TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment[1].
SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
STF-31 is an inhibitor of glucose transporter 1 (GLUT1, IC50 = 1 μM).IC50 value: 1 μMTarget: GLUT1in vitro: STF 31 is a glucose uptake inhibitor in RCC (renal cell carcinoma) 4 cells. By limiting glucose uptake in cancer cells, the immense energy requirements for the cancer cell is not met and the cell does not have the resources to rapidly proliferate.STF-31, which selectively kills RCCs by specifically targeting glucose uptake through GLUT1 and exploiting the unique dependence of these cells on GLUT1 for survival. STF-31 decreases glycolysis by decreasing glucose transport and not by inhibiting a particular glycolytic step or enzyme.[1]in vivo: STF-31 selectively targets the von Hippel-Lindau (VHL)-deficient kidney cancer cells. STF-31 inhibits VHL-deficient cancer cells by inhibiting Glut1. Daily intraperitoneal injection of a soluble analogue of STF-31 effectively reduces the growth of tumors of VHL-deficient cancer cells grafted on nude mice. On the other hand, STF-31 appears to be an inhibitor with a narrow cell target spectrum.[2]
Novel antitumor agent, inducing PKR-mediated apoptosis and synergizing with IFN
Cytarabine hydrochloride is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM.
Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.Target: CYP11B1Metyrapone is a drug used in the diagnosis of adrenal insufficiency and occasionally in the treatment of Cushing's syndrome (hypercortisolism). Metyrapone blocks cortisol synthesis by reversibly inhibiting steroid 11β-hydroxylase. This stimulates ACTH secretion, which in turn increases plasma 11-Deoxycortisol levels.
BIIB021 is an orally available, fully synthetic inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively.
Dasatinib hydrochloride is a potent and dual AblWT/Src inhibitor IC50 of 0.6 nM/0.8 nM respectively; also inhibits c-KitWT/c-KitD816V with IC50 of 79 nM/37 nM.
8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity[1][2][3].
Danshensu, an active ingredient of Salvia miltiorrhiza, shows wide cardiovascular benefit by activating Nrf2 signaling pathway.
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[1][2][3].
Enzastaurin is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis[1][2][3].
Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz., has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
Soyasapogenol B, an ingredient of soybean, exerts anti-proliferative, anti-metastatic activities. Soyasapogenol B triggers endoplasmic reticulum stress, which mediates apoptosis and autophagy in colorectal cancer[1][2].
Erlotinib mesylate inhibits purified EGFR kinase with an IC50 of 2 nM.
Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
Fmoc-Pro-OH-1-13C is a 13C-labeled Sulfabenzamide. Sulfabenzamide (N-Sulfanilylbenzamide) is an antimicrobial agent and usually consumed in combination with Sulfathiazole and Sulfacetamide. Sulfabenzamide is effective against Gram-positive and negative ba
Hemin is an iron-containing porphyrin. Hemin is an Heme oxygenase (HO)-1 inducer.
17-AAG is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90.
Bexarotene-d3 (LGD1069-d3) is the deuterium labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma[1][2][3][4].
Corynoxine is an enantiomer of Corynoxine B; induces autophagy in different neuronal cell lines, including N2a and SHSY-5Y cells.IC50 value:Tareget: Autophagy inducerIn vivo, Cory promotes the formation of autophagosomes in the fat bodies of Drosophila. By inducing autophagy, Cory promotes the clearance of wild-type and A53T α-syn in inducible PC12 cells. Interestingly, different from its enantiomer Cory B, Cory induces autophagy through the Akt/mTOR pathway as evidenced by the reduction in the levels of phospho-Akt, phospho-mTOR and phospho-p70 S6 Kinase [1]. Corynoxine significantly decreased locomotor activity after oral administration to mice [2].
(Rac)-Hesperetin-13C,d3 is the 13C- and deuterium labeled. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
HaloPROTAC-E is a novel HaloPROTAC potent degrader, inducing reversible degradation of two endosomally localized proteins, SGK3 and VPS34, with a DC50 of 3-10 nM, remarkably selective inducing only degradation of the Halo tagged endogenous VPS34 complex (VPS34, VPS15, Beclin1, and ATG14).
Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
Silibinin-d5 is the deuterium labeled Silibinin. Silibinin (Silibinin A), an effective anti-cancer and chemopreventive agent, has been shown to exert multiple effects on cancer cells, including inhibition of both cell proliferation and migration.
CCT128930 is a potent and selective inhibitor of Akt2 (IC50 6 nM) with 28-fold selectivity over the closely related PKA kinase (IC50 168 nM), as well as 20-fold selectivity over p70S6K (IC50 120 nM).
(-)-Epigallocatechin Gallate is an antioxidant polyphenol flavonoid form green tea, and inhibits the activation of EGFR, HER2 and HER3, with antitumor activity.