JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model[1].
Lipid CL1 is a novel ionizable lipid for rna delivery.
Lanraplenib (GS-9876) is a highly selective and oral SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans[1][2][3].
(S)-4-Nitrophenyl 4-amino-2-((tert-butoxycarbonyl)amino)-4-oxobutanoate is an asparagine derivative[1].
Fmoc-Lys(Alloc)-OH is a lysine derivative[1].
QS-IN-1 (Compound 3a) is a quorum sensing inhibitor against pseudomonas aeruginosa. QS-IN-1 inhibits biofilm formation[1].
pTH (13-34) (human) is apTH ((Human parathyroid hormone) fragment.
Carbazeran (citrate), a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran (citrate) can be used for the research of metabolic disease[1].
Mogroside IIe, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities[1].
CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.IC50 value: 1.5 uM [1]Target: Rho signaling inhibitorin vitro: CCG-1423 selectively inhibited spontaneous PC-3 prostate cancer cell invasion through a Matrigel matrix, but not the Gαi-dependent LPA-stimulated SKOV-3 ovarian cancer cell invasion, in vitro. At 100 μM, nearly complete inhibition of invasion was achieved with a lesser degree of toxicity than that induced by CCG-1423 at 10 μM [1]. SRF binds to this site in vivo and the SRF inhibitor CCG-1423 completely blocks STARS proximal reporter activity in H9c2 cells [3]. pharmacological MKL-inhibition with CCG-1423 significantly inhibited CCN1 promoter activity as well as mRNA and protein expression[4].in vivo: Pharmacological SRF inhibition by CCG-1423 reduced nuclear MKL1 and improved glucose uptake and tolerance in insulin-resistant mice in vivo [2].
Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19[1][2][3][4][5].
Pinoresinol Diglucoside is one of the major lignans with various pharmacological activities which could be isolated from Duzhong and other plant species.
GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. (R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor.
Rivabazumab is a recombinant antibody against Pseudomonas aeruginosa pcrV[1].
Anticancer agent 77 (Compound 6c) shows anticancer activity, and can be widely used in synthesis and medicinal chemistry research[1].
Impurity C of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).IC50 value:Target: vitamin D receptorCalcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) displays calcemic actions. Calcitriol stimulates intestinal and renal Ca2+ absorption and regulates bone Ca2+ turnover. Calcitriol (1,25-Dihydroxyvitamin D3; Rocaltrol )exhibits antitumor activity; Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) inhibits in vivo and in vitro cell proliferation in a wide range of cells including breast, prostate, colon, skin and brain carcinomas and myeloid leukemia cells.
Cichoriin is an active compounds against SARS-CoV-2, and may be a potential candidate in treating severe COVID-19[1].
Bedaquiline fumarate, a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections.
Cruzain-IN-1 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.
Sincalide is a rapid-acting, synthetic analog of cholecystokinin for intravenous use in postevacuation cholecystography. Sequence: Asp-{SO3H-Tyr}-Met-Gly-Trp-Met-Asp-Phe-NH2.
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity[1][2].
Methyl protogracillin (NSC-698793), isolated from the roots of Dioscorea opposite Thunb, exhibits strong anti-cancer activity[1].
LHRH, the luteinizing hormone-releasing hormone, is a neuropeptide hypothalamic. LHRH regulates reproduction. LHRH can be used for the research of cancer[1].
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes[1]. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities[2].
AMPK activator 7 (compound I-3-24) is a an AMPK activator with the EC50 of 8.8 nM. AMPK activator 7 can be used for the research of diseases involving AMPK, particularly diseases such as type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia and/or hypertension[1].
Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells[1].
6-Hydroxy-2-phenethylchromone possesses antioxidant activity[1].
WAY-213613 is a potent, selective human EAAT2 inhibitor (IC50, 85 nM), exhibits 59- and 45-fold selectivity over human EAAT1 and EAAT3. Inhibits glutamate uptake in rat cortical synaptosomes[1].
Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 µM in PBMC cell. It is an antiviral drug for the treatment of HIV infection.
18-Norabieta-8,11,13-trien-4α-ol (Compound 4) is a natural product that can be isolated from the resins of Populus euphratica[1].