nm 107

NM107 (2'-C-Methylcytidine) is a ribonucleoside with broad-spectrum antiviral activity and acts as a nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase, demonstrating an EC50 of 1.85 μM in wild-type replicon cells.

(Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol/L) and VEGFR-3 autophosphorylation (IC50: 45 nmol/L) in HEK cells, respectively. SAR131675 is highly specific for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is a highly specific VEGFR-3-TK inhibitor with significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.

Etamicastat can be used in the research of cardiovascular diseases. Etamicastat (BIA 5-453) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM.

Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a peripherally selective dopamine beta-hydroxylase inhibitor that reduces hypertension.

PCSK9 ligand 1 is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9(Ki of 107 nM).

AGH-107 is a highly selective 5-HT7 receptor agonist that can cross the blood-brain barrier, featuring a Ki value of 6 nM and an EC50 value of 19 nM. Demonstrating high selectivity for central nervous system targets, AGH-107 also exhibits high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.

(R)-SR-C-107 is an orally active inhibitor developed based on ENL (containing YEAST domain protein), designed to target acute myeloid leukemia (AML). The inhibitor has an IC50 of 40 nM and a KD of 144 nM for ENL. In a xenograft mouse model of AML, (R)-SR-C-107 demonstrated in vivo efficacy, achieving a tumor regression rate of 45% at a dosage of 200 mg/kg (PO; QD).

SARS-CoV-2-IN-107 (Compound A7) is an inhibitor of SARS-CoV-2 3CLpro, with an IC50 of 261.3 nM. It inhibits the replication of SARS-CoV-2, exhibiting an EC50 of 11.7 μM. Additionally, SARS-CoV-2-IN-107 demonstrates anti-inflammatory activity in LPS-stimulated RAW264.7 macrophages, with a NO inhibition rate of 68.6%.

CDK9/PARP-IN-1 (compound 37) is an inhibitor of CDK9 and PARP. It demonstrates IC50 values of 118 nM for CDK9 and 107 nM for PARP1. This compound exhibits a broad-spectrum anti-proliferative effect across various cancer cell lines.

PARP1/CDK12-IN-1 (107) is a dual inhibitor that targets both CDK12 and PARP1, exhibiting IC50 values of 285 nM and 34 nM, respectively.

PROTACSOS1 degrader-10 (Compound 11o) is a degrader of son of sevenless 1 (SOS1) that functions through CRBN- and protease-dependent mechanisms. It effectively degrades SOS1 in KRAS-mutated cancer cells SW620, A549, and DLD-1, with DC50 values of 2.23, 1.85, and 7.53 nM, respectively. Additionally, PROTACSOS1 degrader-10 inhibits the proliferation of SW620, A549, and DLD-1 cells, with IC50 values of 36.7, 52.2, and 107 nM, and suppresses ERK phosphorylation.

EBOV-IN-9 (compound 2b) is a Diphyllin derivative that inhibits Ebola virus entry with an EC50 of 40 nM. It effectively combats EBOV-infected monocyte-derived macrophages, showing an EC50 of 107 nM.

PD-L1/HDAC3-IN-1 (PH3) is a dual inhibitor of PD-L1 and HDAC3, exhibiting IC50 values of 89.4 nM for PD-1/PD-L1 and 107 nM for HDAC3. It induces apoptosis and arrests the cell cycle in the G0/G1 phase. PD-L1/HDAC3-IN-1 demonstrates anticancer activity both in vitro and in vivo.

Norquetiapine (N-Desalkylquetiapine) is a metabolite of Quetiapine and acts as a selective HCN1 channel inhibitor with an IC50 of 13.9 μM. It selectively inhibits norepinephrine reuptake and serves as a partial agonist at the 5-HT1A receptor (Ki = 45 nM). Norquetiapine also functions as an antagonist at presynaptic α2 (Ki = 237 nM), 5-HT2C (Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Additionally, it blocks human cardiac sodium channels Nav1.5 in a state-dependent manner. In LPS-injected C57BL/6 mice, Norquetiapine displays partial anti-inflammatory effects. This compound is utilized in research related to depression and inflammation.

SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2.SM1-71 can be used as a kinase probe with anticancer activity and inhibits the proliferation of various cancer cell lines.

Potent Smo antagonist (IC50 = 5 nM). Attenuates the leukemia-initiation potential of AML cells in a serial transplantation mouse model. Also eliminates self-propagation capacity of AML cells. Munchhof et al (2011) Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened. ACS Med.Chem.Lett. 3 106 PMID:24900436 |Fukushima et al (2016) Small-molecule Hedgehog inhibitor attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Sci. 107 1422 PMID:27461445 |Giordani et al (2016) The human Smoothened inhibitor PF-04449913 induces exit from quiescence and loss of multipotent Drosophila hematopoietic progenitor cells. Oncotarget 7 55313 PMID:27486815

SP-96 is a highly effective and selective inhibitor of Aurora B with an IC50 of 0.316 nM. SP-96 shows selective growth inhibition in NCI60 screening, including MDA-MD-468 (GI50=107 nM). SP-96 can be used in triple negative breast cancer studies.

ZLD2218, a potent inhibitor of BRD4 with an IC50 value of 107 nM, has been demonstrated to mitigate kidney injury and fibrosis through extensive studies.

AMPK-IN-3 is a novel, selective and potent AMPK inhibitor with inhibitory effects on AMPK (α2), AMPK (α1) and KDR, with IC50 values of 60.7, 107 and 3820 nM, respectively.AMPK-IN-3 showed anticancer activity in K562 cells.

A2A receptor antagonist 3 (Example 92) is an adenosine A2A receptor antagonist (Ki: 0.4 nM) and a receptor (Ki: 1467 nM).

MEK/PI3K-IN-2 (compound 6s), a potent inhibitor of both MEK and PI3K, demonstrates IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), effectively reducing pAKT and pERK1/2 levels and exhibiting anti-proliferative activity against various tumor cell lines [1].

YX-2-107 is a selective and potent CDK6-degrading PROTAC with an IC50 value of 4.4 nM.YX-2-107 inhibits RB phosphorylation and FOXM1 expression in vitro, and inhibits the development of Ph+ ALL in rats.YX-2-107 can be used for the prophylaxis and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). YX-2-107 can be used for the prevention and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL).

HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis.

Porcn-IN-2 (Example 107) is a potent Wnt pathway inhibitor with an IC50 of 0.05 nM, applicable in cancer research including sarcoma, melanoma, skin cancer, hematological tumors, lymphoma, carcinoma, and leukemia [1].