KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF. KLTWQELYQLKYKGI is active in gastric ulcer healing in rodents when administered either orally or systemically. KLTWQELYQLKYKGI shows the ability to induce capillary formation and organization in vitro[1].
α-Glucosidase-IN-3 is an oleanolic acid (OA) oxime ester derivativ eagainst α-glucosidase(IC50=0.35 µM) and α-amylase.
UNC3230 is a potent, selective and ATP-competitive phosphatidylinositol 4-phosphate 5 kinase type 1C (PIP5K1C) inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases. UNC3230 has antinociceptive and anticancer effects[1].
(2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion[1].
Anti-inflammatory agent 14 (compound 28) is an anti-inflammatory agent, with a MIC50 of 2 μM for Mtb H37Rv[1].
Sorbifolin, a flavone glucoside, can be isolated from the Pterogyne nitens. Sorbifolin has myeloperoxidase inhibitory and radical scavenging activities. Sorbifolin is also a MPO inhibitor with an IC50 value of 19.2 nM[1].
Bz 423 is a pro-apoptotic 1,4-benzodiazepine with therapeutic properties in murine models of lupus demonstrating selectivity for autoreactive lymphocytes, and activates Bax and Bak.
TTPU is a soluble epoxide hydrolase (sEH) inhibitor with IC50 values of 37 and 3.7 nM for monkey and human sEH, respectively.
Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases[1][2].
GAT228, the enantiomer of GAT211, is an allosteric cannabinoid receptor 1 (CB1) ligand[1].
Buclizine dihydrochloride is an orally active antihistamine antiallergic compound. Buclizine dihydrochloride is a potent teratogen in the rat[1][2][3].
KDM2B-IN-1 is a histone demethylase (kdm2b) inhibitor and can be used for hyperproliferative diseases research[1].
FR-901235 is a new type of immunoactive substance produced by an imperfect fungus, Paecilomyces carneus F-4882. FR-901235 partially restored the impaired delayed-type hypersensitivity to sheep red blood cells in tumor-bearing mice[1].
IL-17 modulator 1 is an orally active, highly efficacious small molecule IL-17 modulators extracted from patent WO 2020127685. IL-17 modulator 1 can be used for the research of preventing, treating or ameliorating a variety of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis[1].
Glycyrrhetic acid 3-O-β-D-glucuronide, isolated from glycyrrhiza, is an important derivative of glycyrrhizin (GL) with an anti -allergic activity[1]. Glycyrrhetic acid 3-O-β-D-glucuronide (GAMG) shows that β‐glucuronidases (β‐GUS) are key GAMG-producing enzymes, displaying a high potential to convert GL directly into GAMG[2].Glycyrrhetic acid 3-O-β-D-glucuronide is valuable as a sweetener.
CYP3A4-IN-2 is a specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.055 μM. CYP3A4-IN-2 is a ritonavir analogue with increased hydrophobicity of the R2 side group and stronger inhibitory effect compared to ritonavir. CYP3A4-IN-2 can be used as an antiviral agent and immunosuppressants[1].
CD161 is a potent and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 28.2 nM and a Ki of 8.2 nM for BRD4 BD1[1]. CD161 is a C-type lectin-like receptor expressed on the majority of natural killer (NK) cells. CD161 demonstrates high selectivity over 24 non-BET proteins containing bromodomains[2].
CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM[1].
Levalbuterol ((R)-Albuterol) hydrochloride is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol hydrochloride is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD[1].
KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.
μ-Conotoxin-CnIIIC is a 22-residue conopeptide that can be isolated from Conus consors. μ-Conotoxin-CnIIIC is a potent and persistent blocker of NaV1.4 channel. μ-Conotoxin-CnIIIC has analgesic, anaesthetic and myorelaxant properties[1][2].
Monolaurin (1-Monolaurin) possesses anti-viral and anti-bacterial activity[1][2].
Clobetasol propionate is a anti-inflammatory corticosteroid used to treat various skin disorders.Target: Glucocorticoid ReceptorClobetasol propionate is a corticosteroid of the glucocorticoid class used to treat various skin disorders including eczema and psoriasis. It is also highly effective for contact dermatitis caused by exposure to poison ivy/oak. Clobetasol belongs to US Class I (Europe: class IV) of the corticosteroids, making it one of the most potent available. It comes in shampoo, mousse, ointment and emollient cream presentations. It has very high potency and typically should not be used with occlusive dressings, or for extended continuous use (beyond two weeks). It is also used to treat several auto-immune diseases including alopecia areata, vitiligo and lichen planus (auto immune skin nodules). From Wikipedia.
Fraxin isolated from Acer tegmentosum, F. ornus or A. hippocastanum, is a glucoside of fraxetin and reported to exert potent anti-oxidative stress action[1], anti-inflammatory and antimetastatic properties. Fraxin shows its antioxidative effect through inhibition of cyclo AMP phosphodiesterase enzyme[2].
Dicamba-5-hydroxypentanoic acid (DCo), synthesized from commercially available 5-hydroxy-dicamba, is an immunizing and heterologous hapten. Dicamba-5-hydroxypentanoic acid (DCo) is chemoselectively activated using one equivalent of DSC (N,N- disuccinimidyl carbonate)[1].
ODN 2395 is a C class oligodeoxynucleotide and can be used as vaccine adjuvant. ODN 2395 is also a TLR9 agonist. Sequence: 5'-tcgtcgttttcggcgc:gcgccg-3'[1].
AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research[1].
Satralizumab, a humanized monoclonal antibody, is a potent Interleukine-6 (IL-6) inhibitor. Satralizumab prevents dTAA formation and progression in rattus norvegicus. Satralizumab can be used for neuromyelitis optica spectrum disorder (NMOSD) and descending thoracic aorta aneurysm (dTAA) research[1][2].
Splenopentin diacetate is a synthetic immunomodulating pentapeptide corresponding to the residues 32-36 of the splenic hormone splenin. Splenopentin diacetate influences both early T and B cell differentiation, to increase the number of antibody-forming cells in mice after gamma irradiation[1][2].
Isoandrographolide possesses cell differentiation inducing and hepatoprotective effect. Isoandrographolide inhibits NLRP3 inflammasome activation and attenuates silicosis in mice[1][2].