BET-IN-16 (Comp I) is a BET inhibitor. BET-IN-16 shows anticancer activity. BET-IN-16 inhibits prostate cancer cell growth, with IC50 values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cells, respectively[1].
Maprotiline-d5 hydrochloride is the deuterium labeled Maprotiline hydrochloride. Maprotiline hydrochloride is a selective noradrenalin re-uptake inhibitor and a tetracyclic antidepressant[1][2].
MK-6240 Precursor (6e) is the synthetic precursor of (18)F]-MK-6240. (18)F]-MK-6240 is a tau positron emission tomography (PET) tracer for neurofibrillary tangles (NFTs), exhibiting high specificity and selectivity for binding to NFTs[1].
Fmoc-Asn(Dod)-OH is an asparagine derivative[1].
Aurein 1.1 is an antibiotic peptide that can be found in the Australian Bell Frogs Litoria raniformis[1].
Fluocinolone Acetonide is a glucocorticoid derivative used topically in the treatment of various skin disorders.Target: Glucocorticoid ReceptorFluocinolone acetonide is a corticosteroid primarily used in dermatology to reduce skin inflammation and relieve itching. It is a synthetic hydrocortisone derivative. The fluorine substitution at position 9 in the steroid nucleus greatly enhances its activity. A typical dosage strength used in dermatology is 0.01-0.025%. One such cream is sold under the brand name Flucort-N and includes the antibiotic neomycin. The Glucocorticoid Receptor(GR) binding affinity (IC50) for Fluocinolone Acetonide(FA) was 2.0 nM, respectively. The values is similar to the GR transactivation EC50 of 0.7 nM for FA, respectively [1, 2].
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats[1].
6-Iododiosmin is a impurity of Diosmin (HY-N0178) raw materials[1].
N-Formyl-D-phenylalanine is a phenylalanine derivative[1].
ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM. ROCK-IN-6 is extracted from patent WO2021164351 A1, example 7, has the potential for glaucoma and retinal diseases research[1].
Fmoc-PEG3-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
3’-O-t-Butyldimethylsilyladenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
m-PEG6-amino-Mal is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
DL-Isoleucine is an isoleucine derivative[1].
FN-1501-propionic acid is a CDK2/9 ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader (HY-130709)[1].
Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.Target: AntibacterialEthambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].
Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research[1][2].
NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB)[1].
DIDS sodium salt is a dual ABCA1 and VDAC1 inhibitor.
Fenvalerate-d6 is the deuterium-labeled Fenvalerate (HY-B2006)[1].
5-Bromo-2’-O-methyluridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Pin1 modulator 1 (compound IIb-219) is a modulator that specifically targets β-Catenin and inhibits the Wnt pathway. Pin1 modulator 1 can be used in the study of Wnt-mediated related diseases, such as cancer[1].
Monlunabant ((S)-MRI-1891) is a solid dispersions compound, as well as a cannabinoid CB1 receptor inhibitor[1].
Riviciclib (P276-00 free base) is a potent CDK9-cyclinT1, CDK4-cyclin D1, CDK1-cyclinB, CDK2-cyclin A, CDK2-cyclin E, CDK6-cyclin D3, and CDK9-cyclin H inhibitor with IC50 values of 20 nM, 63 nM, 79 nM, 224 nM, 2500 nM, 396 nM, 2900 nM, respectively[1].Riviciclib shows antitumor activity on cisplatin-resistant cells[3].
Amisulpride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
3’-O-(2-Methoxyethyl) uridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
SNNF(N-Me)GA(N-Me)IL is a biological active peptide. (Double N-methylated derivatives of amyloidogenic and cytotoxic partial IAPP sequence)
Phospho-Glycogen Synthase Peptide-2 (substrate) is peptide substrate for glycogen synthase kinase-3 (GSK-3) and can be used for affinity purification of protein-serine kinases[1].
Parsatuzumab (Anti-EGFL7; RG 7414) is a humanized monoclonal antibody, acts as an immunomodulator and binds to EGFL7. Parsatuzumab selectively blocks the interaction between EGFL7 and endothelial cells, potentially inhibiting vascular regrowth and reducing vascular endothelial growth factor (VEGF) inhibition[1].