Wybutosine is a modified base adjacent to the anticodon of tRNA(Phe)[1].
Eucatropine is a potent muscarinic acetylcholine receptor (mAChR) inhibitor with an IC50 value of 0.583 μM. Eucatropine is an anticholinergic agent[1].
G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-14 respectively.IC50 value: 0.4/0.6/3.5/7.5 nM(Wt Flt3/D835Y/MV4-11/Molm-14) [1]Target: Flt3 inhibitorG-749 showed potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays. G-749 retained its inhibitory potency in various drug-resistance milieus such as patient plasma, FLT3 ligand surge, and stromal protection. Furthermore, it displayed potent antileukemic activity in bone marrow blasts from AML patients regardless of FLT3 mutation status, including those with little or only minor responses to AC220 or PKC412. Oral administration of G-749 yielded complete tumor regression and increased life span in animal models.
2’-Deoxy-2’-fluoro-5-methylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
M-525 is a first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction with binding IC50 of 3.3 nM in FP assays; inhibits MV4;11 (MLL fusion) and HL60 (No MLL fusion) cell growth with IC50 of 2.7 and 2,000 nM, respectively; significantly down-regulates the expression of MEIS1, HOXA9 and HOXA11 genes in a dosedependent anner at ow nanomolar concentrations, also effectively suppresses the expression of MEIS1 and HOX genes in the MOLM-13 cell line at 3 nM.
Zymosterol is a Cholesterol (HY-N0322) biosynthesis metabolite. Zymosterol, a precursor of Cholesterol, is found mostly in the plasma membrane. Zymosterol circulates within the cell[1][2].
(RS)-Carbocisteine is the S-carboxymethyl cysteine with no detectable inhibitory effect. (RS)-Carbocisteine is the inactive enantiomer of Carbocisteine.
Aβ-IN-3 (compound 1) is a potent amyloid β (Aβ) inhibitor. Aβ-IN-3 inhibits Aβ42 aggregation. However, Aβ-IN-3 can not alleviate the neurotoxicity of Aβ42 in SH-SY5Y cells. Aβ-IN-3 can not change the aggregation state of Aβ42 into a nontoxic one[1].
PBT434 methanesulfonate is a potent, orally active and cross the blood-brain barrier α-synuclein aggregation inhibitor. PBT434 methanesulfonate can be used as a iron chelator and modulates transcellular iron trafficking. PBT434 methanesulfonate inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein. PBT434 methanesulfonate prevents the loss of substantia nigra pars compacta neurons (SNpc). PBT434 methanesulfonate has the potential for the research of Parkinson’s disease (PD)[1][2].
HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis[1].
Boc-His(Boc)-OH.DCHA is a histidine derivative[1].
3-Deoxyaconitine is a diterpenoid alkaloid, isolated from Aconitum Carmichaeli Debx.[1].
3-Methyladenine-d3 is the deuterium labeled 3-Methyladenine[1]. 3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K[2].
Copteroside G is a bisdesmosidic glycoside isolated from the epigeal part of the Climacoptera transoxana[1].
Flavokawain B (Flavokavain B) is a chalcone isolated from the root extracts of kava-kava plant and a potent apoptosis inducer for inhibiting the growth of various cancer cell lines. Flavokawain B (Flavokavain B) shows strong antiangiogenic activity. Flavokawain B (Flavokavain B) inhibits human brain endothelial cell (HUVEC) migration and tube formation with very low and non-toxic concentrations[1][2].
Gelucire 44/14 is a potential and safe absorption enhancer for improving the absorption of poorly absorbable drugs including insulin and calcitonin by pulmonary delivery.
DDX3-IN-2 is an active DEADbox polypeptide 3 (DDX3) inhibitor with an IC50 value of 0.3 μM. DDX3-IN-2 shows a broad spectrum of antiviral activity. DDX3-IN-2 has the potential to overcome HIV resistance[1].
Compound 4B proved to be the most effective tyrosinase inhibitor (ic50= 3.80 μ M) It also showed good antioxidant activity.
EN460 is a small molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1); interacts selectively(IC50=1.9 uM) with the reduced, active form of ERO1α and prevents its reoxidation.IC50 value: 1.9 uM [1]Target: ERO1 inhibitorin vitro: Exposure of cells to EN460 or QM295 resulted in the accumulation of an ERO1α form with lower mobility, indicative of the reduced state. EN460 and QM295 were also found to activate an unfolded protein response reporter in cultured 293T cells.
D-Fructose-13C2 is the 13C labeled D-Fructose. D-Fructose (D(-)-Fructose) is a naturally occurring monosaccharide found in many plants.
3-Bromo-L-phenylalanine is a phenylalanine derivative[1].
Tin(IV) mesoporphyrin IX dichloride (Stannsoporfin) is a heme oxygenase (HO) inhibitor being developed for the prevention of hyperbilirubinemia in infants at risk of developing jaundice, extracted from patent WO2011103196A1[1].
Safflower yellow is extracted from the flowers of the plant safflower (Carthamus tinctorius) and as the traditional Chinese medicine it has been extensively used for the treatment of cardio cerebrovascular diseases.
Gamma-decalactone, γ-decalactone is used as an essential food additive with a ruity peach flavor[1]. Ricinoleic acid (12-hydroxy-octadec-9-enoic acid) is used as the substrate in most production processes of γ-decalactone[2].
Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].
BTK-IN-11 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-11 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022063101A1, compound Z2)[1].
α Amylase-IN-1 (Compound 11) is an α-Amylase inhibitor with an IC50 value of 0.5509 μM. α Amylase-IN-1 has antioxidant activity with an IC50 value of 53.49 μM for scavenging DPPH free radicals. IC50 can be used in the study of diabetes and oxidative stress-related diseases.[1]
BCRP-IN-1 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research[1].
PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively [1].