SGC-STK17B-1 is a potent, selective, ATP-competitive inhibitor of death-associated protein kinase family member STK17B (DRAK2) with IC50 of 34 nM, >100-fold selectivity over STK17A;SGC-STK17B-1 is also >100-fold selective over all of the other kinases tested, with only STK17A, CAMKK1, and AURKB (IC50s=5-9 uM) in panel of 403 wild type human kinase assays.SGC-STK17B-1 demonstrated the highest cell potency in the NanoBRET target engagement assay (IC50=190 nM).SGC-STK17B-1 is the first truly potent and selective chemical probe of STK17B.
Mal-VC-PAB-PNP is a cleavable ADC Linker (ADC Linker). Mal-VC-PAB-PNP can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
Astin C (Asterin) is a cyclic pentapeptide with anticancer and anti-inflammatory properties[1].
Cabozantinib is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
3-Cyanovinylcarbazole phosphoramidite is an antiviral drug that inhibits the synthesis of viral DNA. The modified nucleoside in the compound is synthesized by modifying the ribonucleotide with cyano group at the C-3 position, and can be used as a phosphoric acid amide for DNA synthesis[1].
STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer[1].
28-Demethyl-β-amyrone (28-Norolean-12-en-3-one) is one of the main triterpenes from Pistacia lentiscus var. Chia[1]. 28-Demethyl-β-amyrone is an antitoxin and can effectively for the toxic effects of Staphylococcal enterotoxins (SEs)[2].
eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC50 of less than 0.5 nM.
tert-Butyl L-valinate hydrochloride is a valine derivative[1].
VSPPLTLGQLLS is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation[1][2].
MONIRO-1 is a T-type and N-type calcium channel blocker with IC50 values of 34, 3.3, 1.7 and 7.2 µM against hCav2.2, hCav3.1, hCav3.2 and hCav3.3, respectively[1].
CLinDMA, a cationic lipid, can cause inflammatory response. CLinDMA can be used for the synthesis LNP201. LNP201 is a liposome assembly for systemic delivery of siRNA[1].
Simvastatin sodium is a lactone prodrug, can be hydrolysed to active hydroxy-acid by non-specific carboxyesterases or non-enzymatic processes. Simvastatin sodium shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM[1][2].
DG5128 is a preferential α2-adrenoceptor antagonist. DG5128 exhibits 7.4 times higher affinity (pKi=6.28) toward α2-adrenoceptor than α1-adrenoceptor.
CTA056 is an ITK (IL-2-inducible T-cell kinase) inhibitor with an IC50 of 0.1 μM. CTA056 selectively targets malignant T cells and modulates oncomirs. CTA056 induces apoptosis and is a potential therapeutic agent for the treatment of T-cell leukemia and lymphoma[1].
L-Epinephrine bitartrate is an α-adrenergic and β-adrenergic receptor agonist. L-Epinephrine is a hormone secreted by the medulla of the adrenal glands.
RD20000 is a corticosteroid which is obtained by esterifying with propionic acid the 17-position of the prednisolone skeleton and deoxidating its 21-position.
Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system[1].
TG 100801 Hydrochloride is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
guanosine analogue. 3-Methyl-8-(2'-deoxy-β-D-ribofuranosyl)isoxanthopterin is widely used in studies of DNA binding and dynamics, with an absorbance maximum at 350 nm and an emission maximum at 430 nm[1].
Chamaejasmenin A is a C-3/C-3’’ linkage biflavanone that can be isolated from Stellera chamaejasme L.[1].
IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM[1].
PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe2+ ion and induces the formation of an “Arg367-out” pocket[1].
Nordefrin ((±)-Cobefri), a Norepinephrine derivative, is a vasoconstrictor agent[1].
DT-6 is an effective TGF-β1 inhibitor. DT-6 inhibits M2 macrophage induced epithelial to mesenchymal transition and invasive migration of cancer cells. DT-6 can be used for cancer diseases research[1].
Alacizumab pegol (CDP-791) is a pegylated antibody fragment directed against KDR. Alacizumab pegol can be used for the research of cancer[1].
β-Maaliene can be isolated from the fresh leaves of Vitex densiflora (Maaliene) and is the main component in the isolate. β-Maaliene can significantly reduce the exercise capacity of mice at certain doses[1].
Antioxidant agent-18 (compound 5) is a flavonol glycoside with antioxidant activity isolated from Ginkgo biloba. Antioxidant agent-18 scavenges DPPH radicals (IC50: 15.8 μM) and reduces cytochrome c (IC50: 14.7 μM).
Ac-Phe-Gly-pNA is the chymotrypsin specific substrate[1].