TBK1-IKKε inhibitor II is a potent, selective dual inhibitor of TBK1/IKKε with IC50 of 13 nM/59 nM, respectively; displays 100- to 1000-fold less activity against other tested protein kinases including PDK1, PI3K family members and mTOR; inhibits LPS-induced expression of IFNβ (IC50=62 nM), and the IFNβ target genes IP10 (IC50=78 nM) and Mx1 (IC50=20 nM); effectively blocks TLR3-dependent IRF3 nuclear translocation in cells with IC50<100 nM.
Cortistatin-14, a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties[1][2][3][4].
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer[1].
D-myo-Inositol 1,4,5-trisphosphate hexapotassium salt is the hexapotassium salt of D-myo-Inositol 1,4,5-trisphosphate (1,4,5-IP3), which is a second messenger that stimulates the discharge of calcium from the endoplasmic reticulum.
PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, 100-fold selectivity versus Chk2 (Ki, 47 nM).
Amino-PEG2-C2-acid is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Perflubron(1-Bromoheptadecafluorooctane;Heptadecafluorooctyl bromide; Perfluorooctyl bromide) is a contrast medium for magnetic resonance imaging and sonography. Perflubron (1-Bromoheptadecafluorooctane;Heptadecafluorooctyl bromide; Perfluorooctyl bromide) can be emulsified with egg phospholipids (EYP) and shows exceptionally fast excretion characteristics[1][2].
3-Maleimidopropionic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
NBD-X acid is a fluorescent probe for the study of fatty acids and sterols. NBD-X acid provides better yields for labelling biopolymers compared to NBD chloride and fluoride. The fluorescence spectrum of the NBD derivative is highly sensitive to the environment and the fluorescence intensity is significantly reduced in aqueous solutions[1].
ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II[1][2].
KRAS G12C inhibitor 30 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 2. KRAS G12C inhibitor 30 can be used for the research of cancer[1].
SHP836 is a distinct, allosteric site 2 SHP2 inhibitor with IC50 of 12 uM (SHP2 1-525), and selective over the phosphatase domain (SHP2 PTP IC50>100 uM).downregulates DUSP6 mRNA, a downstream MAPK pathway marker, in KYSE-520 cancer cells; enhances pharmacological pathway inhibition in cells combined with SHP099.
5’-O-(p-Toluoyl)-2’-O-acetyl-3’-deoxy-3’-fluoro-6-chloroinosine 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].
Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol[1]. Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin[2][3].
4-Phenyl-7,8-dihydroxycoumarin is a coumarin derivative and can be used for bronchiectasiss research[1].
Boc-Asp-OMe is an aspartic acid derivative[1].
Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP) (extracted from patent WO2021076124A1)[1].
3,5,7-Trimethoxyflavone, a flavonoid compound, can inhibit the TNF-α-induced high expression and secretion of MMP-1 by cells. 3,5,7-Trimethoxyflavone can be used to ameliorate skin damage[1].
Vindesine sulfate is a potent tubulin inhibitor with an Ki of 0.110 µM. Vindesine sulfate shows anti-proliferation effect in vitro. Vindesine sulfate shows antitumor effect in vivo[1].
(2S)-2-[[(tert-Butoxy)carbonyl](methyl)amino]-3-methylbutanoic acid is a valine derivative[1].
Monomethyl auristatin E intermediate-12 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs)[1].
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases[1].
Norcholic acid is a normal minorbile C23 bile acid having four side chain and exsits in human urine and meconium. Norcholic acid can become prominent under certain pathological conditions. Norcholic acid is efficiently absorbed from intestine and quickly excreted into the bile but not into urine[1].
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
GYKI-47261 dihydrochloride is a competitive, orally active, and selective AMPA receptor antagonist with an IC50 of 2.5 μM. GYKI-47261 has broad spectrum anticonvulsive activity and neuroprotective effects. GYKI-47261 dihydrochloride is also a potent inducer of CYP2E1[1][2].
Cinnarizine is an antihistamine and a calcium channel blocker, promote cerebral blood flow, used to treat cerebral apoplexy, post-trauma cerebral symptoms, and cerebral arteriosclerosis.
Calcineurin autoinhibitory peptide is a selective inhibitor of Ca2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. Calcineurin autoinhibitory peptide could protect neurons from excitatory neuronal death[1][2].
Methyl (R)-2-((tert-butoxycarbonyl)amino)-3-iodopropanoate is an alanine derivative[1].
Licoricone is an flavonoid extracted from licorice, exhibits anti-helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains[1].
Isovitexin is a flavonoid isolated from rice hulls of Oryza sativa, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.