a 204

A 204 is a polycyclic polyether monocarboxylic acid antibiotic isolated from fermentation of strain of Streptomyces albus.

Jagged-1 (188-204) TFA(219127-21-6 free base) is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epidermal maturation. Exposing submerged keratinocytes monolayers to JAG-1 with elevated calcium concentration produces stratification with loricrin expression and NF-alphaB activation.

JAG-1, scrambled TFA is a scrambled sequence of JAG-1(188-204).

ODM-204 is a novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme (IC50s of 80 nM and 22 nM, respectively).

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM).

Terfenadine ((±)-Terfenadine) is a prodrug metabolized by intestinal CYP3A4 into fexofenadine, an active selective histamine H1-receptor antagonist that possesses antihistaminic and non-sedative effects.

Anticanceragent 204 (Compound 6) is a fluorinated derivative of cinnamamides with anticancer activity. It can arrest the cell cycle of HepG2 cells in the G1 phase and induces apoptosis by reducing mitochondrial membrane polarization (MMP) levels.

Antitumor agent-204 (compound 15a) is a potent antitumor drug with cytotoxic properties. It induces the release of nitric oxide (NO) and the production of reactive oxygen species (ROS). Additionally, Antitumor agent-204 triggers apoptosis and causes cell cycle arrest at the G2/M phase, demonstrating significant antitumor activity.

NLX-204 is a selective, potent agonist of ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor with pKi value of 10.19.

NLX-204 hydrochloride is a potent and selective ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist(pKi = 10.19).

LK 204-545 is a highly selective antagonist of beta1-adrenoceptor.

BSJ-03-204 is a selective Cdk4/6 degrader.

Sdz 204-090 is a cyclic octapeptide analog of somatostatin.

Triptorelin is a GnRH agaonist shown to inhibit estradiol-induced cancer cell proliferationIn vivo: (1) Triptorelin can improve the pregnancy rate by 12% to 15% in ewes6 and downregulate ovarian GnRHR-I expression of female rats, especially in late-growing follicles.(2) Triptorelin immunity blocked EET and UWT, inhibited uterine growth and development and enhance the expression levels s of ESR1, LHR, and FSHR proteins. [1]. Wei S et al. Triptorelin and cetrorelix induce immune responses and affect uterine development and expressions of genes and proteins of ESR1, LHR, and FSHR of mice. Immunopharmacol Immunotoxicol. 2016 Jun;38(3):197-204.

BAY-204 is a CSNK1α/δ inhibitor that can be used in the treatment of proliferative diseases.

VT101 is a TEAD Auto-palmitoylation inhibitor that Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. VT101 inhibited the firefly luciferase reporter dose-dependently and had no 204 effect on the Renilla luciferase reporter.

VT-102 is a TEAD Auto-palmitoylation inhibitor that Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. VT102 inhibited the firefly luciferase reporter dose-dependently and had no 204 effect on the Renilla luciferase reporter.

GC-204 is a selective inhibitor of carbonic anhydrase ix (caix)

BSJ-03-204 triTFA is a potent and selective Cereblon- and CDK-targeted PROTAC (PROteolysis TArgeting Chimera) featuring Palbociclib-based ligands for the degradation of CDK4/6. It exhibits IC50 values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1, indicating strong inhibitory capabilities. Notably, it spares IKZF1/3 from degradation and possesses anti-cancer activity [1].

Leucettinib-92 (compound 92) is a kinase inhibitor selective for the DYRK/CLK families, with IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, 0.8 μM for CLK3, 124 nM for DYRK1A, 204 nM for DYRK1B, 0.16 μM for DYRK2, 1.0 μM for DYRK3, 0.52 μM for DYRK4, and 2.78 μM for GSK3 [1].

Compound 8g (hCA/VEGFR-2-IN-2) is an indolinonylbenzenesulfonamide identified as a potential dual inhibitor targeting cancer-associated isozymes hCA IX/XII and the angiogenic receptor VEGFR-2. It demonstrates VEGFR-2 inhibition with an IC50 of 204 nM and high affinity for hCAs, exhibiting Kis of 3.6 nM for hCA IX, 16.1 nM for hCA II, 16.7 nM for hCA XII, and 75.3 nM for hCA I. Furthermore, compound 8g exhibits antiproliferative effects on breast cancer cells overexpressing VEGFR-2 [1].

Compound 5K (Multi-target kinase inhibitor 2) is a multi-targeted kinase inhibitor demonstrating activity against EGFR, Her2, VEGFR2, and CDK2 with IC50 values between 40 to 204 nM. It exhibits cytotoxic effects on HepG2, HeLa, MDA-MB-231, and MCF-7 cell lines, with IC50 values of 41, 57, 51, and 59 μM, respectively. Additionally, it induces cell cycle arrest and apoptosis specifically in HepG2 cells.

UFP101 is a synthetic peptide that functions as an antagonist of the nociceptin receptor, demonstrating high affinity with a Ki of 0.06 nM in CHO cells expressing the human receptor. It exhibits selectivity for the nociceptin receptor over the κ-opioid receptor, with a Ki of 204 nM in CHO cells expressing the rat receptor. The compound effectively inhibits GTPγS release from the nociceptin receptor in CHO cell membranes, with an EC50 of 1.86 nM. When administered intracerebroventricularly at a dose of 10 nmol/animal, UFP101 prolongs the latency to tail withdrawal in the tail-flick test in mice, indicating its potential as an analgesic. Additionally, at doses of 0.003, 0.03, and 0.3 mg/kg, UFP101 enhances survival in a sepsis mouse model induced by cecal ligation and puncture, suggesting potential therapeutic applications in sepsis management.

Antibacterial agent 204 (Compd P2-56-3) enhances the activity of Rifampin (RIF) against Acinetobacter baumannii and Klebsiella pneumoniae by disrupting the outer membrane of A. baumannii. T [1].