Iberdomide (CC-220) is a cereblon modulator with an IC50 of 60 nM.
pTH-Related Protein (1-37) (human, mouse, rat), the peptide analogue of pTH-Related Protein (pTHrP). pTHrP refers to parathyroid-hormone-related protein, involved in physiological regulation of bone formation[1].
hCA I-IN-1 (Compound 6q) is a human carbonic anhydrase I (hCA I) inhibitor with Ki values of 38.3, 716.4, 940.1 and 192.8 nM against hCA I, hCA II, hCAIX and hCAXII, respectively[1].
Amylocaine is a local anaesthetic of the ester type. Amylocaine can cause reversible insensitization near the area where it is administered. Amylocaine is used mostly in spinal anesthesia[1].
Chymase-IN-2 is a chymase modulator which is useful in the treatment of inflammatory and serine protease mediated disorders.
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2]Target: HIV Proteasein vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2].in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].
VU0152099 is a potent, selective, CNS-penetrant positive allosteric modulator of M4 mAChR with EC50 of 403 nM; shows no agonist activity but potentiates responses of M(4) to acetylcholine, and is devoid of activity at other mAChR subtypes or at a panel of other GPCRs; reverses amphetamine-induced hyperlocomotion in rats.
D-Nonamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Nonamannuronic acid can be used for the research of pain and vascular dementia[1][2][3][4].
Lansoprazole D4 (AG-1749 D4) is a deuterium labeled Lansoprazole. Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid[1].
O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity[1][2].
TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells[1].
K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM.IC50 value: 4.3 uM [1]Target: SphK2in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30±0.06 uM , while no inhibition of SphK1 at concentrations up to 10 uM was observed. Lineweaver-Burk analysis revealed a Ki of 6.4±0.7 uM for SphK2 and indicated that K145 is a substrate competitive inhibitor (with sphingosine). K145 accumulates in U937 cells, suppresses the S1P level, and inhibits SphK2. K145 also exhibited inhibitory effects on the growth of U937 cells as well as apoptotic effects in U937 cells, and that these effects may be through the inhibition of down-stream ERK and Akt signaling pathways [1].in vivo: K145 also significantly inhibited the growth of U937 tumors in nude mice by both intraperitoneal and oral administration, thus demonstrating its in vivo efficacy as a potential lead anticancer agent [2].
Cassyfiline (Cassythine) is an aporphine alkaloid. Cassyfiline has potent vasorelaxing effects on precontracted rat aortic preparations with an IC50 of 0.09 μM[1].
Bederocin (REP8839) is a Methionyl-tRNA synthetase inhibitor. Bederocin can be used in research of bacterial infection, including S. aureus and MRSA[1].
Fmoc-HoCys(ACM)-OH, a homolog of cysteine, is synthesized from L-methionine. Fmoc-HoCys(ACM)-OH also can be used for the synthesis of solid phase peptide[1].
DDRI-18 is a DNA damage response inhibitor that inhibits the non-homologous end-joining (NHEJ) DNA repair process. DDRI-18 is an effective chemosensitizing agent[1].
m-PEG24-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 191.08, 132.65, and 113.98 nM, respectively. EGFR/HER2/CDK9-IN-3 exhibits remarkable antitumor activity[1].
2-Hydroxypinocembrin is a 2-hydroxyflavanones substrate of flavonoid C-glycosyltransferases[1].
Broussonol E is a diprenylated flavonol. Broussonol E can be isolated from the leaves of Broussonetia kazinoki. Unlike some dinonylated flavonol derivatives, Broussonol E has no cytotoxicity to human tumor cell lines (A549, HCT-8, KB)[1].
Norcaesalpinin E is a natural cassane-type diterpene found in the seed kernels of Caesalpinia crista[1].
4-Allyltoluene, an aromatic compound, can elicite antennal olfactory response of Mediterranean fruit fly measured by electroantennography (EAG)[1].
Glycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local anesthetic that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease[1].
DBCO-S-S-PEG3-biotin is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
3,4-Difluoro-L-phenylalanine is a phenylalanine derivative[1].
GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
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Nevadistinel (NYX-458; NYX-3054) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease[1].
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth[1].
R-30-Hydroxygambogic acid is polyprenylated xanthone epimer that can be isolated from gamboges of Garcinia hanburyi. R-30-Hydroxygambogic acid shows cytotoxicities to Human Leukemia K562 cell lines of IC50 values of 2.89 and 1.27 μM for K562/R and K562/S, respectively. R-30-Hydroxygambogic acid can be used for the research of cancer[1].