Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active[1][2].
TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM[1].
2-Deoxy-D-glucose-13C-1 is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
Mal-amido-PEG3-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Pomalidomide is an anti-angiogenic agent and an immunomodulator. Pomalidomide inhibits TNF-α release in LPS stimulated human PBMC with an IC50 of 13 nM.
Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor.
Carubicin hydrochloride is a microbially-derived compound. Carubicin hydrochloride is an effective inhibitor of VHL-defective (VHL−/−) CCRCC cell proliferation. Carubicin hydrochloride also induces apoptosis by a mechanism independent of p53 or hypoxia-inducible factor HIF2. Carubicin hydrochloride has the potential for the research of cancer diseases[1][2].
BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.
Geniposidic acid is an effective anticancer and radioprotection agent.Target: OthersMice were given an intraperitoneal injection of Geniposidic acid (GA) (12.5, 25, 50 mg/kg) 1 h before receiving GA against d-galactosamine (GalN) (800 mg/kg)/LPS (40 μg/kg). Liver and blood samples were collected 1 and 8 h after GalN/LPS injection. The survival rate of the GA group was significantly higher than the control. GalN/LPS increased serum aminotransferase activity, serum tumor necrosis factor-α level and hepatic lipid peroxidation and decreased hepatic glutathione content [1]. GA enhanced significantly the postirradiation responses of splenic blastogenesis by PHA. In addition, GA is a potent tumor growth inhibitor when combined with the X-irradiation, though there was no significant synergetic effect on their combined antitumor activity. The preliminary results of GA on hematological and blastogenic observations in this study suggested that it may very well, partially, play a role in an effective anticancer product with the ability to decrease undesirable radiation damage to the hematologic tissue after high dose irradiation [2].
STING agonist-34 (Compound 12L) is a potent STING agonist with an IC50 value of 1.15 μM and an EC50 of 0.38 μM in THP1 cells. STING agonist-34 could be used in cancer research[1].
Stilbamidine is a diamidine compound derived from Stilbene and used chiefly in the form of its crystalline isethionate salt in treating various fungal infections.
C75 trans is an enantiomer of C75. C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM.
PROTAC VEGFR-2 degrader-2（PROTAC-4）, a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100μM)[1].
MNS is a potent and selective inhibitor of Src and Syk tyrosine kinases. target: src, syk. [1]IC50:29.3 (src), 2.5 uM (syk); [1]In vitro: no direct effects on protein kinase C, Ca2+ mobilization, Ca2+-dependent enzymes, PKC activation. MNS potently prevents GPIIb/IIIa activation and platelet aggregation without directly affecting other signaling pathways required for platelet activation. [1] [2] MNS is much more potent than genistein in inhibiting platelet aggregation and protein tyrosine phosphorylation. [2]
Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist[1].
P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.8 nM[1].
N-Boc-MeVal is an ADC linker with BOC protecting group[1].
Lacutoclax is a Bcl-2 inhibitor with antineoplastic activity[1].
Ajoene, a garlic-derived compound, is an antithrombotic and antifungal agent. Ajoene inhibits proliferation and induces apoptosis of human leukaemia CD34-negative cells including HL-60, U937, HEL and OCIM-I. Anticancer activities[1][2].
Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid that can be isolated from Glycosmis chlorosperma. Aristolactam A IIIa is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells[1].
Fmoc-azetidine-3-carboxylic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-azetidine-3-carboxylic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
Stearic acid-1-13C is the 13C labeled Stearic acid. Stearic acid is a long chain dietary saturated fatty acid which exists in many animal and vegetable fats and oils.
AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020)[1].
Tempo-d18 is the deuterium labeled Tempo[1]. Tempo is a classic nitroxide radical and is a selective scavenger of 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[2][3][4][5].
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer[1].
Voruciclib hydrochloride is a clinical stage oral CDK9 inhibitor. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL)[1].
Ala-Ala-Asn-PAB is a peptide cleavable ADC linker for antibody-drug conjugates (ADCs)[1].
Taragarestrant (D-0502) is a potent, orally active estrogen receptor degrader. Taragarestrant has antiproliferative activity against estrogen receptor-positive breast cancer cell lines and has anticancer activity. Taragarestrant can be used for cancer research[1][2].
M435-1279 is a UBE2T inhibitor. M435-1279 acts inhibit the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1[1].
PG-11047 (CGC-11047) is a polyamine analogue. PG-11047 can be used for the research of breast cancer[1].