Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research[1].
CM-10-18 is a potent inhibitor of ER α-glucosidase. CM-10-18 demonstrated superior in vitro antiviral activity against representative viruses from four viral families causing hemorrhagic fever. CM-10-18 efficiently protected the lethality of dengue virus infection of mice.
W13 is a potent MsbA inhibitor. W13 is an ATPase stimulator with an EC50 of 5.5 µM[1].
Exaluren (ELX-02) is an synthetic eukaryotic ribosome-selective glycoside that induces read through of nonsense mutations, resulting in normally localized full-length functional proteins. Exaluren is used for the research of cystic fibrosis caused by nonsense mutations[1].
Teduglutide is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide is associated with trophic effects on gut mucosa. Teduglutide can be used for the research of short bowel syndrome (SBS) and Crohn's disease (CD)[1][2].
Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM.
Eberconazole is a dichlorinated imidazole derivative with antifungal activity. Eberconazole is more active than Clotrimazole, Ketoconazole, and Miconazole. Eberconazole has the potential for the research of dermatophytoses with a topical administration[1].
WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM.
5-Fluoroorotic is a selective agent in yeast molecular genetics. 5-Fluoroorotic possesses a well-expressed anticandidal effect close to that of 5-fluorocytosine, as well as moderate antidermatophytal effects[1][2].
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities[1].
MDNI-caged-L-glutamate (MDNI-glu) rapidly and efficiently releases glutamate when photolysed (350-365 nm excitation). MDNI-caged-L-glutamate is inactive at neuronal glutamate receptors (up to 200 μM) and stable at neutral pH. MDNI-caged-L-glutamate is activated by laser to evoke a rapid increase in intracellular ca2+ concentration in astrocytes.
Famciclovir(BRL 42810) is a guanine analogue antiviral drug used for the treatment of various herpesvirus infections.IC50 Value: Refer to penciclovirTarget: HSVFamciclovir is the diacetyl 6-deoxy analog of the active antiviral compound penciclovir with potential use in the treatment of infections caused by the herpes family of viruses [1]. Famciclovir, a synthetic acyclic guanine derivative, is a prodrug which, after oral administration, is rapidly metabolised to the highly bioavailable antiviral compound penciclovir [2].in vitro: Famciclovir induced rapid, dose-dependent suppression of viral replication and reduction in alanine aminotransferase (ALT), with greatest efficacy in the 500-mg tid treatment group. HBV DNA reduction was maintained throughout the treatment period. ALT also steadily declined during the treatment period [3]. in vivo: In rat, following dosing at 40 mg/kg, famciclovir was rapidly and extensively metabolized to the active antiviral compound penciclovir, which reached peak concentrations in the plasma (mean 3.5 micrograms/ml) at 0.5 h [4]. Necrotic hepatitis was significantly (p < 0.01) reduced by treatment with FCV, VACV and ACV at a dose of 50 mg/kg per day divided into 3 doses. No significant effect was achieved with BVDU at 200 mg/kg per day. Treatment with FCV at 50 mg/kg per day, ACV at 100 mg/kg per day, and VACV at 200 mg/kg per day significantly (p < 0.001) decreased mortality in mice [5].Clinical trial: Famciclovir Pediatric Formulation In Children 1 to 12 Years Of Age With Herpes Simplex Infection. Phage3
Methoxycoronarin D can be isolated from Hedychium coronarium J. Koenig and is a potent inhibitor of NF-魏B with an IC50 value of 7.3 渭M. Methoxycoronarin D is also a selective inhibitor of COX-1 with an IC50 value of 0.9 渭M[1].
Tris(dihydrocaffeoyl)spermidine is an active compound. Tris(dihydrocaffeoyl)spermidine can be isolated from potato (Solanum tuberosum) tubers. Tris(dihydrocaffeoyl)spermidine can be used for the research of metabolism[1].
Ribociclib (LEE011) is a highly specific CDK4/6 inhibitor with IC50s of 10 nM and 39 nM, respectively.
FTX-6058 is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 can induce HbF protein expression in cell and murine models. FTX-6058 can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia[1][2].
Propargyl-PEG2-Ms is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
ARTD10/PARP10-IN-2 (compound 19) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1 with IC50s of 2.0 μM, and 9.7 μM, respectively[1].
1b-Benzoyl-8a-cinnamoyl-4a,5a-dihydroxydihydroagarofuran is a sesquiterpenoid isolated from the root bark of Tripterygium hypoglaucum containing a benzoyl and a cinnamoyl group[1].
Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM[1].
Pilsicainide hydrochloride (SUN-1165) is an orally active sodium channel blocker and potent class Ic antiarrhythmic agent[1][2].
Aristolone is a sesquiterpene isolated from Aristolochia debilis[1].
Atorvastatin 3-Deoxyhept-2E-Enoic Acid ((2E)-2,3-Dehydroxy Atorvastatin) is an impurity of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids[1].
HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers[1][2].
Acetyl tetrapeptide-3 combined with Biochanin A (HY-14595) and Acetyl tetrapeptide-3, can stimulate dermal papilla extracellular matrix (ECM) proteins by increasing hydroxyproline, Collagen Type 3, and laminin, yielding a significant improvement in hair follicle size and hair anchoring[1].
Tempo is a classic nitroxide radical and is a selective scavenger of mitochondrial ROS that dismutases superoxide in the catalytic cycle. Tempo induces DNA-strand breakage. Tempo can be used as an organocatalyst for the oxidation of primary alcohols to aldehydes. Tempo has mutagenic and antioxidant effects[1][2][3][4].
Antiproliferative agent-39 (Compound 12) inhibits proliferation of A549, SNU-638, Col2, HT1080, MCF-7 with IC50s of 11, 25, 14, 11, 6.3 μM respectively[1].
Ecallantide (DX-88) is a specific recombinant plasma kallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide can be used to prevent acute attacks of angioedema[1].
SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively.
Isobavachin, an antioxidant isaolated from Psoralea morisiana with a prenyl group at position 8 of ring A, promotes neuronal differentiation and the potential role of its protein prenylation[1][2].