23-hydroxybetulinic acid is one of the bioactive components responsible for its anticancer activity.In vitro: 23-hydroxybetulinic acid also shows different proliferation inhibitory activity against B16, HeLa, and HUVEC, with the IC50 value of 78.5, 80, and 94.8 uM, respectively. 23-hydroxybetulinic acid can promote cell cycle arrest at S phase and induce apoptosis via intrinsic pathway. 23-hydroxybetulinic acid disrupts mitochondrial membrane potential significantly (p<0.01) and selectively downregulates the levels of Bcl-2, survivin and upregulates Bax, cytochrome C, cleaved caspase-9 23-hydroxybetulinic acid can induce apoptosis in K562 cells. [1] 23-hydroxybetulinic acid enhances sensitivity of doxorubicin (DOX, ADR) on MCF-7/ADR cell lines, indicating its potential to be developed as a novel MDR modulator.[2] 23-HBA significantly improve the sensitivity of the tumor to doxorubicin. [3]
Glycyltyrosine dihydrate is a tyrosine derivative[1].
Idelalisib (CAL-101) is a highly selective and potent p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
Levomefolic acid (5-MTHF) is the natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions. IC50 value: Target: Folate analogLevomefolic acid has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers. Levomefolic acid (5-MTHF) has the prominent antioxidant activity. A high dose of 5-MTHF or folic acid does not influence Natural killer (NK) cell function in vitro.
β-Amyloid (10-35), amide is composed of 26 aa (10-35 residues of the Aβ peptide) and is the primary component of the amyloid plaques of Alzheimer’s disease.
QM385 is a potent sepiapterin reductase (SPR) inhibitor with an IC50 of 1.49 nM, which blocks T-cell proliferation and autoimmunity at nanomolar potency and with good oral bioavailability[1].
A-395 is a novel antagonist of Polycomb repressive complex 2 (PRC2) protein–protein interactions that potently inhibits the trimeric PRC2 complex (EZH2–EED–SUZ12) with an IC50 of 18 nM.
Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
ATX inhibitor 14 (compound 4), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 0.41 nM. ATX inhibitor 14 has the potential for fibrosis relevant diseases research[1].
N-tert-Butyloxycarbonyl-L-histidine is a histidine derivative[1].
TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
D-Erythrose-2-13C is the 13C labeled D-Erythrose[1].
MRGPRX4 modulator-2 (compound 1-55) is a potent MRGPR X4 modulator, possessing antagonist activity against MRGPR X4 with an IC50 < 100 nM. MRGPRX4 modulator-2 can be used for researching autoimmune diseases such as psoriasis, multiple sclerosis, Steven Johnson’s Syndrome, and other chronic itch conditions[1].
R406 is a competitive Syk inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value.
Fmoc-Gly(allyl)-OH is a Glycine (HY-Y0966) derivative[1].
Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole can be used for the research of certain bacterial and protozoal diseases in poultry, swine dysentery and genital trichomoniasis in cattle[1].
GHGVYGHGVYGHGPYGHGPYGHGLYW (DgHBP-2) is 26-amino-acid-long consensus peptide derived from histidine-rich beak protein-2 (DgHBP-2). GHGVYGHGVYGHGPYGHGPYGHGLYW can be used fabricated glucose-responsive insulin delivery system[1].
Fmoc-D-Thr(Trt)-OH is a threonine derivative[1].
Pseudocoptisine (Isocoptisine) chloride is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine chloride inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects[1][2].
2-Carboxybenzaldehyde is a chemical compound. 2-Carboxybenzaldehyde consists of a benzene ring, with an aldehyde and a carboxylic acid as substituents that are ortho to each other. 2-Carboxybenzaldehyde can be used to form ligands with metal ions. Ni(II) and Cu(II) complexes of 2-Carboxybenzaldehyde thiosemicarbazone has anticancer and antibacterial activities[1].
Epimedin A1 is a flavonoid extracted from Herba Epimedii which is one of commonly used Chinese medicines.
D-{Ala-Ala-Ala-Ala-Ala} is a pentapeptide and can be used as an inhibitor of the immunological reactions[1].
MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo.
Ikshusterol 3-O-glucoside is a phytochemical that inhibits PLA2 from snake venoms[1].
Phosphatidylserine is a conserved anti-inflammatory and immunosuppressive signal that is highly dysregulated in the tumor microenvironment and autoimmune diseases. During apoptosis and cellular stress，the related disrupting enzymes Xkr8 and TMEM16 mediate Phosphatidylserine externalization. Phosphatidylserine externalization produces a "eat me" signal that initiates endocytosis and helps clear the body of apoptotic cells. When pathogens use Phosphatidylserine and apoptotic mimicry to evade host immune responses，targeting Phosphatidylserine strategies can stimulate immune activity[1].
CWI1-2 is an IGF2BP2 inhibitor that binds IGF2BP2 and inhibits its interaction with m6A-modified target transcripts, induces apoptosis and differentiation, and shows promising anti-leukemic effects[1].
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
Cyclocurcumin is a potent p38α inhibitor. Cyclocurcumin shows antirheumatic, antivasoconstrictive and antioxidant activities[1][2][3].
HDAC8/BRPF1-IN-1 (Compound 23a) is a dual inhibitor of HDAC8 and BRPF1 with an IC50 of 443 nM against human HDAC8 and a Kd of 67 nM against human BRPF1. HDAC8/BRPF1-IN-1 shows low in vitro activity against HDAC1 and 6[1].
Lobenzarit, an immunomodulator, possesses anti-oxidative[1].