DOCK Inhibitor

Cholesterol sulfate sodium is a naturally occurring, orally active cholesterol derivative that is widely distributed in various tissues and body fluids. Cholesterol sulfate sodium acts as a DOCK2 inhibitor, with IC₅₀ values of 2 μM and 2.9 μM against mouse and human targets, respectively. Cholesterol sulfate sodium restricts excessive neutrophil infiltration and alleviates intestinal inflammation and damage. Cholesterol sulfate sodium serves as an activator of protein kinase C (PKC), which promotes squamous cell differentiation and inhibits skin carcinogenesis. Cholesterol sulfate sodium regulates cholesterol homeostasis and cellular metabolism by activating the AMPK-Sirt1 pathway. Cholesterol sulfate sodium can be used in research related to actinic keratitis, ulcerative colitis, skin cancer, and other conditions.

CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2^DHR-2 for Rac1 in a dose-dependent manner with an IC₅₀ of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9.

Cholesterol sulfate is a naturally occurring, orally active cholesterol derivative that is widely distributed in various tissues and body fluids. Cholesterol sulfate acts as a DOCK2 inhibitor, with IC₅₀ values of 2 μM and 2.9 μM against mouse and human targets, respectively. Cholesterol sulfate restricts excessive neutrophil infiltration and alleviates intestinal inflammation and damage. Cholesterol sulfate serves as an activator of protein kinase C (PKC), which promotes squamous cell differentiation and inhibits skin carcinogenesis. Cholesterol sulfate regulates cholesterol homeostasis and cellular metabolism by activating the AMPK-Sirt1 pathway. Cholesterol sulfate can be used in research related to actinic keratitis, ulcerative colitis, skin cancer, and other conditions.

TBOPP is a selective inhibitor of DOCK1 with an IC₅₀ of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (K_d of 7.1 μM), has anti-tumor activity for broader types of tumors.

Cholesterol sulfate sodium-d₇ is the deuterium labeled Cholesterol sulfate sodium. Cholesterol sulfate sodium is a naturally occurring, orally active cholesterol derivative that is widely distributed in various tissues and body fluids. Cholesterol sulfate sodium acts as a DOCK2 inhibitor, with IC₅₀ values of 2 μM and 2.9 μM against mouse and human targets, respectively. Cholesterol sulfate sodium restricts excessive neutrophil infiltration and alleviates intestinal inflammation and damage. Cholesterol sulfate sodium serves as an activator of protein kinase C (PKC), which promotes squamous cell differentiation and inhibits skin carcinogenesis. Cholesterol sulfate sodium regulates cholesterol homeostasis and cellular metabolism by activating the AMPK-Sirt1 pathway. Cholesterol sulfate sodium can be used in research related to actinic keratitis, ulcerative colitis, skin cancer, and other conditions.

DOCK2-IN-1 (Compound 3) is an analog of CPYPP (HY-110100) and a DOCK2 inhibitor (IC₅₀ = 19.1 μM). DOCK2-IN-1 binds to the DHR-2 domain of DOCK2 and inhibits its mediated Rac guanine nucleotide exchange factor activity. DOCK2-IN-1 blocks chemokine receptor- and antigen receptor-mediated activation of Rac in lymphocytes. DOCK2-IN-1 significantly inhibits chemotaxis and T cell activation. DOCK2-IN-1 can be used in the research of transplant rejection and organ-specific autoimmune diseases.

DOCK5-IN-1 (Compound 14) is the inhibitor for DOCK5 and exhibits no toxicity (100 μM) in cell RAW264.7.

E197 is the inhibitor for DOCK5 that destroys the podosome belt structure of osteoclasts, thereby inhibiting the bone resorption (IC₅₀=3.44 μM in human osteoclast). E197 inhibits the Rac in DOCK5 expressing HEK293 cell with an IC₅₀ of 36 μM. E197 prevents the bone loss in mouse ovariectomized models.