RUVBL1/2 ATPase-IN-1 (compound 18) is a potent and selective inhibitor of RUVBL1/2 ATPase with IC50 values of 6.0 and 7.7 μM, respectively. RUVBL1 and RUVBL2 are highly conserved AAA ATPases (ATPases Associated with various cellular Activities) and highly relevant to the progression of cancer. RUVBL1/2 ATPase-IN-1 has the potential for the research of cancer diseases[1].
DIPSO is a biological zwitterionic buffer with the useful pH range from 7.0 to 8.2. DIPSO can interfere meiotic regulation in mouse oocytes. DIPSO also has surfactant activity at 10 mM[1][2].
Myristoyl-(Lys12,27,28)-VIP-Gly-Gly-Thr (free acid) is a high-affinity and selective VPAC2 receptor antagonist[1].
Carasiphenol C is a stilbenoid. Carasiphenol C can be isolated from Caragana sinica. Caragana sinica is widely used as a folk medicine[1].
Methylthiomcresol-C1-benzoic acid is a fenthion hapten that can be used for immunoreagent production (protein conjugates and polyclonal antibodies)[1].
Cimigenol-3-O-α-L-arabinoside is a triterpenoid isolated from Cimicifuga foetida L[1].
Sodium dodecyl sulfate D25 is a deuterium labeled Sodium dodecyl sulfate. Sodium dodecyl sulfate is the most widely used of the anionic alkyl sulfate surfactants[1].
N-(3-Fluoranthyl)maleimide is a thiol fluorescent probe with a lifetime of 20 nsec. N-(3-Fluoranthyl)maleimide has a maximum excitation wavelength of 370 nm and can be used to study the time-dependent processes of biopolymers[1].
DZ2002 is a potent and reversible S-Adenosyl-L-homocysteine Hydrolase(SAHH; AdoHcy Hydrolase) inhibitor with Ki of 17.9 nM.IC50 value: 17.9 nM(Ki) [1]Target: AdoHcy Hydrolase inhibitorin vitro: The cytotoxicity of DZ2002 is significantly less than DHCaA with an IC50 of 100 to 600 μM compared with 6 to 14 μM and shows very little cytotoxicity up to 100 μM. DZ2002 had little effects on lymphocyte proliferation (0.1 μM = 150,604 ± 13,862, 1 μM = 159,894 ± 11,152, and 10 μM = 136,157 ± 21,943 cpm) versus untreated Con A-stimulated cells (168,725 ± 8025 cpm). Similarly, little effect was seen in regards to IL-2 production from DZ2002-treated cells (0.1 μM = 1,838 ± 88, 1 μM = 1,793 ± 58, and 10 μM = 1,731 ± 36 pg/ml) versus untreated Con A-stimulated cells (1,806 ± 43 pg/ml). Although DZ2002 had little effect when T cells were stimulated with Con A, DZ2002 suppressed the MLR by 24.5, 42.3, and 46.0% at dosages of 0.1, 1, and 10 μM, respectively [1]. DZ2002 (500 μmol/L) significantly suppressed TLR agonists-stimulated up-regulation in IL-6, IL-12p40, TNF-α, and IgG and IgM secretion as well as in HLA-DR and CD40 expression of dendritic cells among human PBMCs in vitro. DZ2002 (100 μmol/L) also significantly suppressed TLR agonists-stimulated up-regulation in IL-6 and IL-23p19 production in murine BMDCs, and prevented Th17 differentiation and suppressed IL-17 secretion by the T cells in a BMDC-T cell co-culture system [3].in vivo: As compared with controls, consecutive 7-day i.p. injections of DZ2002 inhibited hemolysis by 24.5 and 18.4% at doses of 0.08 and 2 mg/kg, respectively, thus decreasing anti-SRBC antibody production in vivo [1]. Male C57BL/6 mice immunized with ovalbumin (OVA) were treated with DZ2002 (1, 5, and 25 mg/kg/day) after which lymphocyte proliferation, cytokine production, and IgG responses to OVA were monitored. Administration of DZ2002 dose dependently suppressed OVA-specific lymphocyte proliferation and anti-OVA IgG production compared with controls [2]. Treatment of the mice with DZ2002 significantly attenuated the progression of glomerulonephritis and improved the overall health. In ex vivo studies, treatment of the mice with DZ2002 suppressed the development of pathogenic Th17 cells, significantly decreased IL-17, TGF-β, IL-6, and IL-23p19 production and impeded activation of the STAT3 protein and JNK/NF-κB signaling in splenocytes [3].
H-Glu(Met-OH)-OH could induce oxidation of hydroxyl radical[1].
14-Deoxycoleon U is a natural abietane-type diterpene. 14-Deoxycoleon U exerts an inhibitory effect on tumor cells proliferation. 14-Deoxycoleon U may be a potent anti-cancerous lead compound for lung cancer research[1].
LY 222306 is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor with a Ki of 0.77 nM.
Monohydroxy Netupitant is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist.
Ostarine(MK-2866; GTX-024) is a modulator of human androgen receptor.IC50 value:Target: androgen receptorOstarine (MK-2866) is an androgen receptor modulator (SARM) with an ED50 of 0.44 mg/day. Ostarine (MK-2866) has anabolic activity. Lack of PSA increases in men and hair growth in women further corroborated selective anabolic effects of Ostarine (MK-2866). Ostarine (MK-2866) also resulted in a dose-dependent decrease in LDL and HDL cholesterol levels, with the average LDL/HDL ratio for all doses remaining in the low cardiovascular risk catergory.
2,3,6-Trichlorophenol-d2 is the deuterium labeled 2,3,6-Trichlorophenol[1].
TOK-8801 is a synthesized dihydroimidazothiazole carboxamide and is under development as an immunomodulator.
5,6-Epoxyergosterol is a natural product that can be isolated from endophytic fungus Phyllosticta capitalensis[1].
4-(Benzo[d]oxazol-2-yl)aniline is a potent antitumor agent. 4-(Benzo[d]oxazol-2-yl)aniline has inhibitory activity against mammary carcinoma cell lines[1].
Athidathion(GS-13006) is an organophosphate insecticide.
S-(5′-Adenosyl)-L-cysteine is a cysteine derivative[1].
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Sprengerinin is a potential angiogenesis inhibitor. Sprengerinin exerts anti-tumorigenic effects in vitro[1].
Solasurine is a steroidal alkaloid that can be isolated from Solanum surrattence. Solasurine can interact with the C3-like protease (SARS-CoV-2 main protease) amino acids Phe8, Pro9, Ile152, Tyr154, Pro293, Phe294, Val297, and Arg298[1].
VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia[1].
C6 NBD Phytoceramide is a fluorescently labeled short-chain ceramide analog that can be recognized by mammalian GlcCer synthase (GCS)[1].
N-[(9H-Fluoren-9-ylmethoxy)carbonyl]-2,4-difluoro-D-phenylalanine is a phenylalanine derivative[1].
6-Benzylaminopurine-d5 (Benzyladenine-d5) is the deuterium labeled 6-Benzylaminopurine. 6-Benzylaminopurine is a cytokinin[1].
α-Tocopherol (vitamin E phosphate) is the compound demonstrating the highest vitamin E activity, which is available both in its natural form as RRR-alpha-tocopherol isolated from plant sources.
1-Ethyl-3-methylbenzene-d5 is the deuterium labeled 1-Ethyl-3-methylbenzene[1].
PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.