D-Lin-MC3-DMA, an ionizable cationic lipid, is a potent siRNA delivery vehicle.
Anticancer agent 9, a glycine derivative, is an anticancer agent. Anticancer agent 9 can inhibit tumor cells viability of myelogenous leukemia and human prostate cancer[1].
mEH-IN-1 (Compound 62) is a potent microsomal epoxide hydrolase (mEH) inhibitor with the IC50 of 2.2 nM. The mEH is a mammalian α/β-fold hydrolase enzyme, expressed in almost all tissues, hydrolyzes a wide range of epoxide containing molecules. The mEH is mainly localized in the endoplasmic reticulum (ER) of eukaryotic cells. mEH-IN-1 can be used for the research of preeclampsia, hypercholanemia and cancer[1].
Puerarin 6''-O-Xyloside, isolated from radix of Pueraria lobata (Willd.), possesses snti-osteoporotic and anti-tumor activity. Puerarin 6''-O-Xyloside induces the mitochondria-mediated apoptosis pathway.[1][2].
5-Nitro-1-(3-azido-3-deoxy-β-D-ribofuranosyl)-2(1H)-pyridinone 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].
Coleon-U-quinone is a potent P-gp inhibitor. Coleon-U-quinone can inhibit cancer cells viability and sensitize multidrug resistance cancer cells to Doxorubicin (HY-15142A)[1].
(24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid is a potent PTP1B inhibitor, with an IC50 of 0.4 μM. (24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid exhibits potent PTP1B inhibitory activity without cytotoxicity[1].
HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM.
KYN-101 (KYN101) is a potent, selective synthetic antagonist of aryl hydrocarbon receptor (AHR) with IC50 of 22 nM in human HepG2 DRE-luciferase reporter assay and 23 nM in murine Hepa1 Cyp-luc assay.KYN-101 reverses IDO/TDO-mediated tumor progression and improves the efficacy of PD-1 blockade in B16 IDO tumor-bearing mice, as well as CT26 colorectal cancer model expressing endogenous high levels of IDO.
BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–drug conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research[1].
ICMT-IN-2 (compound 45) is an inhibitor of ICMT (IC50=0.168 μM)[1].
Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.IC50 value: HDM2 ubiquitin ligaseTarget: in vitro: JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells. JNJ 26854165 is an oral Mdm2 inhibitor which can inhibit the interaction of Mdm2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of Mdm2. A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116.in vivo:JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks.
Hydroxychloroquine sulfate is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling.
UAMC-3203 is a potent and selective Ferroptosis inhibitor with an IC50 of 12 nM.
Veldoreotide (DG3173) a somatostatin analogue, that can bind to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent[1]
hCAIX-IN-10 (Compound 6i) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 61.5 and 586.8 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells[1].
MYC-IN-2 is a MYC protein-protein inhibitor. MYC-IN-2 can be used for the research of cancer[1].
GJ103 is a read-through compound that can induce read through of premature stop codons. GJ103 has potential for the research of genetic disorders caused by nonsense mutations[1].
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research[1][2].
ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity[1][2].
Cepharanthine, an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities[1][2][3]. Cepharanthine attenuates muscle and kidney injuries induced by limb ischemia/reperfusion (I/R)[3]. Cepharanthine induces autophagy, apoptosis and cell cycle arrest in breast cancer cells[4]. Cepharanthine inhibits the HIV-1 entry process by reducing plasma membrane fluidity[5].
Dauricine, a bisbenzylisoquinoline alkaloid in Asiatic Moonseed Rhizome, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer[1].
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib[1][2][3][4].
MHY908 is a potent dual agonist of PPARα and PPARγ[1]. MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity[2].
Treating Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.
Upifitamab rilsodotin (XMT-1536) is an antibody-drug conjugate targeting NaPi2b. Upifitamab rilsodotin can be used for the research of cancer, including Ovarian cancer[1][2].
PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1(JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1 ) histone demethylase an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC5 s of 6 and 4.9 μM, respectively[1].
ATR-IN-7 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-7 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021238999A1, compound 1)[1].
Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, disrupting the formation of actin polymers, with Kd value of 1.4-2.2 nM for F-actin.
Mitophagy activator 1 (compound 16) is an activator of mitophagy. Mitophagy activator 1 is the isomer of EP-0035985[1].