ERK

Cat. No.

A24129

CAS No.

1611483-29-4

CLH304a

Synonyms: (E)-GABAB receptor antagonist 1

CLH304a (compound 14) is a selective and noncompetitive negative allosteric modulator (NAM) of the GABA$_B$ receptor. It specifically targets the heptahelical domain of the GB2 subunit, inhibiting receptor activity with inverse agonist properties. CLH304a reduces GABA-induced inositol trisphosphate (IP₃) production with an IC₅₀ of 37.9 μM and does not affect other Class C GPCRs, including mGluR1, mGluR2, and mGluR5, indicating high selectivity. Additionally, CLH304a inhibits Baclofen-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABA$_B$ receptors, further supporting its function as a negative modulator. This compound is a valuable tool for investigating GABA$_B$ receptor function and holds potential for therapeutic research in neurological disorders involving GABAergic signaling dysregulation.

Cat. No.

A24158

CAS No.

948044-25-5

ACA-28

ACA-28 (compound 2a) is a potent modulator of the ERK MAPK signaling pathway that exerts anticancer effects through a unique mechanism involving ERK hyperactivation. Rather than inhibiting ERK activity directly, ACA-28 induces sustained ERK activation, which paradoxically triggers apoptosis in cancer cells. It demonstrates selective cytotoxicity, inhibiting the growth of melanoma cells (SK-MEL-28) with an IC₅₀ of 5.3 μM, while showing lower toxicity toward normal human melanocytes (NHEM), with an IC₅₀ of 10.1 μM. ACA-28's ability to exploit ERK signaling dysregulation for selective induction of apoptosis makes it a promising candidate for further development in cancer therapy, particularly in ERK-dependent malignancies.

Cat. No.

A24189

CAS No.

781652-57-1

CDPPB

CDPPB is a selective, orally active allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances AKT and ERK1/2 signaling and upregulates BDNF mRNA expression. CDPPB also inhibits caspase-3 activation and mitigates mitochondrial dysfunction, demonstrating therapeutic potential in improving cognitive impairment, depression, and Huntington’s disease.

Cat. No.

A25644

CAS No.

120481-38-1

Asperosaponin V

Asperosaponin V is an indirect modulator of key signaling pathways, including PI3K/AKT, BMP-2/p38, and ERK 1/2. This compound stimulates the proliferation of marrow stromal cells and promotes differentiation into osteoblasts, making it valuable for studying bone metabolism. Asperosaponin V holds potential for applications in osteoporosis research and fracture healing studies.