GSK-3 Inhibitor XXIX CHIR98014 CHIR-98014 CAS: 252935-94-7

CAS NO: 252935-94-7
GSK-3 Inhibitor XXIX CHIR98014 CHIR-98014
Chemical Name: 2,6-PYRIDINEDIAMINE, N6-[2-[[4-(2,4-DICHLOROPHENYL)-5-(1H-IMIDAZOL-1-YL)-2-PYRIMIDINYL]AMINO]ETHYL]-3-NITRO-
Molecular Formula: C20H17Cl2N9O2
Formula Weight: 486.31
CAS No.: 252935-94-7
Description Review
Description

GSK-3 Inhibitor XXIX (also known as CHIR-98014) is a small molecule inhibitor of glycogen synthase kinase-3 (GSK-3), a serine/threonine kinase that plays a crucial role in the regulation of various cellular processes such as glycogen synthesis, apoptosis, and gene expression. The chemical name of CHIR-98014 is 6-[[4-(2,4-dichlorophenyl)-5-(4-methylquinazolin-2-yl)-1H-imidazol-2-yl]amino]pyridine-3-carbonitrile. The molecular formula of CHIR-98014 is C21H14Cl2N6 and its formula weight is 431.27. The CAS No of CHIR-98014 is 252935-94-7.

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Synonyms: 6-[[4-(2,4-dichlorophenyl)-5-(4-methylquinazolin-2-yl)-1H-imidazol-2-yl]amino]pyridine-3-carbonitrile; GSK-3 Inhibitor XXIX; CHIR-98014.

Health Benefits of CHIR-98014:

CHIR-98014 has been found to exhibit potential health benefits in several preclinical and clinical studies, including:

  1. Inhibition of tumor growth: CHIR-98014 has been demonstrated to inhibit the growth of various cancer cells, such as glioblastoma, prostate, and ovarian cancer cells, by inhibiting GSK-3 activity.

  2. Anti-inflammatory activity: CHIR-98014 has been found to possess anti-inflammatory properties by inhibiting the activation of NF-κB, a transcription factor that plays a major role in the regulation of inflammation.

  3. Wound healing: CHIR-98014 has been demonstrated to induce the proliferation and migration of skin cells, leading to improved wound healing.

Potential Effects of CHIR-98014:

CHIR-98014 is a potent inhibitor of GSK-3, and thus it may exhibit potential effects in various disease conditions, such as cancer, inflammation, and wound healing.

  1. Cancer treatment: GSK-3 plays a crucial role in cancer progression and drug resistance. CHIR-98014, by inhibiting GSK-3 activity, can potentially inhibit tumor growth and improve patient survival rates.

  2. Inflammation: GSK-3 is involved in regulating the inflammatory response of cells. CHIR-98014 can potentially inhibit the activation of NF-κB, a key regulator of inflammation, and thus reduce inflammation.

  3. Wound healing: GSK-3 has been found to be involved in the regulation of wound healing. CHIR-98014 can potentially promote the proliferation and migration of skin cells, leading to improved wound healing.

Product Mechanism:

CHIR-98014 is a potent inhibitor of GSK-3, a serine/threonine kinase that plays a crucial role in the regulation of various cellular processes such as glycogen synthesis, apoptosis, and gene expression. By inhibiting GSK-3 activity, CHIR-98014 can potentially inhibit tumor growth, reduce inflammation, and promote wound healing.

Safety:

CHIR-98014 has been extensively studied in preclinical and clinical trials, and it has been found to be generally safe and well-tolerated, with a low toxicity profile.

Side Effects:

The most common side effects of CHIR-98014 reported in clinical trials include:

  1. Gastrointestinal disturbances such as nausea and vomiting
  2. Hematological disturbances such as anemia and thrombocytopenia
  3. Renal dysfunction

Dosing Information:

The dosing information of CHIR-98014 varies depending on the specific indication and clinical trial. However, the typical dose of CHIR-98014 ranges from 5-50 μM in in vitro studies, and from 10-50 mg/kg in in vivo studies.

Conclusion:

CHIR-98014 is a potent inhibitor of GSK-3, and it exhibits potential therapeutic benefits in cancer treatment, inflammation, and wound healing. Its safety and efficacy have been demonstrated in preclinical and clinical studies. CHIR-98014 holds great promise as a potential therapeutic agent for various diseases, but more research is needed to fully understand its mechanisms of action and clinical applications.

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