TGF-β Receptor Inhibitor

LDN193189 (DM-3189) Tetrahydrochloride (Standard) is the analytical standard of LDN193189 Tetrahydrochloride (HY-12071A). This product is intended for research and analytical applications. LDN193189 (DM-3189) Tetrahydrochloride is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC₅₀ values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.

Nuvisertib hydrochloride (TP-3654 hydrochloride) is an orally active second-generation pan-PIM kinase inhibitor with K_i values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib hydrochloride inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib hydrochloride selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib hydrochloride can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma.

Dorsomorphin (dihydrochloride) (Standard) is the analytical standard of Dorsomorphin (dihydrochloride). This product is intended for research and analytical applications. Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).

M4K2009 hydrochloride is an orally active, blood-brain barrier permeable type I ALK2 inhibitor, with an IC₅₀ value of 8-13 nM against human ALK2. M4K2009 hydrochloride exhibits moderate off-target inhibitory activity against hERG potassium channels (Potassium Channel), with an IC₅₀ of 8 μM against the human channel. M4K2009 hydrochloride can be used in studies related to diffuse intrinsic pontine glioma.

Itacnosertib (Standard) is the analytical standard of Itacnosertib (HY-109179). This product is intended for research and analytical applications. Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC₅₀=8 nM) and JAK2 (IC₅₀=8540 nM). Itacnosertib exhibits anti-leukemic activity.

N-Acetyltaurine hemimagnesium is an orally active endogenous sulfonate that is synthesized from taurine and acetate in the renal cortex. N-Acetyltaurine hemimagnesium supports bacterial growth as a sole fixed nitrogen or carbon source. N-Acetyltaurine hemimagnesium buffers acetyl moieties of mitochondrial acetyl‑CoA in skeletal muscle. N-Acetyltaurine hemimagnesium reduces food intake and body weight in obese and lean wild‑type mice in a GFRAL‑dependent manner. N-Acetyltaurine hemimagnesium can be used for the research of diet‑induced obesity, hyperacetatemia and diabetes.