Danshensu (sodium salt) is odium salt of danshensu from the widely used Chinese herb Danshen. It can inhibited phenylephrine- and CaCl2-induced vasoconstriction in Ca2+-free medium.In vitro: Sodium danshensu showed a biphasic effects on vessel tension. While low dosage of sodium danshensu produced small contraction possibly through transient enhancement of Ca2+ influx, high dosage produced significant vasodilation mainly through promoting the opening of non-selective K+ channels and small-conductance calcium-sensitive K+ channels in the vascular smooth muscle cells.[1]In vivo: Danshensu did not change the expression of AGEs but partly blocked the increased expression of RAGE in the hippocampus of diabetic mice. Danshensu could ameliorate the cognitive decline in streptozotocin-induced diabetic mice by attenuating advanced glycation end product-mediated neuroinflammation.[2]
Glyphosate-d2 is the deuterium labeled Glyphosate. Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants[1].
AM580 is a selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively.
Chenodeoxycholic acid sodium is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
C16 PEG-Ceramide is a polyethylene glycolylated ceramide. C16 PEG-Ceramide can be used for lipid carrier to delivery. C16 PEG-Ceramide induces autophagy. C16 PEG-Ceramide can be used for cancer research[1][2].
Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity[1][2].
Dantrolene sodium hemiheptahydrate is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction. Dantrolene sodium hemiheptahydrate is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm.
Ungeremine, a phenanthridine type alkaloid, is extracted of the bulbs of Pancratium Illyricum. Ungeremine effectively targets mammalian as well as bacterial type I and type II topoisomerases. Ungeremine displays cytotoxic activity towards the 9 cancer cell lines, including drug-sensitive and MDR phenotypes. Ungeremine induced ferroptosis, necroptosis, autophagy as well as apoptosis mediated by caspase activation, MMP alteration and increase ROS production[1][2].
QW24 exerts potent anti-tumor activity by down-regulating BMI-1 and is used as an effective therapeutic agent for clinical colorectal cancer treatment.
Apocynin-d3 is the deuterium labeled Apocynin[1]. Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM[2][3][4].
Quinacrine is a fluorescent probe for the conformational transitions of the cholinergic receptor protein. Quinacrine shows activity in the low μM range with a mean IC50 of 2.30 μM In the patient AML cells.IC50 value: 2.30 μM (for AML cells)Target:in vitro: Quinacrine is a fluorescent probe for the conformational transitions of the cholinergic receptor protein in its membrane-bound state.[1] In the patient AML samples, Quinacrine showed activity in the low μM range with a mean IC50 of 2.30 μM, statistically significantly lower than that of normal PBMCs; 3.54 μM (P=0.0327; Student's t-test). Samples from patients with chronic lymphocytic, acute myeloid and lymphocytic leukemias as well as peripheral blood mononuclear cells (PBMC) were tested in response to 1266 compounds from the LOPAC1280 library. 25 compounds were defined as hits with activity in all leukemia subgroups (<50% cell survival compared with control) at 10 μM drug concentration. Only Quinacrine showed concurrent high activity in all leukemia subgroups and low activity in normal PBMCs and was, therefore, selected for further preclinical evaluation. Quinacrine also induced early inhibition of both DNA and protein synthesis. Quinacrine have repositioning potential for treatment of acute myeloid leukemia by targeting of ribosomal biogenesis.[2]
Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression[1][2][3][4][5].
Thalidomide D4 is a deuterium labeled Thalidomide. Thalidomide is initially promoted as a sedative, inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties[1][2].
Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor with an IC50 of 12 nM.
5-Azacytidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.
Pentoxifylline-d6 (BL-191-d6) is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
Nilotinib-d3 (AMN107-d3) is the deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1][2].
Forigerimod (IPP-201101) is a CD4 T-cell modulator. Forigerimod is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) [1][2][3][4].
MLi-2 is an a potent, highly selective, orally available, brain penetrant inhibitor of LRRK2 with an IC50 of 0.76 nM.
Heparin sodium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa.
Pyriproxyfen is a juvenile hormone analog, preventing larvae from developing into adulthood and thus rendering them unable to reproduce. Pyriproxyfen is a pyridine-based pesticide which is found to be effective against a variety of arthropoda.
Necrostatin-1 is a potent, selective and cell-permeable necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. It acts by inhibiting the death domain kinase RIP (RIP1) in the necroptosis pathway.
A potent PIKfyve inhibitor that inhibits autophagy by impairing lysosomal maturation, potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A; blocks the Ca(2+)-dependent exocytosis of lysosomes induced by ionomycin or plasma membrane wounding, without affecting the process of resealing, induces the formation of giant vacuoles.
Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca2+ channel antagonist and vasodilator[1][2][3].