAD51 Cancer
    DIDS sodium salt (MDL101114ZA) is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research .
    DIDS sodium salt
  • HY-124808
    IMM-01

    		Ras Apoptosis Cancer
    IMM-01 is a mammalian Diaphanous (mDia)-related formins agonist that inhibits DID-DAD (diaphanous inhibitory domain-diaphanous autoregulatory domain) binding with an IC50 of 140 nM. IMM-01 acts by disrupting the autoinhibitory bond between the DID and DAD domain and thus activates formins. IMM-01 shows anticancer effects .
    IMM-01
  • HY-N3394
    Lecanoric acid

    		Others Infection
    Lecanoric acid is a histidine-decarboxylase inhibitor isolated from fungus. The inhibition by lecanoric acid is competitive with histidineand noncompetitive with pyridoxal phosphate. Lecanoric acid did not inhibit aromatic amino acid decarboxylase .
    Lecanoric acid
  • HY-121693
    DIDS

    MDL101114ZA free base

    		 VDAC RAD51 Cancer
    DIDS is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research .
    DIDS
  • HY-121918
    RU 41656

    		Others Others
    RU 41656 partially alleviated triazolam-induced memory impairment but did not counteract the sedative effects of this agent .
    RU 41656
  • HY-105578A
    Letimide hydrochloride

    MA 1143 hydrochloride

    		 Endogenous Metabolite Inflammation/Immunology
    Letimide hydrochloride (MA 1143 hydrochloride) is an analgesic with potent analgesic activity. Letimide hydrochloride has shown cytogenetic effects on human lymphocytes in in vitro experiments. Letimide hydrochloride did not exhibit significant chromosomal aberrations or sister chromatid exchanges in in vivo studies in mouse bone marrow cells. Teratogenic studies conducted on mice with Letimide hydrochloride also did not show obvious effects on inducing congenital malformations .
    Letimide hydrochloride
  • HY-129548
    Prumycin

    		Antibiotic Infection
    Prumycin is an antifungal antibiotic with activity against cucumber powdery mildew. Prumycin significantly inhibited the disease, whereas other metabolites such as bacillomycin D and surfactin did not. Prumycin did not induce the expression of plant defense genes, indicating that its effects were not through plant defense responses. Observation of cucumber cotyledons treated with prumycin showed that it could inhibit spore germination of P. fusca .
    Prumycin
  • HY-129548A
    Prumycin di(hydrochloride)

    		Fungal Infection
    Prumycin dihydrochloride is an antifungal antibiotic with activity against cucumber powdery mildew. Prumycin dihydrochloride significantly inhibited the disease, whereas other metabolites such as bacillomycin D and surfactin did not. Prumycin dihydrochloride did not induce the expression of plant defense genes, indicating that its effects were not through plant defense responses. Observation of cucumber cotyledons treated with prumycin showed that it could inhibit spore germination of P. fusca .
    Prumycin di(hydrochloride)
  • HY-169422
    WRN inhibitor 16

    		DNA/RNA Synthesis Cancer
    WRN inhibitor 16 (Example 83) is an orally available WRN inhibitor. WRN inhibitor 16 did not induce tumor regression in the SW48 xenograft mouse tumor model.
    WRN inhibitor 16
  • HY-126742
    MBX-1162

    		Bacterial Others
    MBX-1162 is a bisindole compound. In the study of its resistance mechanism in Staphylococcus aureus, it did not show cross-resistance with related compounds and was related to the substrate specificity of MepA and MepR.
    MBX-1162
  • HY-N4108
    Hypophyllanthin

    		P-glycoprotein Inflammation/Immunology Cancer
    Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity .
    Hypophyllanthin
  • HY-149616
    PPM-3

    		PROTACs ERK Cancer
    PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages .
    PPM-3
  • HY-108602
    Bryostatin 3

    		PKC Cancer
    Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion .
    Bryostatin 3
  • HY-N8487
    7-Methoxyflavone

    		Others Neurological Disease Inflammation/Immunology
    7-Methoxyflavone is a compound isolated from Zornia brasiliensis. 7-Methoxyflavone has peripheral antinociceptive activity. 7-Methoxyflavone inhibits paw-licking time in the neurogenic phase of the formalin pain response (65.6%) and did not decrease the nociceptive response in the inflammatory phase .
    7-Methoxyflavone
  • HY-108519
    AS1892802

    		ROCK Neurological Disease
    AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain .
    AS1892802
  • HY-N4108R
    Hypophyllanthin (Standard)

    		P-glycoprotein Inflammation/Immunology Cancer
    Hypophyllanthin (Standard) is the analytical standard of Hypophyllanthin. This product is intended for research and analytical applications. Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity .
    Hypophyllanthin (Standard)
  • HY-108900
    Leu-AMS

    		Aminoacyl-tRNA Synthetase Bacterial Infection Cancer
    Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria .
    Leu-AMS
  • HY-121700
    L-751788

    		5 alpha Reductase Others
    L-751788 is a selective inhibitor of type I of 5α-reductase. L-751788 does not have a significant impact on the differentiation of the external genitalia in animals. When administered orally to pregnant rhesus monkeys, L-751788 (2, 10 mg/kg) did not cause abnormalities in fetal external genitalia .
    L-751788
  • HY-106055
    Murabutide

    		HIV Inflammation/Immunology
    Murabutide is a safe synthetic immunomodulator. Murabutide can reduce CD4 and CCR5 receptor expression and secrete high levels of beta-chemokines. Murabutide enhances nonspecific resistance against viral infections. Murabutide did not affect virus entry, reverse transcriptase activity or early proviral DNA formation in the cytoplasm of infected cells .
    Murabutide
  • HY-149405
    Squalene synthase-IN-1

    		Others Metabolic Disease
    Squalene synthase-IN-1 (compound 1) is a potent antihyperlipidemic agent acting through Squalene Synthase inhibition. Squalene synthase-IN-1 exhibits an outstanding antioxidant and anti-inflammatory activity. Squalene synthase-IN-1 displays a significant reduction not only of glucose but also of oxidative stress levels, while it did not cause any toxicity .
    Squalene synthase-IN-1
  • HY-135238
    (rel)-RSD 921

    PD-117302

    		 Opioid Receptor Others
    (rel)-RSD 921 (PD-117302) is a κ-opioid receptor agonist. (rel)-RSD 921 did not have a greater food-inducing effect in obese than in lean Zucker rats; in both obese and lean Zucker rats, lean rats were more sensitive to its initial food-inducing effect but ultimately ate less.
    (rel)-RSD 921
  • HY-121490
    IMM-02

    		Apoptosis Cancer
    IMM-02 is a DID-DAD binding inhibitor with activity promoting actin assembly and microtubule stabilization. IMM-02 is able to trigger serum response factor-mediated gene expression and lead to cell cycle arrest and apoptosis. IMM-02 has shown the ability to slow tumor growth in a mouse colon cancer xenograft model .
    IMM-02
  • HY-137494
    Ethyl β-carboline-3-carboxylate

    		GABA Receptor Neurological Disease
    Ethyl β-carboline-3-carboxylate (fl-CCE) is a ligand and short-acting antagonist of benzodiazepine receptors. Ethyl β-carboline-3-carboxylate did not affect cerebellar cGMP levels when used alone, but when taken together with Diazepam, it significantly inhibited the cGMP levels that were upregulated by Diazepam .
    Ethyl β-carboline-3-carboxylate
  • HY-115381
    Lipoxin A5

    		Endogenous Metabolite Cardiovascular Disease
    Lipoxin A5 is an eicosapentaenoic acid derived from pig white blood cells. Lipoxin A5 slowly contracted the guinea pig lung parenchymal strips with a contractile force similar to that of LXA4 and LXB4.2, but LXA5 did not have the vasodilating effect on the aortic smooth muscle shown by LXA4 and LXB4.2 .
    Lipoxin A5
  • HY-116680
    LY53857

    		5-HT Receptor Cardiovascular Disease Neurological Disease
    LY53857 is a potent antagonist of vasoconstriction and serotonin-mediated 5-HT2 receptors. LY53857 did not reduce mean arterial blood pressure in spontaneously hypertensive rats (SHR) at doses that blocked the depressor response to serotonin and blocked central serotonin receptors. In addition, LY53857 was able to enhance neurotransmitter release in rat vas deferens and guinea pig ileal nerves .
    LY53857
  • HY-117219
    SKF 104976

    		Cytochrome P450 HMG-CoA Reductase (HMGCR) Endogenous Metabolite Metabolic Disease
    SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitory activity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin .
    SKF 104976
  • HY-109089S
    Epeleuton-d5

    15(S)-HEPE-d5 ethyl ester; 15(S)-Hydoxy EPA-d5 ethyl ester; 15(S)-Hydoxy eicosapetaeoic acid-d5 ethyl ester

    		 Isotope-Labeled Compounds Others Others
    Epeleuton-d5 (15(S)-HEPE-d5 ethyl ester) is deuterium labeled Epeleuton. Epeleuton is a second-generation synthetic N-3 fatty acid derivative with activity in patients with non-alcoholic fatty liver disease, although it did not reach the primary endpoints of alanine aminotransferase and liver stiffness, but it can significantly reduce triglycerides, glycated hemoglobin, plasma glucose and inflammatory markers .
    Epeleuton-d5
  • HY-167681
    Carprazidil

    Ro 12-4713

    		 Endogenous Metabolite Cardiovascular Disease
    Carprazidil (Ro 12-4713) is a potent vasodilator with activity in suppressing severe hypertension and mild heart failure. The use of carprazidil may lead to sodium retention and increased heart rate, requiring increased doses of diuretics or beta-blockers in some cases. Carprazidil and mecycline may both cause hirsutism, limiting their long-term use in women. Carprazidil did not cause adverse side effects on hematological parameters, liver, or kidney function .
    Carprazidil
  • HY-117902
    SRI-31142

    		Dopamine Transporter Neurological Disease
    SRI-31142 is a putative, brain-penetrant allosteric inhibitor of the dopamine transporter (DAT). In behavioral studies using intracranial self-stimulation (ICSS), SRI-31142 did not produce the abuse-related effects seen with cocaine and GBR-12935, but instead reduced ICSS responses and dopamine levels in the nucleus accumbens (NAc) at effective doses. SRI-31142 also blocked cocaine-induced increases in ICSS and NAc dopamine .
    SRI-31142
  • HY-122742
    HBT1

    		iGluR Neurological Disease
    HBT1 is a potent α-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor (AMPA-R) potentiator. HBT1 bonds with S518 in the ligand-binding domain (LBD) of AMPA-R in a glutamate-dependent manner. HBT1 did not show remarkable bell-shaped response in brain-derived neurotrophic factor (BDNF) production in primary neurons .
    HBT1
  • HY-12172
    MK-8141

    ACT-077825

    		 Renin Cardiovascular Disease
    MK-8141 (ACT-077825) is a renin inhibitor that significantly increases levels of immunoreactive renin (ir-AR) by sevenfold but does not result in sustained reductions in blood renin activity (PRA). This study evaluated the antihypertensive efficacy of MK-8141 in hypertensive disease. Despite its effects on ir-AR, MK-8141 (ACT-077825) did not produce significant blood pressure-lowering effects in the absence of sustained PRA inhibition.
    MK-8141
  • HY-160912
    ELOVL6-IN-5

    		ELOVL Cancer
    ELOVL6-IN-5 (compound B) is an inhibitor of the elongase enzyme of long-chain fatty acid family 6 (ELOVL6). ELOVL6 is a rate-limiting enzyme for the elongation of saturated and monounsaturated long-chain fatty acids and is an effective target for inhibiting diabetes. ELOVL6-IN-5 reduces hepatic fatty acid levels in a mouse model of diet-induced obesity (DIO). However, ELOVL6 inhibition by ELOVL6-IN-5 did not improve insulin resistance .
    ELOVL6-IN-5
  • HY-123525
    COR628

    		GABA Receptor Neurological Disease
    COR628 is a positive allosteric modulator of GABA(B) receptors with the activity of enhancing GABA-induced GTPγS stimulation. COR628 showed significant activity in in vitro studies but did not exhibit endogenous agonist activity. COR628 has shown efficacy in experiments in mice by enhancing the sedation/hypnosis induced by baclofen, shortening the onset time and extending the duration of loss of righting reflex when combined with non-sedating doses of baclofen . The cytotoxic effect of COR628 is comparable to or higher than that of GS39783 or BHF177 in concentration .
    COR628
  • HY-N7536
    Voacangine

    		TRP Channel Others
    Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .
    Voacangine
  • HY-117649
    RU-39411

    		Estrogen Receptor/ERR Cancer
    RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
    RU-39411
  • HY-116240
    2′,3′-Dideoxy-5-ethyluridine

    ddEtUrd

    		 HIV Infection
    2′,3′-Dideoxy-5-ethyluridine (ddEtUrd) is an antiretroviral compound with weak anti-HIV activity. The 3'-substituted derivatives of 2′,3′-Dideoxy-5-ethyluridine did not show significant antiviral effects. 2′,3′-Dideoxy-5-ethyluridine was less potent in inhibiting HIV replication in human MT4 lymphocytes. Although phosphorylation induced by 2′,3′-Dideoxy-5-ethyluridine is essential for antiviral activity, there is no strong correlation between its affinity for human dThd kinase or dCyd kinase .
    2′,3′-Dideoxy-5-ethyluridine
  • HY-138660
    HM Janelia Fluor® 526, SE

    HM-JF526 NHS

    		 Fluorescent Dye Others
    HM Janelia Fluor® 526, SE (HM-JF526 NHS) is a derivative of hydroxymethyl JF526 (HM-JF526). SMLM (single-molecule localization microscopy) imaging in standard phosphate-buffered saline (pH 7.4) revealed that the HM-JF526 label showed spontaneous blinking behavior throughout the imaging session and did not require short-wavelength activation light . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
    HM Janelia Fluor® 526, SE
  • HY-N1638
    1-Methyl-2-undecyl-4(1H)-quinolone

    		Monoamine Oxidase Neurological Disease
    1-Methyl-2-undecyl-4(1H)-quinolone is a potent, irreversible and selective inhibitor of type B monoamine oxidase (MAO-B). 1-Methyl-2-undecyl-4(1H)-quinolone shows a selective inhibition of MAO-B activity with the IC50 and Ki values of 15.3 μM and 9.91 μM, respectively, but did not inhibit type A MAO (MAO-A) activity. Methyl-2-undecyl-4(1H)-quinolone, as a quinolone alkaloid, is isolated from fresh leaves and fruits of Evodia rutaecarpa HOOK. f. et THOMS .
    1-Methyl-2-undecyl-4(1H)-quinolone
  • HY-121535
    Levosemotiadil

    		Sodium Channel Calcium Channel Others
    Levosemotiadil, an S-isomer of semotiadil, exhibits stronger binding affinity to human serum albumin (HSA) compared to its R-isomer counterpart. This study utilized high-performance frontal analysis (HPFA) to demonstrate that levosemotiadil binds approximately three times more strongly to HSA than semotiadil. The binding parameters were evaluated using Scatchard analysis, revealing specific interactions with the diazepam binding site on HSA. The presence of diazepam decreased the binding affinity of both enantiomers, while warfarin did not alter their binding characteristics. These findings highlight levosemotiadil's potential as a Ca- and Na-channel blocker with significant binding preferences for HSA, crucial for understanding its pharmacokinetics and therapeutic effects .
    Levosemotiadil
  • HY-117881
    CJ-15208

    		Opioid Receptor Neurological Disease
    CJ-15208 is a potent and selective κ-opioid receptor antagonist with significant opioid activity. CJ-15208 exhibited strong analgesic effects in the warm water tail withdrawal test in mice and was mediated through multiple opioid receptors. The stereoisomers of CJ-15208 exhibited different opioid activity characteristics, for example, one stereoisomer exhibited κ-opioid receptor antagonism, while the other exhibited δ-opioid receptor antagonism. All stereoisomers of CJ-15208 had no significant effects on respiration. The stereoisomers of CJ-15208 did not lead to the development of drug tolerance, which makes it potential in the further development of safe opioid analgesics .
    CJ-15208
  • HY-122010
    NVP-AAD777

    		VEGFR Others
    NVP-AAD777 is a specific inhibitor of VEGFR-2, demonstrated in vivo by its effective suppression of phospho-VEGFR-2 (Tyr1175) signaling in rat lung tissues. Unlike the nonspecific VEGFR inhibitor SUG-5416, NVP-AAD777 did not induce emphysematous changes in the lungs after three weeks of treatment, even when combined with exposure to cigarette smoke. Additionally, there were no alterations observed in vascular density compared to control animals. This indicates NVP-AAD777's targeted action in inhibiting VEGFR-2 without adverse pulmonary effects, highlighting its potential therapeutic utility in managing conditions associated with aberrant VEGFR-2 signaling .
    NVP-AAD777
  • HY-119396
    DY3002

    		Endogenous Metabolite Cancer
    DY3002 is a selective and highly potent EGFR inhibitor with activity in overcoming T790M-mediated drug resistance in non-small cell lung cancer. DY3002 exhibited superior inhibitory effects against EGFR T790M mutants in kinase assays (IC50 = 0.71 nM), compared to weaker inhibitory effects against wild-type EGFR (IC50 = 448.7 nM). DY3002 was significantly superior to rociletinib and osimertinib in selectivity, showing an extremely high selectivity index (SI = 632.0). In cell experiments, DY3002 had an IC50 value of 0.037 μM against H1975 cells, showing enhanced inhibitory potency. In addition, DY3002 was superior to other alternative compounds in terms of biological properties and did not cause hyperglycemia .
    DY3002
  • HY-155718
    fac-[Re(CO)3(L6)(H2O)][NO3]

    		Apoptosis Cancer
    fac-[Re(CO)3(L6)(H2O)][NO3] (compound 6), the rhenium(I) tricarbonyl aqua complex, is an anticancer agent associated with mitochondrial dysfunction. fac-[Re(CO)3(L6)(H2O)][NO3] is cytotoxic to prostate cancer cells, IC50=50 nM (PC-3 cells). fac-[Re(CO)3(L6)(H2O)][NO3] mainly accumulates in the nucleus, down-regulates ATP production in PC3 cells, and promotes apoptosis. However, fac-[Re(CO)3(L6)(H2O)][NO3] did not induce necrosis, pyrodeath and autophagy .
    fac-[Re(CO)3(L6)(H2O)][NO3]
  • HY-155719
    fac-[Re(CO)3(L3)(H2O)][NO3]

    		Paraptosis Cancer
    fac-[Re(CO)3(L3)(H2O)][NO3] (compound 3), the rhenium(I) tricarbonyl aqua complex, is an anticancer agent associated with mitochondrial dysfunction. fac-[Re(CO)3(L3)(H2O)][NO3] is cytotoxic to prostate cancer cells with IC50=0.32 μM (PC-3 cells). fac-[Re(CO)3(L3)(H2O)][NO3] mainly accumulates in mitochondria, down-regulates ATP production in PC3 cells, and promotes paraptosis. However, fac-[Re(CO)3(L3)(H2O)][NO3] did not induce necrosis, apoptosis and autophagy .
    fac-[Re(CO)3(L3)(H2O)][NO3]
  • HY-136720
    ZXX2-77

    		COX Others
    ZXX2-77 is a cyclooxygenase-1 (COX-1) selective inhibitor belonging to the benzenesulfonylanilide class of compounds. It is reported as a novel analgesic that does not cause gastric damage. ZXX2-77 has a weak analgesic effect but exhibits potent COX-1 inhibitory activity in vitro. The low oral absorption rate of ZXX2-77 leads to its weak analgesic effect in vivo. At a dose of 30 mg/kg, the maximum plasma concentration of ZXX2-77 (1.2 mM) did not reach its COX-1 IC50 value (3.2 mM). In contrast, its derivative ZXX2-79, although weaker in vitro COX inhibitory activity, is better absorbed, exhibits stronger analgesic effect and hardly causes gastric damage. These findings suggest that ZXX2-77 and its derivatives as COX-1 selective inhibitors may become effective analgesics that do not cause gastric damage.
    ZXX2-77
  • HY-102093A
    ZD 7155

    		Angiotensin Receptor Others
    ZD 7155 is an AT1R selective antagonist with renal function modulating activity. The effects of ZD 7155 on glomeruli and tubules were measured in 1- (N = 9) and 6-week-old (N = 13) lambs. Pretreatment with ZD 7155 after L-NAME infusion did not alter glomerular function in 1- or 6-week-old lambs. During postnatal development, Ang II modulates the effects of NO on electrolyte handling via AT1R and AT2R. In 6-week-old lambs, selective inhibition of AT1R and AT2R increased the excretion of Na+, K+, and Cl-. In 6-week-old lambs, pretreatment with ZD 7155 and PD 123319 followed by the addition of L-NAME increased urine flow rate by 200%, free water clearance by 50%, and decreased urine osmolality by 40%. The same trends of changes in these variables were also observed when L-NAME was added to ZD 7155 or PD 123319, although to a lesser extent.
    ZD 7155
  • HY-121708
    KI-328

    		c-Kit Cancer
    KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
    KI-328
  • HY-117947
    (R)-OR-S1

    		Histone Methyltransferase Cancer
    (R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
    (R)-OR-S1

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