Ionizable Lipid Products

TAS-116 is a potent and selective HSP90α/β inhibitor with Kis of 34.7 nM, 21.3 nM, respectively.

PD-1-IN-17 is a programmed cell death- 1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM[1].

LXH254 is a potent CRAF inhibitor extracted from patent WO2018051306A1, Compound A. LXH254 also is a potent BRAF inhibitor.

BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.

LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2 with an IC50 of 15 nM.

CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.

GDC-0334 (GDC0334) is a highly potent, selective, orally bioavailable TRPA1 antagonist with IC50 of 1.7 nM in cell-based assays.GDC-0334 demonstrated potent TRPA1 inhibition in several species, including human (IC50=1.7 nM), cynomolgus (IC50=3.6 nM), mouse (IC50=2.7 nM), guinea pig (IC50=11.1 nM), and dog (IC50=102 nM).GDC-0334 displays good selectivity against human TRPV1, TRPM8, and TRPC6 (all IC50s>10 uM).GDC-0334 also inhibits calcium flux in human primary cells, HASMCs and HLFs, treated with the TRPA1 agonist AITC.GDC-0334 suppresses AITC-induced edema in vivo in rat (1-10 mg/kg), reduces OVA-induced asthma model in rats and guinea pigs and guinea pig model of cough.GDC-0334 is a potent inhibitor of AITC-induced dermal blood flow (DBF) in vivo in rats and guinea pigs, reduces AITC-induced perfusion and nocifensive behavior in rats and itch and pain scores in humans.

ML141(CID-2950007) is a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase(IC50=200 nM) with low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7).

SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.

BMS-626529 is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.

Cyclobenzaprine Hcl is a skeletal muscle relaxant and a central nervous system (CNS) depressant.Cyclobenzaprine is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine was thought to be an alpha 2-adrenoceptor agonist that reduced muscle tone by decreasing the activity of descending noradrenergic neurons. Cyclobenzaprine reduced the monosynaptic reflex amplitude dose dependently and this effect was not inhibited by the alpha 2-adrenoceptor antagonists idazoxan and yohimbine. Cyclobenzaprine-induced monosynaptic reflex depression was not attenuated by noradrenergic neuronal lesions produced by 6-hydroxydopamine. Cyclobenzaprine is a 5-HT2 receptor antagonist and that its muscle relaxant effect is due to inhibition of serotonergic, not noradrenergic, descending systems in the spinal cord [1]. The inhibitory effects of cyclobenzaprine on mono- and polysynaptic reflex potentials are due to the inhibition of descending serotonergic systems through 5-HT(2) receptors in the spinal cord [2].

Juglone is a yellow pigment found in black walnut (Juglans regia). Juglone also shows antimicrobial activity[1].

Acalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.

FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 and ERK2, respectively.

CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Item No. 11690) in preclinical models of pancreatic cancer.

Dalbavancin is a lipoglycopeptide antibiotic agent that is active against gram-positive pathogens.

Nedisertib (M3814, MSC2490484A) is a highly potent, selective, orally bioavailable inhibitor of DNA-PK.

H3B-6527 (H3 Biomedicine) is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice.

Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.

Bumetanide(Ro 10-6338; PF 1593) is an inhibitor of Na(+)-K(+)-2Cl(-) co-transporter (NKCC) with an IC50 of 0.6 uM.