target 5

Target 5 has a wide range of applications in life science related research.

Multi-target kinase-IN-5 (Compound 23) is an orally active ERK1/2 inhibitor with IC50 values of 3.04 nM and 1.57 nM, respectively. It notably suppresses cancer cell proliferation, migration, and invasion, while inducing apoptosis and cell cycle arrest. By inhibiting the phosphorylation of ERK1/2 and downregulating the activity of its downstream substrate RSK, Multi-target kinase-IN-5 exhibits antitumor effects. This compound can be utilized in cancer research.

P53R3 is a potent reactivator of p53, effectively restoring sequence-specific DNA binding to several p53 hot spot mutants, namely p53 R175H, p53 R248W, and p53 R273H. This compound exhibits p53-dependent antiproliferative effects with significantly higher specificity compared to PRIMA-1 and promotes the recruitment of both wild-type p53 and p53 M237I to various target gene promoters. Additionally, P53R3 markedly increases the mRNA, total protein, and cell surface expression of death receptor 5 (DR5), demonstrating its utility in cancer research.

5-fluorouridine is also known as FUrd, 5-Fluorouracil 1-beta-D-ribofuranoside, 5-Fur, or 5-Fluoro-uridine. 5-fluorouridine is a solid. This compound belongs to the pyrimidine nucleosides and analogues. These are compounds comprising a pyrimidine base attached to a sugar. 5-fluorouridine is known to target uridine phosphorylase. FUrd is often used in chemical and biochemical comparison studies with fluorouracil and thymine analogs.

2'-Deoxyguanosine 5'-monophosphate disodium (5'-dGMP disodium) is a GTP derivative that serves as an oxidizable target and is used in forming polycomplexes with other compounds.

Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.

5-Methyluridine (Thymine riboside) is an endogenous methylated nucleoside found in human fluids; methylated purine bases are present in higher amounts in tumor-bearing patients compared to healthy controls.DNA hypermethylation is a common finding in malignant cells and has been explored as a therapeutic target for hypomethylating agents.

D-α-Hydroxyglutaric acid disodium [Disodium (R)-2-Hydroxyglutarate] is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with a Ki of 0.628 mM.

Thymine is one of the four bases of DNA and is able to act as a target for 5-fluorouracil in animal cancer models with Km=2.3 μM.

Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH) inhibitor, exhibiting marked anti-inflammatory efficacy and high target selectivity.

5-Aminouridine (4-Chloro-2-isopropyl-5-methylphenol(chlorothymol)) modifies nucleobases and is incorporated into the target DNA. 5-Aminouridine inhibits the growth of tumors, viruses, and fungi.

AVX 13616, Avexa's leading antibacterial candidate, demonstrates significant in vivo antibacterial efficacy, especially against drug-resistant Staphylococcus pathogens, with an IC50 value of 2-4 µg/ml (MICs) and is targeted as an antibacterial agent. Comparable in activity to mupirocin within a nasal decolonization model, AVX13616 necessitated only a single application for effectiveness. This compound, alongside others, exhibited broad-spectrum antibacterial action, achieving MICs of 2-4 micrograms per milliliter against various isolates, including S. aureus, coagulase-negative staphylococci, enterococci, MRSA, VISA, and VRSA. Aimed for topical use and the treatment of wound infection or catheter-related infections, a solitary 5% (w/w) AVX13616 application (roughly equivalent to 2% mupirocin) proved as efficacious as twice-daily 2% mupirocin over five days in decolonizing MRSA in mice.

AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1). IC50 value: 80 nM [1] Target: DGAT1 in vitro: Plasma AZD7687 exposure was measured repeatedly. AZD7687 markedly reduced postprandial TAG excursion with a steep concent

Liothyronine Sodium is the sodium salt form of liothyronine, a synthetic form of the levorotatory isomer of the naturally occurring thyroid hormone triiodothyronine (T3). Liothyronine sodium (3,3',5-Triiodo-L-thyronine sodium) binds to nuclear thyroid receptors which then bind to thyroid hormone response elements of target genes. As a result, liothyronine sodium induces gene expression that is required for normal growth and development. Liothyronine sodium is more potent and has a more rapid action than thyroxine (T4).

TC-S 7009 is a potent and selective HIF-2α inhibitor (Kd: 81 nM) with significantly higher affinity for HIF-2α than HIF-1α (Kd >> 5μM). TC-S 7009 disrupts HIF-2α heterodimerization, reduces HIF-2α target gene expression, and diminishes DNA binding activity.

Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker composed of PEGs, utilized in the synthesis of various PROTACs that connect two distinct ligands through a linker. One ligand targets an E3 ubiquitin ligase, while the other targets the specific protein of interest, enabling selective protein degradation through the ubiquitin-proteasome system [1].

PROTAC SMARCA2/4-degrader-25 is a PROTAC that targets SMARCA2/4. It consists of the E3 ligase ligand (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, a PROTAC Linker (S)-2-Amino-3,3-dimethylbutanoic acid, and the target protein ligand SMARCA2/4-ligand-3. The conjugate of the E3 ubiquitin ligase ligand and Linker is (S,R,S)-AHPC.

5-Br-4-Cl-Pyrrolo-pyroxypyridine serves as a ligand for target proteins in PROTACs (Ligands for Target Protein for PROTACs). This compound is utilized in the synthesis process.

KRAS ligand 5 acts as the target protein ligand for PROTACK-Ras Degrader-3, which specifically targets and degrades mutated KRAS proteins.

AR ligand-31 is a PROTAC target protein ligand used in synthesizing PROTACAR Degrader-5.

BRD9 Ligand-5 (Compound 172-11) serves as a ligand for the target protein in PROTAC applications. It is utilized in the synthesis of CFT8634.

PROTAC IRAK4 ligand-5, a ligand for the target protein of PROTAC, is instrumental in the synthesis of KT-413.

STAT3ligand 5 is a STAT3 ligand, serving as a target protein ligand for the synthesis of the PROTAC degrader [SD-436].

ER ligand-5 is a ligand for the estrogen receptor (estrogen receptor), which can serve as a target protein ligand for the synthesis of the PROTAC degrader ERαDegrader-10.