Collagen Inhibitor

HIPK2-IN-2 is an orally active and selective HIPK2 inhibitor with an IC₅₀ of 0.36 μM against HIPK2. HIPK2-IN-2 reduces HIPK2 protein expression levels. HIPK2-IN-2 inhibits the proliferation and migration of renal interstitial fibroblasts, alleviates renal tubular injury and collagen deposition, and suppresses TGF-β/Smad3-mediated profibrotic signaling pathways as well as TNF-α/NF-κB-mediated inflammatory signaling pathways in renal cells. HIPK2-IN-2 is used for the study of chronic kidney disease-associated renal fibrosis.

WYRGRLC is a type II collagen-targeting peptide. WYRGRLC specifically binds to type II collagen α1 in articular cartilage in a sequence-dependent manner. WYRGRLC inhibits the binding of WYRGRL-displaying phage (C1-3) to articular cartilage in a sequence-specific manner. WYRGRLC can act as a retention enhancer to improve the cartilage-targeting ability of polymeric nanoparticles and liposomal nanoplatforms, facilitating the delivery of Rapamycin (HY-10219) to chondrocytes. WYRGRLC can be used in studies related to osteoarthritis.

Methyl cholate-d₅ is the deuterium labeled Methyl cholate. Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis.

HIPK2-IN-1 is an orally active and selective HIPK2 inhibitor with an IC₅₀ of 0.56 μM. HIPK2-IN-1 exerts antifibrotic and anti-inflammatory activities. HIPK2-IN-1 binds to HIPK2, inhibits the downstream TGF‑β/Smad3, p53, and TNF‑α/NF‑κB signaling pathways, reduces the expression of fibrotic markers, suppresses cell proliferation and migration, and alleviates renal tubular injury and collagen deposition. HIPK2-IN-1 is used for the study of renal fibrosis associated with chronic kidney disease.

NSC 90469 (Standard) is the analytical standard of NSC 90469. This product is intended for research and analytical applications. NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity.

LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research.

2ccPA (2ccPA18:1) sodium is a chemically stable cyclic phosphatidic acid derivative and antifibrotic inhibitor-inducer. 2ccPA sodium increases intracellular cAMP levels in skin fibroblasts, downregulates the expression of extracellular matrix (ECM) components, and promotes the production of antifibrotic factors HGF and PGE₂. 2ccPA sodium ameliorates Bleomycin hydrochloride (HY-17565A)-induced skin fibrosis in mice and can be used for research on systemic sclerosis (SSc) and other fibrotic disorders.

LOXL2/sGC modulator-2 (Compound 9k) is a selective and orally active lysyl oxidase-like 2 (LOXL2) and soluble guanylate cyclase (sGC) dual-target regulator. LOXL2/sGC modulator-2 shows inhibitory activity for LOXL2 with an IC₅₀ of 0.1 μM and can activate sGC. LOXL2/sGC modulator-2 can ameliorate vascular remodeling and reduce pulmonary artery pressure. LOXL2/sGC modulator-2 can downregulate PKG1, PCNA, α-SMA, collagen I and fibronectin levels. LOXL2/sGC modulator-2 can be used for the research of pulmonary arterial hypertension .

Antifibrotic agent 2 (Compound 636) is a polycyclic pyridinone derivative with antifibrotic activity. Antifibrotic agent 2 reduces the pathological accumulation of fibrosis-related proteins such as fibronectin and collagen, prevents excessive fibrous connective tissue from depositing in organs or tissues, and reverses or delays the remodeling of tissue fibrosisby regulating the abnormal proliferation and activation of fibroblasts. Antifibrotic agent 2 can be used for research on pulmonary fibrosis.

C11 peptide-1 is an antifibrotic agent that binds directly to Collagen I. C11 peptide-1 physically disrupts Collagen I interaction with Lumican. C11 peptide-1 reduces inflammatory infiltration and inhibits the ERK1/2 and Smad2/3 signaling pathways. C11 peptide-1 can be used for the research of liver fibrosis.

12-O-Tiglyl-phorbol 13-dodecanoate (TD13) is a potential inhibitor with anti-hepatic fibrosis activity, and it belongs to a series of derivatives of oral APOL2 inhibitors and anti-hepatic fibrosis agents. It shows no obvious toxicity in preclinical models. Compounds of the 12-O-Tiglyl-phorbol 13-dodecanoate series inhibit the expression of fibronectin, type I collagen and α-smooth muscle actin in hepatic stellate cells. 12-O-Tiglyl-phorbol 13-dodecanoate can be isolated from the Euphorbiaceae plant Euphorbia fischeriana, and it is applicable to the research of hepatic fibrosis.

Sapanisertib (INK-128; MLN0128; TAK-228) Standard is the analytical standard of Sapanisertib (HY-13328). This product is intended for research and analytical applications. Sapanisertib (INK-128; MLN0128; TAK-228) is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.

680C91 (Standard) is the analytical standard of 680C91 (HY-108681). This product is intended for research and analytical applications. 680C91 is an orally active, selective tryptophan 2,3-dioxygenase (TDO) inhibitor with a K_i of 51 nM. TDO is the key enzyme of tryptophan catabolism. 680C91 can be used for the research of cancer immunotherapy and Alzheimer’s Disease.