Tokinolide B is isolated from the rhizomes of Ligusticum porter[1].
Antibacterial agent 47, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Cdc7-IN-15 (Example 108) is a cdc7 kinase inhibitor. Cdc7-IN-15 can be used for cancer research[1].
HPK1-IN-25 (example 94) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a enzymatic activity IC50 of 129 nM. HPK1-IN-25 has the potential for cancer research[1].
Biotin-PEG3-C3-NH2 is a PEG-based PROTAC linker, with NH2 functional group, that can be used in the synthesis of PROTACs[1].
Fmoc-Thr-OBu-t is a threonine derivative[1].
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis[1][2][3].
Lys-Arg-Thr-Leu-Arg-Arg (KRTLRR) is a hexapeptide. Lys-Arg-Thr-Leu-Arg-Arg is a substrate of protein kinase C from EGF receptor. Lys-Arg-Thr-Leu-Arg-Arg can be used to determine the activity of protein kinase C[1].
1-Isopropyltryptophan (1-IsoPT) is a IDO1 inhibitor. 1-Isopropyltryptophan decreases the expression of IFN-γ stimulated ID0-1 and ID0-2 mRNA[1].
Thiorphan methoxyacetophenone derivative-d7 is the deuterium labeled Thiorphan methoxyacetophenone derivative[1].
N-(((9H-Fluoren-9-yl)methoxy)carbonyl)-S-(tert-butylthio)-L-cysteine is a cysteine derivative[1].
PACAP (6-27) (human, ovine, rat) is a PACAP receptor antagonist that blocks the canine adrenal catecholamine response to exogenous vasoactive intestinal peptide (VIP). PACAP (6-27) (human, ovine, rat) has the potential to study cardiovascular and neurological diseases[1].
Pyr-Arg-Thr-Lys-Arg-AMC TFA is a AMC peptide. AMC is a decapeptide that is specifically hydrolyzed by proteases such as trypsin and thrombin. The AMC peptide can be used to determine the activity of protease and the potency of enzyme inhibitors[1].
Henagliflozin (SHR3824) is a potent selective sodium-glucose co-transporter 2 (SGLT2) inhibitor with the IC50 values of 2.38 and 4324 nM for human SGLT2 and SGLT1, respectively. Henagliflozin can be used in diabetes research[1].
Mycobactin-IN-2 (compound 49) is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-2 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway[1].
Kukoamine A is a natural occurring spermine derivative, acts as a potent inhibitor of trypanothione reductase (Ki, 1.8 μM), with antihypertensive activity[1].
Libivirumab (17.1.41) is a humanized anti-HBV monoclonal antibody. Libivirumab shows neutralization activity with IC50s of 35, 130 ng/mL for HBsAg, HBeAg, respectively[1].
Alosetron is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.IC50 Value: N/ATarget: 5-HT3 ReceptorAlosetron has an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract. While being a 5-HT3 antagonist like ondansetron, it is not classified or approved as an antiemetic. Since stimulation of 5-HT3 receptors is positively correlated with gastrointestinal motility, alosetron's 5-HT3 antagonism slows the movement of fecal matter through the large intestine, increasing the extent to which water is absorbed, and decreasing the moisture and volume of the remaining waste products. From Wikipedia.
PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity[1].
Calcitetrol(1α, 24, 25-Trihydroxy VD3) is the hormonally active form of vitamin D with three hydroxyl groups.IC50 value:Target: Calcitriol increases blood calcium levels ([Ca2+]) by promoting absorption of dietary calcium from the gastrointestinal tract and increasing renal tubular reabsorption of calcium, thus reducing the loss of calcium in the urine. Calcitriol also stimulates release of calcium from bone by its action on the specific type of bone cells referred to as osteoblasts, causing them to release RANKL, which in turn activates osteoclasts.
Xininurad (XNW3009) is a urate transporter (URAT) inhibitor[1]
Catalpol, an iridoid glycoside, has neuroprotective, anti-inflammatory, and anti-hepatitis virus effects.IC50 Value:Target: neuroprotective, anti-inflammatory, and anti-hepatitis virus natural product.In vitro: Catalpol could be encapsulated into composite nanofibers and induce differentiation of hASCs into neural-like cells, which might offer new avenues in nerve regeneration [1].In vivo: The pharmacokinetics of catalpol in normal and doxorubicin-induced chronic kidney disease rats after oral administration of Rehmannia glutinosa extract was determined, and the extraction recoverie of catalpol was higher than 68.24% [2]. The protective effect of catalpol on renal IRI mice through suppressing phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt)-endothelial nitric oxide synthase (eNOS) and against inflammation, and the possible underlying mechanism [3].
P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1[1].
Ganoderic acid can Inhibitt of the JAK-STAT3 signaling pathway, also inhibit proliferation, viability, ROS.In vitro: A lower doses of Ganoderic acid enhance HLA class II-mediated antigen presentation and CD4+ T cell recognition of lymphoma. [1] ganoderic acid A promots cisplatin-induced cell death by enhancing the sensitivity of HepG2 cells to cisplatin mainly via the signal transducer and activator of transcription 3 suppression. [2] Ganoderic acid A inhibits proliferation, viability, ROS, DPPH, and analyzed the expression of SOD1, SOD2, and SOD3 by Real time PCR in a PC-3 cell in a dose-dependent manner.[3] GA-A effectively inhibites the proliferation of human osteosarcoma HOS and MG-63 cells in a dose-dependent manner, and induced obvious cell apoptosis in both cells.[4]In vivo: Ganoderic acid -treatment significantly prolonged survival of EL4 challenged mice and decreased tumor metastasis to the liver.[1]
Carbon can be used as an excipient, such as decolorizer. 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].
Cyhalofop(Cyhalofop acid) is a recently registered herbicide from the aryloxyphenoxy propionate group in India to control a wide range of grass weed species at various growth stages in rice crop.
Moronic acid, a triterpenoid, is an anti-HIV agent. Moronic acid inhibits viral replication with an EC50 value <1 μg/mL, and shows cytotoxicity in H9 lymphocytes with an IC50 value of 18.6 μg/mL. Moronic acid can be isolated from Brazilian propolis[1].
2′,3′-Anhydroadenosine 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].
Cyclopetide 1 (Compound 1) is an antimicrobial peptide with moderate activity against B. subtilis, with a MIC of 25 μg/mL[1].
4-Oxobedfordiaic acid is an orally active natural product, that can be isolated from Xanthium cavanillesi. 4-Oxobedfordiaic acid shows anti-ulcerogenic activity[1].