Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant.Target: Glucocorticoid ReceptorDeflazacort is an inactive prodrug which is converted rapidly to the active metabolite 21-desacetyldeflazacort. Maximum concentrations of 21-desacetyldeflazacort averaged 116 ng/ml and were observed after 1.3 h. The average area under the curve was 280 ng/ml.h, and the terminal half-life was 1.3 h. 21-Desacetyldeflazacort was cleared significantly faster than both methylprednisolone and prednisolone [1]. Two of 40 boys treated with deflazacort died at 13 and 18 years of age from cardiac failure. The treated boys were significantly shorter, did not have excessive weight gain and 22 of 40 had asymptomatic cataracts. Deflazacort has a very significant impact on health, quality of life and health care costs for boys with DMD and their families, and is associated with few side effects [2].
PIM1-IN-6 (compound 5h) is a potent PIM-1 inhibitor, with an IC50 of 0.60 μM. PIM1-IN-6 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 1.51 and 15.2 μM, respectively[1].
AZD-7295 is a HCV NS5A protein inhibitor, with an EC50 of 7 nM for GT-1b replicon[1][2].
HCV-IN-29 is a hepatitis C virus (HCV) inhibitor exacted from patent US8329159B2, compound 1e[1].
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
[D-Ala2] Leu-Enkephalinamide is an enkephalin analog. [D-Ala2] Leu-Enkephalinamide has great corneal permeability and analgesic effect. [D-Ala2] Leu-Enkephalinamide can be used for the research of ocular diseases[1][2].
3’-Deoxy-3’-α-C-methyl-5-methyluridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
PFE-360 is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo[1][2].
BMS-764459 is a CRF1 antagonist. BMS-764459 can be used for the research of neurological disorders such as depression and anxiety. BMS-764459 is also an atypical CYP1A1 inducer[1][2].
Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression[1].
N-Succinylglycine is a Glycine (HY-Y0966) derivative[1].
NSC 108602 is a nucleoside HIV-1 reverse transcriptase inhibitor.
Tilfrinib (compound 4f) is a potent and selective inhibitor of breast tumor kinase (Brk) with an IC50 of 3.15 nM, which displays anti-proliferative activity and acts as a promising antitumor agent[1].
N-Hexanoyl-DL-homoserine lactone is a bacterial quorum sensing molecule produced in the rhizosphere. N-Hexanoyl-DL-homoserine lactone, a bacterial quorum sensing signal, induces transcriptional changes in Arabidopsis and may contribute to tuning plant growth to the microbial composition of the rhizosphere[1].
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
Sulfapyridine(Dagenan) is a sulfonamide antibacterial.Target: AntibacterialSulfapyridine(Dagenan) is a sulfonamide antibacterial. Sulfapyridine is not prescribed for the treatment in humans any more. However, it may be used to treat Linear IgA Disease. It is a good antibacterial drug, but its water solubility is very dependent on PH. Thus, there is a risk of crystallization within the bladder or urethra, which could lead to pain or blockage. The drug sulfasalazine is structurally one molecule of mesalamine linked to one molecule of Sulfapyridine with an azo bond [1].
PC-766B is a macrolide antibiotic. PC-766B is active against Gram-positive bacteria, and some fungi and yeasts, but inactive against Gram-negative bacteria. PC-766B shows antitumor activity against murine tumor cells. PC-766B has weak inhibitory activity against Na+, K+-ATPase[1][2].
Onalespib (AT13387) is a potent inhibitor of Hsp90, with a Kd of 0.71 nM.
1,2-Diaminoanthraquinone is a sensitivity, specificity and nontoxic nitric oxide (NO) fluorescent probe. 1,2-Diaminoanthraquinone can be used to detect NO productions in live cell and animals with a maximum of absorption at about 540 nm and a detection limit of 5 μM for NO[1][2].
Flavin Adenine Dinucleotide Disodium is a redox cofactor, more specifically a prosthetic group of a protein, involved in several important enzymatic reactions in metabolism.
Nodakenetin, isolated from Angelica decursiva, possesses antioxidant anti-inflammatory activities. Nodakenetin has the potential to be an antiarthritic and nerve tonic[1][2].
(Rac)-Methylindazone ((Rac)-IAA-94) is the racemate of Methylindazone. Methylindazone is a potent CLIC1 channel blocker[1].
Benzaldehyde-PEG4-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
3-Azaspiro[5.5]undecane (4,4-Pentamethylenepiperidine) hydrochloride is an inhibitor targeting the WT influenza A virus M2 (A/M2), with an IC50 of 1 μM[1].
IDH1 Inhibitor 7 (Compound 88) is an IDH1 inhibitor with an IC50 of less than 100 nM[1].
Nimesulide D5 is a deuterium labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties[1][2].
Adenosine-d2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio
Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.
Entrectinib is a potent and orally available Trk, ROS1, and ALK inhibitor; inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively.