T2124

PJ34 hydrochloride (PJ34 HCl) is a potent specific inhibitor of PARPl/2.

Sodium caprate (Sodium decanoate) is the sodium salt of caproic acid, a 10-carbon saturated fatty acid. It has an amphiphilic character and can form liquid crystalline phases and micelles in an aqueous solution.

NSI-189 Phosphate is a novel neurogenic molecule with pleiotropic properties, including antidepressant, procognitive, synaptoplastic, and neurotrophic activities demonstrated in preclinical studies. Its antidepressant activity is monoamine-independent.

Arf1-GEFs-IN-1 is a potent and orally active inhibitor of ADP-ribosylation factor 1-guanine nucleotide exchange factors (Arf1-GEFs), exhibiting an IC50 value of 40 μM in CT26 cells. Primarily, Arf1-GEFs-IN-1 induces tumor regression by triggering anti-tumor immune responses rather than direct cytotoxicity. It effectively enhances CCL5 expression and demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 is applicable in colon cancer research.

PNR-3-80 is a selective inhibitor of apoptotic endonuclease G (EndoG), with an IC50 of 0.67 μM, showing greater inhibition than against DNase I. It exhibits no inhibitory activity against DNase II, RNase A, proteases, lactate dehydrogenase, and superoxide dismutase 1. PNR-3-80 effectively protects human prostate cancer cells from cell death induced by Cisplatin and Docetaxel and inhibits DNA damage and autophagy (autophagy) prompted by Etoposide. This compound is applicable in studies of cellular damage.

Xanthine oxidase-IN-17 is a potent xanthine oxidase (XOD) inhibitor with an IC50 of 298 nM and a Ki of 167 nM. By inhibiting the catalytic activity of XOD, it reduces uric acid production and subsequently decreases the formation of O₂⁻ free radicals. Xanthine oxidase-IN-17 is non-cytotoxic in AML-12 liver cells while effectively inhibiting uric acid formation. It is suitable for research on hyperuricemia and gout.

c-Kit-IN-11 (Compound A7) is a c-Kit inhibitor with an IC50 of 76 nM against Mo7e cells. This compound is applicable for research in inflammatory conditions like asthma and malignant cancers.

5-HT2C agonist-10 (Compound 21) is a 5-HT2C receptor agonist with an EC50 of less than 10 nM. It is utilized in the study of mental disorders.

K-833 is a GPR119 agonist with EC50 values of 39.8 nM, 100 nM, 75.4 nM, and 12.6 nM for human, mouse, rat, and dog respectively. In acute intestinal peptide secretion in mice, K-833 modestly increases the secretion of glucagon-like peptide-1 (GLP-1) and, when used in combination with AM-5262, can synergistically enhance GLP-1 levels. K-833 is applicable in weight loss research.

2-Amino-3,4,8-trimethylimidazo4,5-fquinoxaline-D3 is the deuterium-labeled version of 2-Amino-3,4,8-trimethylimidazo[4,5-f]quinoxaline.

PROTACHer3-binding moiety 2 is an inhibitor of Her3. It is applicable in the synthesis of PROTACHer3 Degrader-8.

VVD-442 is a covalent RAS-PI3K inhibitor that binds covalently to cysteine at position 242 in the RAS-binding domain of PI3Kp110α, thereby inhibiting the interaction between RAS and PI3K. VVD-442 is applicable for research in cancers such as breast cancer.

FLT3-IN-32 hydrochloride is a potent, orally active FLT3 inhibitor with IC50 values of 0.29 nM for FLT3-ITD, 0.77 nM for FLT3-D835Y, and 2.07 nM for FLT3-N676K. It induces apoptosis in FLT3-mutant Ba/F3 cells by reducing the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT). In MV4-11 xenograft models, it demonstrates significant antitumor effects. This compound is suitable for research in acute myeloid leukemia (AML).

GPR40 agonist 8 (Compound 2) is a GPR40 agonist with an EC50 value of 5 nM for hGPR40Ca2+. It is applicable in research related to type II diabetes and obesity.

SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor that disrupts the interaction between PD-1 and PD-L1. It enhances the numbers of T cells, B cells, and natural killer cells. SCL-1 exhibits potent tumor growth inhibitory effects by inducing effector T cells within the tumor and upregulating the expression of long non-coding RNAs as neoantigens, thereby activating cytotoxic T lymphocytes. SCL-1 is applicable in cancer research, including studies on triple-negative breast cancer.

Steroid sulfatase-IN-10 (Example 216) is a potent inhibitor of steroid sulfatase, with an IC50 range of 0.03-0.27 µM. It is applicable in research on inflammatory diseases such as rheumatoid arthritis, type 1 and type 2 diabetes, and systemic lupus erythematosus.

MAGL-IN-22 (Compound 40) is a reversible, competitive, and selective inhibitor of MAGL that is capable of crossing the blood-brain barrier, with an IC50 of 0.34 μM for hMAGL. It exhibits significant antioxidant and anti-inflammatory properties, activating the Nrf2 pathway and markedly suppressing NFκB-mediated inflammation, without inducing cytotoxic effects. MAGL-IN-22 is applicable in research on neurodegenerative diseases, chronic pain, and cancer.

EVT0185 is an orally active ATP citrate lyase (ACLY) inhibitor. In the liver, it is converted by SLC27A2 into a CoA thioester, which interacts with the CoA binding site of ACLY. EVT0185-CoA inhibits ACLY activity with an IC50 of 2.5 μM. It mimics the immune and antitumor effects seen with ACLY gene deletion. Additionally, EVT0185 elevates levels of tumor-infiltrating B cells and the chemokine CXCL13. It is applicable in cancer research, including hepatocellular carcinoma (HCC).

mGluR2 modulator6 (Compound 25-a) acts as an mGluR2 modulator demonstrating anticonvulsant activity in the 6Hz epilepsy model, with enhanced effects when used in combination with Levetiracetam. This compound is valuable for epilepsy research.

Allantoxanamide inhibits uricase.

SMI-10B13 is an inhibitor of oncostatin M (OSM) with a dissociation constant (KD) of 6.6 μM. It effectively inhibits OSM-mediated STAT3 phosphorylation in T47D and MCF-7 cell lines, with IC50 values of 136 nM and 164 nM, respectively. SMI-10B13 demonstrates antitumor activity in a human breast cancer mouse model.

1,3-Dibromobenzene-D4 is the deuterated form of 1,3-Dibromobenzene (TMSM-4314).

PDGFRαkinase-IN-2 is a potent inhibitor of PDGFR-α with an IC50 of 2.1 nM. It exhibits anticancer activity against human colon cancer HT-29 cells, with an IC50 of 1.48 μM. Additionally, PDGFRαkinase-IN-2 demonstrates anti-angiogenic properties in zebrafish models with low embryotoxicity, making it suitable for research in colon cancer and anti-angiogenesis.

Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active activator of Kv7.2/Kv7.3 channels and the TSPO. It activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). This compound protects motor neurons from degeneration caused by exposure to astrocyte-conditioned media from mice and humans with amyotrophic lateral sclerosis/frontotemporal dementia. Additionally, Kv7.2/Kv7.3 activator-3 stimulates axonal growth in dorsal root ganglia through TSPO and Kv7.2/3 activation and exhibits anticonvulsant effects in epilepsy models. It alleviates hyperalgesia in diabetic neuropathy patients, enhances the survival and regeneration of neurons after cervical neuropathy in rats, and accelerates the recovery of normal function in sensory and motor neurons.