Propargyl-PEG8-SH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
1-Eicosanol is a natural compound with antioxidant activity isolated from Hypericum carinatum[1].
Papilostatin-2 is an anti-angiogenic peptide. Papilostatin-2 can be used for the research of anti-angiogenic[1].
ACT-709478 is a potent, selective, oral active, and brain penetrating T-type calcium channel blocker, with IC50s of 6.4, 18, 7.5 and 2410 nM for Cav3.1, Cav3.2, Cav3.3, Cav1.2, respectively. ACT-709478 is effective on rat and mice, dog, and cynomolgus T-type calcium channel, with no significant species differences. ACT-709478 is used in the research of generalized epilepsies[1].
Ambazone is an orally active membrane active antitumor agent. Ambazone also shows antibacterial and weak antiviral activities[1].
Liriodendrin is an HSF1 agonist can be isolated from E. ulmoides[1].
Phenosulfazole is an effective antiviral agent. Phenosulfazole has the potential for the research of poliomyelitis virus[1].
PDE5-IN-42 (Compound 42) is a potent and orally active PDE5 inhibitor with an IC50 of 0.04 nM. PDE5-IN-42 maintains selectivity over PDE6 and PDE11[1].
Vin-C01 is a potent pancreatic β-cells protective agent with an EC50 of 0.22 µM. Vin-C01 effectively promotes β-cell survival and protects β-cells from STZ-induced apoptosis. Vin-C01 can be used for type 2 diabetes mellitus research[1].
Hoechst 33342 is a DNA minor groove binder used fluorochrome for visualizing cellular DNA.
6-Chlorovanillin is identified in waste waters from bleached kraft pulp mills in Ontario and earlier also elsewhere>[1].
Volucrin is a dimeric phenanthrene derivative that can be isolated from the orchid lusia volucris[1].
MK204 is an aldose reductase (AR) inhibitor that can be used in diabetes research[1].
Methylproamine is a DNA-binding radioprotector which, on the basis of published pulse radiolysis studies, acts by repair of transient radiation-induced oxidative species on DNA.IC50 Value: N/ATarget: DNA-binding radioprotectorin vitro: The extent of radioprotection at the clonogenic survival endpoint increased with methylproamine concentration up to a maximum dose modification factor (DMF) of 2.0 at 10 μM. At least 0.1 fmole/nucleus of methylproamine is required to achieve a substantial level of radioprotection (DMF of 1.3) with maximum protection (DMF of 2.0) achieved at 0.23 fmole/nucleus. The γH2AX focus yield per cell nucleus 45 min after irradiation decreased with drug concentration with a DMF of 2.5 at 10 μM [1]. Methylproamine-treated cells had fewer γH2AX foci after IR compared to untreated cells. Also, the presence ofmethylproamine decreased the amount of lower molecular weight DNA entering the gel as shown by the pulsed field gel electrophoresis assay [2]. Experiments with V79 cells have shown that methylproamine is approximately 100-fold more potent than the classical aminothiol radioprotector WR1065. The crystal structures of methylproamine and proamine complexes with the dodecamer d(CGCGAATTCGCG)(2) confirm that the new analogues also are minor groove binders [3].in vivo: N/AClinical trial: N/A
N-methyl-N'-methyl-O-(m-PEG4)-O'-(propargyl-PEG4)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity[1].
Ozanimod (hydrochloride) (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod (hydrochloride) (RPC-1063) has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod (hydrochloride) (RPC-1063) can be used for the research of relapsing multiple sclerosis (MS) [1].
Ganglioside GM3-d5 (Bovine Milk ammonium salt) is deuterium labeled Ganglioside GM3 (Bovine Milk ammonium salt).
Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia[1].
ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-turmerone ((+)-ar-Turmerone) activates apoptotic protein in human lymphoma U937 cells[3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation and constitutes a promising therapeutic agent for various neurologic disorders[4][5].
Shinjulactone M is a quassinoid isolated from various parts of Ailanthus species. Ailanthus, an important genus of the Simaroubaceae family, can be used as an febrifuge (antimalarial) and anthelmintic, and is given for the research of chronic bronchitis, epilepsy and asthma[1].
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
Damulin B is a dammarane-type saponin found in Gynostemma pentaphyllum.Damulin B can induce cell apoptosis and has anti-cancer activities in vitro[1][2].
Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose.Target: OthersMiglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose. It is primarily used in diabetes mellitus type 2 for establishing greater glycemic control by preventing the digestion of carbohydrates (such as disaccharides, oligosaccharides, and polysaccharides) into monosaccharides which can be absorbed by the body. Miglitol inhibits glycoside hydrolase enzymes called alpha-glucosidases. Since miglitol works by preventing digestion of carbohydrates, it lowers the degree of postprandial hyperglycemia. It must be taken at the start of main meals to have maximal effect. Its effect will depend on the amount of non-monosaccharide carbohydrates in a person's diet. Dietary supplementation with miglitol from pre-onset stage in OLETF rats delays the onset and development of diabetes and preserves the insulin secretory function of pancreatic islets [1]. Miglitol was orally administered at 40 mg/100 g of high-fat diet containing 45% kcal as fat to 12-week-old rats for 29 days, and age-matched rats without the agent were used as the respective controls [2].
Cap-dependent endonuclease-IN-22 is a potent cap-dependent endonuclease (CEN) inhibitor[1].
L-threo-PPMP is a GlcT (UDP-Glc: Ceramide β1,1glucosyltransferase) inhibitor. L-threo-PPMP inhibits glycosphingolipid biosynthesis and induces apoptosis. L-threo-PPMP has anti-cancer activity[1].
Benzyl-PEG6-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Selicrelumab is an agonist CD40 antibody, induces changes in the tumor microenvironment. Selicrelumab can be used for the research of pancreatic cance and neoadjuvant study[1].
Rimocidin, a polyene macrolide, is an antifungal compound. Rimocidin shows broad‐spectrum antifungal activity against multiple plant‐pathogenic fungi[1][2].