T6098

Cabotegravir (S/GSK1265744) (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50: 3.0 nM).

PIKfyve-IN-1 is a cell-active and highly potent chemical probe that can be used for the PIKfyve research in virology. PIKfyve-IN-1 inhibits phosphatidylinositol-3phosphate 5-kinase (PIKfyve) (IC 50 = 6.9 nM)[1].

TRPC4/5-IN-1 can be used for the research of skin inflammatory diseases and proteinuric kidney diseases. TRPC4/5-IN-1 is a potent inhibitor of TRP channel 5/4 (TRPC5/4) with IC50 values of 0.54 μM and 2.06 μM, respectively. [1].

BChE-IN-14 (compound 19c) is a selective inhibitor of butyrylcholinesterase (BChE) with IC50 values of 0.011 μM for hBChE and 0.23 μM for eqBChE, exhibiting primary cell safety and good blood-brain barrier permeability. It can restore cognitive impairment in vivo and is useful in Alzheimer's disease research [1].

TH588 hydrochloride, a first-in-class inhibitor of the nudix hydrolase family, selectively and effectively binds to and inhibits MTH1 with an IC50 value of 5 nM.

KCa2 channel modulator 1 (compound 2o) is an effective, subtype-selective K/Ca2 channel positive modulator that potentiates rat KCa2.2 channels with an EC50 value of 0.99 μM and human KCa2.3 channels with an EC50 value of 0.19 μM [1].

KCa2 channel modulator 2 (compound 2q) is an effective, subtype-selective K/Ca 2 channel positive modulator with similar potency on the human K Ca 2.3 channel and rat K Ca 2.2a subtypes, exhibiting EC50 values of 0.60 μM and 0.64 μM, respectively [1].

Androgen receptor antagonist 3 (Compound C18) exhibits anticancer activity as an antagonist of the androgen receptor (AR) with an IC50 value of 2.4 μM [1].

Androgen receptor antagonist 4 (Compound AT2) exhibits anticancer activities by potently antagonizing AR transcriptional activity, inhibiting downstream AR target genes, and blocking DHT-induced nuclear translocation of AR. It is an antagonist of the androgen receptor (AR) with an IC50 of 0.15 μM [1].

Sumatriptan (GR 43175) hydrochloride can be used in the research of migraine headache that is an orally active agonist of 5-HT1 receptor. The Ki values of Sumatriptan hydrochloride against 5-HT1D, 5-HT1B and 5-HT1A receptors are 17 nM, 27 nM and 100 nM, respectively. [1] [2].