Autophagy Inducer

Letrozole (Standard) is the analytical standard of Letrozole. This product is intended for research and analytical applications. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.

Tepotinib (Standard) is the analytical standard of Tepotinib. This product is intended for research and analytical applications. Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC₅₀ of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation. Tepotinib has antitumor effects.

Vistusertib (Standard) is the analytical standard of Vistusertib. This product is intended for research and analytical applications. Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.

Adezmapimod (hydrochloride) (Standard) is the analytical standard of Adezmapimod (hydrochloride). This product is intended for research and analytical applications. Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator.

Cy5-Paclitaxel is a fluorescently labeled drug probe formed by conjugating the fluorescent dye Cy5 (Cyanine 5) with the chemotherapeutic agent Paclitaxel, which is used to track the cellular uptake, subcellular distribution and drug delivery process of Paclitaxel. The Cy5 (Cyanine 5) fluorophore is covalently linked to Paclitaxel, possessing both fluorescent tracing function and the biological activities of Paclitaxel (promoting tubulin polymerization and arresting the cell cycle at the G2/M phase); after entering cells, Cy5 emits far-red fluorescence, enabling real-time monitoring of drug localization and release.

Gefitinib-d₃ (ZD1839-d₃) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.

Latrepirdine is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β (Aβ) secretion.

Rosiglitazone-d₄ is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

Dactolisib (BEZ235) hydrochloride is an orally active, dual pan-class I PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR with IC₅₀ of 4 nM/5 nM/7 nM/75 nM and 20.7 nM, respectively. Dactolisib hydrochloride (BEZ235) inhibits mTORC1 and mTORC2.

Adezmapimod (Standard) is the analytical standard of Adezmapimod. This product is intended for research and analytical applications. Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod can inhibit p38 MAPK and lead to the inhibition of downstream HSP27 phosphorylation. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator.

Iohexol (Standard) is the analytical standard of Iohexol. This product is intended for research and analytical applications. Iohexol is a non-ionic, water-soluble contrast agent used as a reference marker for the determination of glomerular filtration rate (GFR) at the level of renal function. Iohexol can be used for contrast in myelography, computerized tomography (cisternography, ventriculography) and MicroCT imaging.

Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.

Nilotinib (Standard) is the analytical standard of Nilotinib. This product is intended for research and analytical applications. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

Rosuvastatin-d₆ (ZD 4522-d₆) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM. Rosuvastatin potently blocks hERG current with an IC₅₀ of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

Linifanib-d₄ (ABT-869-d₄; AL-39324-d₄) is deuterium-labeled Linifanib (HY-50751).

Valproic acid (sodium) (Standard) is the analytical standard of Valproic acid (sodium). This product is intended for research and analytical applications. Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC₅₀ in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC₅₀, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.

Atorvastatin hemicalcium trihydrate is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin hemicalcium trihydrate inhibits human SV-SMC proliferation and invasion with IC₅₀s of 0.39 μM and 2.39 μM, respectively.

Letrozole-d₄ (CGS 20267-d₄) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC₅₀ of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.

Gefitinib-d₈ (ZD1839-d₈) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC₅₀ of 2-37 nM in NR6wtEGFR cells.

AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor.