Cholesterol-d6 is the deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins[1][2]. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist[3][4].
Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer[1].
Mucicarmine is used in the histological visualization of acid mucopolysaccharides in tissue sections. Mucicarmine can identify mucin (deep rose), which is useful in determining the mucin positive cancer (such as liver carcinoma)[1].
Benurestat is an orally active urease inhibitor. Benurestat can be used for infected ureolysis research[1].
Iedaborbactam, as a beta-lactamase inhibitor (WO2015191907, Example 62), can be used for the research of bacterial infections[1].
Luisol A, an aromatic tetraol, is a major metabolite of an estuarine marine actinomycete of the genus Streptomyces. Luisol A, anthraquinone antibiotic analog, is an ADC Cytotoxin[1].
Urinary Incontinence-Targeting Compound 1 is a sulfonanilide derivative, used in the research of urinary incontinence.
MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of ERK2 by MEK1 with an IC50 value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable[1].
INSCoV-601I(1) is a potent inhibitor of Mpro (3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-601I(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1)[1].
Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA[1][2].
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.IC50 value: 9 nM [1]Target: NMDA receptor subtype of NR1C & NR2Bin vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity [1]. Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays [2].in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation [3].
2-hexyldecanoic acid can be used as an amidating agent [1].
Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon[1][2].
6,7-Dihydroxy-4-coumarinylacetic acid is a potent and selective inhibitor of ALR2. 6,7-Dihydroxy-4-coumarinylacetic acid inhibits ALR2, SDH andALR1 with IC50s of 9.6, 288 and 66.3 μM, respectively. 6,7-Dihydroxy-4-coumarinylacetic acid clearly suppresses galactitol accumulation[1].
H-Ser(Bzl)-OH.HCl is a serine derivative[1].
Pemetrexed-d5 is the deuterium labeled Pemetrexed[1]. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[2].
Firzacorvir is a cyclic sulfamide compound and modulates HBV core protein. Firzacorvir has anti-HBV activity with EC50 < 1 μΜ[1].
Carboxy-PTIO is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model[1][2][3].
Cysteine Thiol Probe is a thiol-based probe designed to label electrophilic natural products. Cysteine Thiol Probe possesses each of the characteristics of an ideal pharmacophore probe, and has a chromophore. Cysteine Thiol Probe is capable of engaging enone-, β-lactam-, and β-lactone-based electrophilic metabolites[1][2].
H-Pro-Met-OH is a dipeptide containing proline and methionine, which can serve as a substrate for prolinase. H-Pro-Met-OH can also be used for the synthesis of polypeptides[1][2].
ATX-002 is a property-tunable lipid for RNA drug delivery.
Cys(Npys)-(Arg)9 is a cell penetrating peptide. Cys(Npys)-(Arg)9 is comprised of 9 D-Arginine residues and an activated cysteine residue C(Npys). Cys(Npys)-(Arg)9 can be used as a carrier peptide applicable in conjugation and cell permable studies[1].
BRD4-IN-2 is a bromodomain BRD4 inhibitor with an IC50 value of 9.9 nM.
Z-Ser(Tos)-OMe is a serine derivative[1].
SN50 is a cell permeable inhibitor of NF-κB translocation. Sequence: Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Val-Gln-Arg-Lys-Arg-Gln-Lys-Leu-Met-Pro;AAVALLPAVLALLAPVQRKRQKLMP.
ADG-2e is a potent antibacterial agent with MICs of 16, 4, 2, and 2 μg/mL for E. coli [KCTC 1682], P. aeruginosa [KCTC 1637], B.subtilis [KCTC 3068], and S. aureus [KCTC 1621], respectively. ADG-2e shows anti-metastatic activity against breast cancer cells[1].
TB500 is a synthetic version of an active region of thymosin β4. TB500 is claimed to promote endothelial cell differentiation, angiogenesis in dermal tissues, keratinocyte migration, collagen deposition and decrease inflammation.
Nanterinone (UK 61260) is a positive inotropic and arterial vasodilating agent. Nanterinone is a phosphodiesterase inhibitor[1].
Compounds 6B and 14g showed significant inhibitory effect on tumor related subtype HCA IX with low nanomolar potency, while 6K was effective on HCA XII. Compounds 6B, 14g and 6K can be considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
DSTYSLSSTLTLSK is a generic human peptide and can be used for infliximab quantitative detection[1]. Infliximab (Avakine) is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α.