Description

Delcasertib (CAS 949100-39-4), also known as KAI-9803, is a potent and selective peptide-based inhibitor of ?-protein kinase C (?-PKC). ?-PKC is critically involved in signaling cascades triggered by ischemia/reperfusion (I/R), where overactivation can lead to mitochondrial dysfunction, cellular necrosis, and ultimately myocardial injury. Delcasertib intervenes by blocking ?-PKC translocation to mitochondria, an action which preserves cardiac myocyte integrity during reperfusion episodes and has demonstrated substantial reduction in infarct sizes within preclinical animal models.

Because the free form of delcasertib exhibits instability, researchers commonly opt for the hydrochloride salt form, which retains identical biological activity while offering enhanced handling stability—making it preferable for long-term experimental setups.

Manufactured under GMP-certified conditions, our delcasertib ensures batch-to-batch purity and consistency, with packaging options suitable for both bulk wholesale and smaller-scale retail research needs. This product serves as a foundational tool in cardioprotection research, ischemia/reperfusion physiology, and signal-transduction studies within academic or pharmaceutical laboratories.

Note: For laboratory research use only; not intended for human or veterinary applications.

Product Specifications

Mechanism of Action & Research Applications

Delcasertib is designed to selectively inhibit ?-protein kinase C. Functionally, it combines a peptide sequence mimicking the ?V1-1 region of PKC? (which blocks its translocation) with a cell-penetrating TAT (HIV-1 transactivator) motif to facilitate intracellular delivery.

In preclinical rodent models of myocardial ischemia/reperfusion, delcasertib administered directly to ischemic myocardium significantly reduced infarct size, improved post-ischemic reperfusion, and preserved early recovery of left ventricular function .

These findings motivated clinical progression into early-phase trials. In a “first-in-human” dose-escalation study (DELTA-MI), delcasertib administered intravenously or intracoronarily during percutaneous coronary intervention (PCI) for ST-elevation myocardial infarction (STEMI) demonstrated acceptable safety and tolerability, with promising trends toward reduced biomarkers of cardiac injury .

However, the larger Phase IIb PROTECTION-AMI trial involving over 1,000 patients did not show statistically significant reductions in infarct size or improvements in clinical outcomes, though trends in some high-risk subsets suggested potential biological activity.

While clinical efficacy remains unconfirmed, delcasertib continues to be a robust experimental tool for probing ?-PKC-mediated reperfusion injury pathways, mitochondrial protection mechanisms, and apoptosis regulation in controlled research settings.

Side Effects (For Reference in Models)

Though intended strictly for research use, studies demonstrate:

• Safety in early-phase trials, with no major adverse events or QT prolongation PubMed+1.

• Preclinical protective effects in animal models without evidence of systemic toxicity.

• In clinical settings, no significant reduction in infarct size but no observed harm, affirming delcasertib’s suitability for experimental protocols.

These profiles support its utility in laboratory investigations, especially those targeting cellular survival and mitochondrial protection. Always implement standard lab safety protocols when handling this compound.

Disclaimer

Delcasertib (KAI-9803) is provided for laboratory research use only. It is not intended for human or veterinary use, diagnosis, or treatment. Researchers must conduct experiments responsibly and under appropriate institutional guidelines.

Keywords

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