n137

Carbetimer is a partially imidized copolymer of ethylene & maleic anhydride with average MW approx 1,200 daltons; capable of specific stimulation of immune response. Carbetimer is a low molecular weight polymer derived from ethylene and maleic anhydride with potent antineoplastic activity. Preclinical studies have shown antitumor effects against many tumor cell lines including B 16 melanoma. Its antitumor actions are felt to include both reduction of uridine and cytidine nucleoside triphosphate as well as the diminution of pyrimidine salvage by inhibiting uridine, cytidine, and thymidine kinase. Besides direct antiproliferative effects, Carbetimer could act through immunomodulation, as suggested by the induction of cytotoxic T-cells in mice and the discordant in vitro and in vivo activities against the Lewis lung carcinoma model.

Jun13728 is a potent and covalent inhibitor of the SARS-CoV-2 papain-like protease, with an IC50 value of 0.1 μM. This compound is applicable for antiviral research related to SARS-CoV-2.

PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R).

CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values ​​of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC.

EGFR-IN-137 (Compound 4c) acts as an inhibitor of aromatase and EGFR, with IC50 values of 1.67 μg/mL and 0.08 μg/mL, respectively. It hinders the proliferation of cancer cells MCF-7 and MDA-MB-231, with IC50 values of 1.62 µM and 4.14 µM. Additionally, EGFR-IN-137 induces cell cycle arrest at the G0/G1 phase in MDA-MB-231 cells and triggers apoptosis through a caspase-dependent pathway.

ASN-1377642 is an NK1 receptor antagonist with a Ki value of 251 nM. It demonstrates antitumor activity in breast cancer cells with high expression of NK1R-Tr.

CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.

Amylin (1-37) (human) (hIAPP (1-37)), a peptide hormone located in pancreatic beta-cell secretory granules, is characterized by an amidated C-terminus and a disulfide bond between cysteine residues 2 and 7 [1].

PTH-Related Protein (1-37) (human, mouse, rat) is a peptide analog of parathyroid-hormone-related protein (pTHrP), which plays a role in the physiological regulation of bone formation [1].

Alpha-Amyrin (alpha-Amyrine) is an inhibitor of trypsin and chymotrypsin with antineoplastic effects. alpha-Amyrin can be used in studies about acting as a hepatomodulatory.

α-Humulene (Alpha-caryophyllene) is extracted from S.officinalis essential oil.α-Humulene can inhibit tumor cell growth.α-Humulene also shows anti-inflammatory effects, probably by interfering with TNFalpha production and COX-2 and iNOS expression.

Alpha-Chaconine has anti-inflammatory effect, associated with the suppression of AP-1, and supports its possible therapeutic role for the treatment of sepsis. Alpha-Chaconine also has cytotoxic effects.

α-Lapachone has antineoplastic activity, it shows an approximately trypanocidal activity against Trypanosoma cruzi.

α-Solanine (alpha-Solanine) is an alkaloid derived from potato with anticancer and antitumor activity, attenuating chondrocyte death by inhibiting the NF-κB pathway. α-Solanine inhibits the proliferation and migration of glioma cells but promotes apoptosis of glioma cells.

α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.

α-Viniferin known as 2-arylbenzofuran flavonoids, that are inhibitors of prostaglandin H2 synthetase. α-Viniferin has anti-Alzheimer's disease, anti-tuberculosis, anti-tumor, anti-inflammation, anti-diabetes and other pharmacological activitie

Alphitolic acid, a terpenoid from Potentilla freyniana Bornm, is a selective 3-hydroxy-3-methylglutamic acid coenzyme-A synthase 2 (HMGCS2) inhibitor with anti-inflammatory and anticancer activity that inhibits T cell proliferation in a concentration-dependent manner. Alphitolic acid induces apoptosis and autophagy.