Bis(7-methyl-1-octyl) Phthalate-3,4,5,6-d4 is the deuterium labeled Bis(7-methyl-1-octyl) Phthalate[1].
Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) is a potent, non-competitive tyrosinase inhibitor with an IC50 value of 49.33 ± 2.64 µM and Ki value of 31.25 ± 0.25 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) have the highest radical scavenging activity to reduce the production of reactive oxygen species (ROS) with an IC50 value of 25.39 ± 0.77 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) can be used for anti-browning substances in the food and agricultural sectors[1].
UDP-sugar pyrophosphorylase (AtUSP) is a broad substrate enzyme that synthesizes nucleotide sugars. UDP-sugar pyrophosphorylase catalyzes the conversion of various monosaccharide 1-phosphates to the respective UDP-sugars in the salvage pathway[1].
Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity[1].
H3 receptor-MO-1 is a modulator of histamine H3 receptor.
Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice[1][2][3][4].
(R)-Pralatrexate is the (R)-enantiomer of Pralatrexate (HY-10446). Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor[1].
GW542573X is a potent and selective Ca2+-activated K+ 2 (SK2) channels activator. GW542573X induces the Ca2+-response curve of hSK1 that left-shifted from an EC50 (Ca2+) value of 410 nM to 240 nM[1].
Murlentamab (3C23K; GM102) is a humanized anti-AMHRII antibody. AMHRII is the anti-Müllerian hormone receptor. Murlentama significantly promotes macrophage-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Murlentama stimulates pro-inflammatory and anti-tumor internal environment, recruits and activates T cells. Murlentama suppresses tumors growth by inducing naïve macrophage orientation and promoting tumor-associated macrophage (TAM) reprogramming[1].
SOMCL-668 is a selective and potent sigma-1 receptor allosteric modulator. ?SOMCL-668 shows positive modulation of improvement in social deficits and cognitive impairment induced by the selective sigma-1 agonist PRE084.?SOMCL-668 displays anti-seizure activities and can be used for psychotic illness research[1].
Propafenone-d5 hydrochloride(Ethyl) (SA-79-d5 hydrochloride(Ethyl)) is the deuterium labeled Propafenone hydrochloride. Propafenone (SA-79）hydrochloride is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias[1].
Besifloxacin hydrochloride is a fourth-generation fluoroquinolone antibiotic. IC50 Value:Target: AntibacterialBesifloxacin has been found to inhibit production of pro-inflammatory cytokines in vitro. Besifloxacin is a novel 8-chloro-fluoroquinolone agent with potent, bactericidal activity against prevalent and drug-resistant pathogens.besifloxacin is the most potent agent tested against gram-positive pathogens and anaerobes and is generally equivalent to comparator fluoroquinolones in activity against most gram-negative pathogens. Besifloxacin demonstrates potent, broad-spectrum activity, which is particularly notable against gram-positive and gram-negative isolates that are resistant to other fluoroquinolones and classes of antibacterial agents.
MC-Val-Ala-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Dorsmanin A is a prenylated flavonoid from the twigs of Dorstenia mannii[1].
Bromoacetamido-PEG3-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
D-α-Tocopherol Succinate (Vitamin E succinate) is an antioxidant tocopherol and a salt form of vitamin E. D-α-Tocopherol Succinate inhibits Cisplatin (HY-17394)-induced cytotoxicity. D-α-Tocopherol Succinate can be used for the research of cancer[1][2].
Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity[1].
APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain[1][2].
S-acetyl-PEG2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PDE4-IN-11 is an inhibitor of phosphodiesterase isoenzyme 4 (PDE4). PDE4-IN-11 displays highly effective bronchodilatory and anti-inflammatory properties, can be used for obstructive or inflammatory airway diseases research[1][2][3].
JI130 (JI-130) is a specific Hse1 inhibitor that inhibits the cancer-associated transcription factor Hes1 via the PHB2 chaperone, blocks Hes1-mediated transcriptional repression; interacts with prohibitin 2 (PHB2), stabilizes PHB2's interaction with Hes1 outside the nucleus, inducing G2/M cell cycle arrest; dose-dependently reduces cell growth of the human pancreatic cancer cell line MIA PaCa-2 (IC50=49 nM); significantly reduces tumor volume in murine pancreatic tumor xenograft models.
SB269970 hydrochloride is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.IC50 Value: 8.3 (pKi for 5-HT7) [1]Target: 5-HT7 receptorin vitro: 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes (pEC(50) of 8.4+/-0.2) was inhibited by SB-269970-A (0.3 microM) with a pK(B) (8.3+/-0.1) in good agreement with its antagonist potency at the human cloned 5-HT(7(a)) receptor and its binding affinity at guinea-pig cortical membranes. 5-HT(7) receptor mRNA was highly expressed in human hypothalamus, amygdala, thalamus, hippocampus and testis [1]. Cortical slices were loaded with [(3)H]-5-HT and release was evoked by electrical stimulation. 5-CT inhibited the evoked release of [(3)H]-5-HT in a concentration-dependent manner. SB-269970 had no significant effect on [(3)H]-5-HT release while the 5-HT(1B) receptor antagonist, SB-224289 significantly potentiated [(3)H]-5-HT release. In addition, SB-269970 was unable to attenuate the 5-CT-induced inhibition of release while SB-224289 produced a rightward shift of the 5-CT response, generating estimated pK(B) values of 7.8 and 7.6 at the guinea-pig and rat terminal 5-HT autoreceptors respectively [2].in vivo: Acute administration of SB-269970 (1 mg/kg) or amisulpride (3 mg/kg) ameliorated ketamine-induced cognitive inflexibility and novel object recognition deficit in rats. Both compounds were also effective in attenuating ketamine-evoked disruption of social interactions [3]. Pretreatment with a dose of SB-269970 (0.5 mM) that significantly affects sleep variables antagonized the LP-44 (2.5 mM)-induced suppression of REMS and of the number of REM periods [4].Toxicity: N/AClinical trial: N/A
Butylparaben is an organic compound, has proven to be a highly successful antimicrobial preservative in cosmetics, also used in medication suspensions, and as a flavoring additive in food.
Retrocyclin-2 is an antimicrobial peptide against human immunodeficiency virus, influenza A and herpes simplex virus[1].
Vancomycin is an antibiotic for the treatment of bacterial infections.
Coccinic acid can be isolated from S. pubescens. Coccinic acid is cytotoxic and has potential for cancer research[1].
Cytarabine is a chemotherapy drug used to treat acute myeloid leukaemia, acting by inhibiting DNA synthesis with an IC50 of 16 nM.
β-Caryophyllene is a CB2 receptor agonist.
Rebaudioside D is a glycoside found in the leaves of Stevia rebaudiana and acts as a sweetener[1].
PNRI-299 is a selective AP-1 transcription inhibitor with IC50 of 20 uM without affecting NF-kappaB transcription (up to 200 uM) or thioredoxin (up to 200 uM).IC50 value: 20 uM [1]Target: AP-1 inhibitorin vitro: PNRI-299 specifically reacts with Ref-1, inhibits AP-1 transcription, and overexpression of the molecular target. Ref-1 attenuates PNRI-299 inhibition of AP-1 transcription. PNRI-299 interacts with the redox nucleophile Cys-65, to aid in the interpretation of structure activity relationships (SARs).in vivo: Treatment with PNRI-299 significantly decreased the influx of eosinophils, monocytes, and macrophages (no significant reduction of lymphocytes was observed) into the lung interstitium and bronchoalveolar lavage fluid, and airway mucus and edema observed in OVA-treated mice.PNRI-299 reduces the pathophysiological responses seen in this murine model of allergic asthma [1]. PNRI-299 had no effects on the inflammatory changes or lethality induced by I/R injury [2].