PIM1-IN-2 is a potent and ATP competitive Pim-1 inhibitor with a Ki of 91 nM. PIM1-IN-2 targets the ATP-binding kinase hinge region not by forming classical hydrogen bonds[1].
CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy[1].
L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype[1].
BTL-104 is a monobiotinylated Phos-tag derivative for the detection of phosphopeptides and phosphoproteins[1].
Fenamic acid is a chloride channel blocker[1].
Thiol-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.IC50 Value: 140 nM (α2δ subunit of calcium channel) [1]Target: Calcium Channelin vitro: Gabapentin, baclofen and CGP 44532 all reduced the electrically stimulated release of [3H]glutamic acid (IC50=20 microM, 0.8 microM and 2 microM, respectively). Gabapentin was without effect on the release of [3H]GABA, whilst baclofen (IC50=8 microM) and CGP 44532 (IC50=1 microM) inhibited [3H]GABA release [2]. A large inhibition of calcium currents by gabapentin was observed in pyramidal neocortical cells (up to 34%). Significantly, the gabapentin-mediated inhibition of calcium currents saturated at particularly low concentrations (around 10 microM), at least in neocortical neurons (IC50 about 4 microM) [3].in vivo: Gabapentin produced an anti-allodynic effect over the 7-day period, reducing the expression of pro-inflammatory cytokines but increasing the expression of IL-10 (TNF-α, 316.0 ± 69.7 pg/mL vs 88.8 ± 24.4 pg/mL; IL-1β, 1,212.9 ± 104.5 vs 577.4 ± 97.1 pg/mL; IL-6, 254.0 ± 64.8 pg/mL vs 125.5 ± 44.1 pg/mL; IL-10, 532.1 ± 78.7 pg/mL vs 918.9 ± 63.1 pg/mL). The suppressive effect of gabapentin on pro-inflammatory cytokine expression was partially blocked by the anti-IL-10 antibody [4].Toxicity: No new safety signals or adverse event trends relating to GEn exposure were identified [5].Clinical trial: N/A
Maximin 8 is a antimicrobial peptide that can be found in B. maxima[1].
MOG (44-54), mouse, human, rat is a biological active peptide. (minimal binding epitope for the CD8 + MOG‐specific T cell)
Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
MBP (83-99) is a MBP-specific T cell lines recognizing the immunodominant epitope. MBP (83-99) induces proliferation and IFN-γ secreting of T cells[1][2].
Triprolidine hydrochloride monohydrate is an orally active, cell-permeable and first-generation histamine H1 antagonist[1]. Triprolidine hydrochloride monohydrate is an antihistamine and can be used in allergic rhinitis; asthma; and urticaria[2].
Dehydrocostus Lactone is a major sesquiterpene lactone isolated from the roots of Saussurea lappa.IC50 value:Target:In vitro: Dehydrocostus Lactone promoted apoptosis with increased activation of caspases 8, 9, 7, 3, enhanced PARP cleavage, decreased Bcl-xL expression and increased levels of Bax, Bak, Bok, Bik, Bmf, and t-Bid. We have demonstrated that Dehydrocostus Lactone inhibits cell growth and induce apoptosis in DU145 cells [1]. Dehydrocostus Lactone inhibits NF-kappaB activation by preventing TNF-alpha-induced degradation and phosphorylation of its inhibitory protein I-kappaB alpha in human leukemia HL-60 cells and that dehydrocostus lactone renders HL-60 cells susceptible to TNF-alpha-induced apoptosis by enhancing caspase-8 and caspase-3 activities [2]. Dehydrocostus Lactone inhibited the production of NO in lipopolysaccharide (LPS)-activated RAW 264.7 cells by suppressing inducible nitric oxide synthase enzyme expression.In vivo: Dehydrocostus Lactone decreased the TNF-alpha level in LPS-activated systems in vivo [3].
Norbatzelladine L (Compound 2) is an inhibitor of the catalytic and functional activity of Pdr5p transporter. Norbatzelladine L inhibits Pdr5p ATPase activity with an IC50 of 3.8 µM. Norbatzelladine L shows antifungal, antiparasitic, antiviral, antibacterial and antitumoral activities[1].
MC-Val-Cit-PAB-NH-C2-NH-Boc is a cathepsin cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Boc-D-Leucine monohydrate (Boc-D-Leu-OH hydrate) is an N-Boc-protected form of D-Leucine (L330150). D-Leucine is an unnatural isomer of L-Leucine (L330110) that acts as an auto-inhibitor of lactic streptococci. D-Leucine shows potent anti-seizure effect[1].
H-1152 is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
Gentianose is a predominant carbohydrate reserve found in the storage roots of perennial Gentiana lutea[1].
3’-F-3’-dG(iBu)-2’-phosphoramidite is a purine nucleoside analog. 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].
Bromhexine is a potent expectorant. Bromhexine increase mucociliary clearance and reduces cough. Bromhexine can be used in study various respiratory diseases[1].
Octahydroaminoacridine, a Tacrine analogue, is an acetylcholinesterse (AChE) and butyrylcholinesterase (BChE) inhibitor. Octahydroaminoacridine can be used for Alzheimer's disease (AD) research[1].
Mevastatin (Compactin; ML236B) inhibits HMGCR (HMG-CoA reductase) (Ki for acid form is 1 nM) which in turn inhibits isoprenoid biosynthesis and therefore blocks protein isoprenylation and reduces plasma cholesterol levels in humans. IC50 value: 1 nM (Ki)Target: HMGCRMevastatin induces apoptosis, arrests cancer cells in G1 phase and downregulates cdk 2, 4, and 6, cyclin D1 and E1, p21 and p27. Mevastatin suppresses TNF-induced NF-κB activation (IC50 = ~17 uM), which potentiates apoptosis in human myeloid leukemia cells and thus, may be useful in treating cancer.
Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research[1].
O-1602 is an agonist of GPR55[1].
Croscarmellose sodium is a commonly used pharmaceutical additive approved by the US Food and Drug Administration (FDA). Croscarmellose sodium is used in injectable preparations as a suspending agent to promote solubilization of compounds with poor water solubility. Croscarmellose sodium is also present in tablets as binder, glidant and antiadherent, in bulk laxatives as active principle and as an additive in food products. Croscarmellose sodium can be used as an excipient, such as excipients, disintegrants, aids in disintegration. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1][2].
Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1)[1].
UM729 is a new pyrimidoindole, which has an additive effect with AhR antagonists in preventing differentiation in most AML specimens; collaborates with Ahr suppressors in preventing AML cell differentiation.IC50 value:Target: SR1 and UM729 can be implemented as a standardized supplement in culture media and will pave the way for studies of self-renewal mechanisms and for the identification of new antileukemic drugs through cell-based assays for primary human AML cells.
2’-Azido-2’-deoxycytidine 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].