AA 2379 is an orally active antirheumatic agent. AA 2379 has antiinflammatory, antipyretic activities and reduces pain sensation[1].
Leucomethylene blue (Mesylate) is a common reduced form of Methylene Blue, Methylene Blue is a member of the thiazine class of dyes. Target:Methylene blue has long been used as an antiseptic and therapeutic agent with both human and veterinary applications.
BMH-22, a benzonaphthyridin, is a RNA polymerase I (Pol I) transcription inhibitor independent of p53 function. BMH-22 causes reorganization of nucleolar marker proteins consistent with segregation of the nucleolus. BMH-22 destabilizes RPA194 in a proteasome-dependent manner and inhibits nascent rRNA synthesis and expression of the 45S rRNA precursor. BMH-22 shows potent anticancer activity across many tumor types[1].
(+)-Hydroxytuberosone (compound 7) is a natural pterocarpanone found in Kudzu vine[1].
LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
Estragole (4-Allylanisole), a relatively nontoxic volatile terpenoid ether, is a major component of the essential oil of many plants. Estragole has potent local anesthetic activity and dose-dependently blocks nerve excitability[1]. Estragole displays anti-toxoplasma activity[2].
Anthramycin, a member of the pyrolobenzodiazepine (PBD) family, is a potent antibiotic. Anthramycin has potent antitumor activity. Anthramycin can act as an potent antagonist of cholecystokinin in the central nervous system in mice[1][2][3].
Rebaudioside G is the minor constituent isolated from the leaves of Stevia rebaudiana Bertoni, used for sweeteners research[1].
Omaciclovir (H2G) is a potent and selective inhibitor of herpesvirus replication. Omaciclovir is a nucleoside analog with antiviral activity[1].
AS601245 is a JNK Inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively.
BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits B cell activation in hWB with an IC50 of 2 nM[1].
(R)-Apremilast ((R)-CC-10004) is a enantiomer of Apremilast[1].
T-448 is a specific and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons[1].
Cinobufotalin is one of the bufadienolides prepared from toad venom; has anticancer activity.IC50 value:Target:in vitro: Cinobufotalin(CB) caused significant DNA fragmentation, decrease of MMP, and an increase in the intracellular Ca(2+) ion and ROS production. In addition, CB induced upregulation of Fas protein, proteolytic activation of cytochrome c, caspase-2, -3, -8 and -9 together with the activation of Bid and Bax [1]. cinobufotalin displayed considerable cytotoxicity against lung cancer cells (A549, H460 and HTB-58 lines) without inducing significant cell apoptosis. cinobufotalin mainly induces Cyp-D-dependent non-apoptotic death in cultured lung cancer cells [2]. cinobufotalin (at nmol/L) significantly inhibited HCC cell growth and survival while inducing considerable cell apoptosis. Further, cinobufotalin inhibited sphingosine kinase 1 (SphK1) activity and induced pro-apoptotic ceramide production. cinobufotalin inactivated Akt-S6K1 signaling in HepG2 cells, which was again inhibited by ceramide synthase-1 shRNA-depletion [3].in vivo: Using a mice xenograft model, we found that cinobufotalin inhibited A549 lung cancer cell growth in vivo [2].
LysRs-IN-1 is a Lysyl-tRNA synthetase (LysRs) inhibitor.
Decanoyl-RVKR-CMK (DecRVKRcmk) TFA inhibits over-expressed gp160 processing and HIV-1 replication[1].
AH13, a bi-phenylethychromone, can be isolated from acetone extract of agalwood from Kalimantan[1].
4-Demethyltraxillaside is a lignan that can be isolated from Caulis Trachelospermi[1].
13β-Hydroxylupanine is a natural product that can be found in Caulophyllum robustum Maxim[1].
Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level[1].
Ambroxol (NA-872) is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus.
FEN1-IN-4 (Compound 2) is a human flap endonuclease-1 (hFEN1) inhibitor[1].
Cotransin is a Sec61 translocation inhibitor that acts in a signal-sequence-discriminatory manner to prevent the stable insertion of select nascent chains into the Sec61 translocation channel. Cotransin selectively inhibits the expression of VCAM-1 and p-selectin proteins by inhibiting their co-translational translocation across endoplasmic reticulum (ER) membranes (IC50=0.5-5 µM). Cotransin has potential for studying inflammation and immunity[1][2].
Vactosertib (EW-7197) is an ATP-competitive inhibitor of ALK5 with an IC50 of 12.9 nM. It also inhibits ALK2 and ALK4 at nanomolar concentrations.
DBCO-NHS ester 2 is a derivative of Dibenzylcyclooctyne (DBCO) used in copper-free click chemistry[1].
α-Zearalenol is a Mycotoxin with high affinity for the estrogen receptors (ER),α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects[1].
Etelcalcetide hydrochloride (AMG 416 hydrochloride) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide hydrochloride is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis[1].
Carassin is a 21 amino acid tachykinin-related peptide, it can be isolated from the goldfish brain. Carassin has moderate affinity for rat tachykinin binding sites[1][2].
CHEMBL333994 is a potent and orally effective Cholecystokinin A (CCK-A) antagonist, with an IC50 of 0.67 nM.
Sozinibercept (OPT 302; VGX-300) is a soluble form of VEGFR-3, potently inhibits the activity of VEGF-C/D, which are the proangiogenic factors, inhibiting angiogenesis and vascular leakage. Sozinibercept also inhibits diabetic retinal edema in rats[1][2][3].