TGF-β Receptor Inhibitor

Finbosertib (ALK5-IN-85) (Compound 19) is a TGFβRI (ALK5) inhibitor with an IC₅₀ of <100 nM. Finbosertib can be used for respiratory diseases including idiopathic pulmonary fibrosis, asthma, COPD and lumg cancer, and dermal and ocular fibrotic conditions research.

CPS-021 is a selective PAK4 PROTAC degrader with a DC₅₀ of 50 nM. CPS-021 degrades PAK4 via the ubiquitin-proteasome system. CPS-021 inhibits the migration and invasion of tumor cells, suppresses TGFβ-induced epithelial-mesenchymal transition (EMT) in tumor cells, and can be used in studies related to lung cancer metastasis.

ALK5-IN-25 (compound EX-02) is a potent ALK-5 inhibitor with an IC₅₀ ≤10 nM.ALK5-IN-25 also inhibits ALK-2 (selectivity ALK2/ALK5≤10). ALK5-IN-25 can be used for the research of cancer.

Klotho-derived peptide 1 (KP1 (human)) is a polypeptide with multiple activities including senescence inhibition and renal protection. Klotho-derived peptide 1 binds to TβR2 and ATAD3A, with a K_d value of 1.41 μM for binding to human TβR2 and a K_d value of 0.319 μM for binding to ATAD3A. By binding to TβR2, Klotho-derived peptide 1 blocks the TGF-β/Smad3 and downstream TGF-β signaling pathways, inhibits the expression of miR-223-3p, induces the expression of lncRNA-TUG1, restores endogenous Klotho at the post-transcriptional level, inhibits cellular senescence markers, fibroblast activation and renal tubular epithelial cell apoptosis, blocks cytochrome c release and caspase activation, maintains the integrity of mitochondrial ultrastructure, and restores mitochondrial protein levels. Klotho-derived peptide 1 enters renal tubular epithelial cells via endocytosis, protects against nephrotoxic and hypoxic injuries, and recapitulates the renal protective and anti-fibrotic effects of full-length Klotho. Klotho-derived peptide 1 can be used in research related to kidney diseases such as chronic kidney disease and SARS-CoV-2-associated acute kidney injury.

M4K2308 is a selective ether-linked inhibitor of ALK2 with an IC₅₀ of 2 nM. M4K2308 exhibits exceptional selectivity for ALK2 over ALK5 (IC₅₀ of 224 nM). M4K2308 has the potential for the study of diffuse intrinsic pontine glioma (DIPG) research.

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.

MU1700, a chemical probe, is an orally active and potent ALK1/2 inhibitor with IC₅₀s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability.

TGFβ-IN-3 (Compound 8) is a long-acting tumor-activating prodrug of TGFβR1 inhibitor. TGFβ-IN-3 can achieve selective drug release in tumors, and the tumor/blood ratio is increased by 2.2 times. TGFβ-IN-3 can be used for the study of colon cancer.

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.

ALK5-IN-27 (Compound EX-04) is a potent ALK-5 inhibitor with an IC₅₀ ≤10 nM. ALK5-IN-27 also inhibits ALK-2 (selectivity ALK2/ALK5 ≤10).

Pixofisiran sodium is a siRNA in STP705. It targets to TGF‐β1. STP705 is composed of 2 siRNA oligonucleotides (Pixofisiran and Lixadesiran) that individually target TGF-β1 and COX-2 mRNA.

HM-279 is a potent and orally active ALK5 inhibitor with an IC₅₀ of 4.7 nM. HM-279 shows cross-reactivity with ALK7 (IC₅₀ = 6.8 nM), but HM-279 has fair to good selectivity against other TGF-β receptor family kinases, with 4.5-693-fold selectivity. HM-279 demonstrates antitumor activity in vivo through CD8⁺ T cell immunity. HM-279 can be used for the research of colon cancer.

BUR1 is a BMP upregulator (EC₅₀: 98 nM) and activates BMPRII signalling. BUR1 induces BMP2 and PTGS2 expression. BUR1 reversed pulmonary arterial pressure in Monocrotaline (HY-N0750) induced rats.

Pixofisiran is a siRNA in STP705. It targets to TGF‐β1. STP705 is composed of 2 siRNA oligonucleotides (Pixofisiran and Lixadesiran) that individually target TGF-β1 and COX-2 mRNA.

J-1063 is a potent, selective and orally active ALK5 inhibitor with an IC₅₀ of 0.039 µM. J-1063 shows anti-fibrotic effect by the inhibition of inflammatory infiltration, collagen deposition, and hepatocytes necrosis. J-1063 has the potential for the research of liver fibrosis.

Butrin is a compound found in Butea monosperma flowers. Butrin reduces expression of SIRT1, AURKB, cyclin D1, pAKT, GSK-3β, β-catenin, and TGF-3β expression, enhances apoptosis and ROS production in cancer cells. Butrin downregulates Wnt and NF-κB signaling, mitigates oxidative stress, reduces proinflammatory cytokine (TNF-α, IL-6 and IL-8) production and suppresses neuroinflammation. Butrin inhibits IKK enzyme activity. Butrin can be used for the researches of colorectal cancer, Alzheimer’s disease, and rheumatoid arthritis.

Compound 19A8.8 is a cyclic peptide derived from a CD36 protein fragment. Compound 19A8.8 inhibits the TGF-β/Smad3 signaling pathway by suppressing the interaction between TSP1 and CD36. Compound 19A8.8 has no obvious cytotoxicity. Compound 19A8.8 can be used for research on colon injury and fibrosis.

MCA17-1 shows stronger bioactivity than the positive control obeticholic acid (OCA) against liver fibrosis.

ALK5-IN-28 (Compound Ex-05) is a selective ALK-5 inhibitor (IC₅₀ ≤ 10 nM) that inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit tumor growth in vivo. ALK5-IN-28 can be used in the research of proliferative diseases such as cancer.

TGFBR1 Rat Pre-designed siRNA Set A contains three designed siRNAs for TGFBR1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.