TCMDC-136879|CAS 1505452-64-1|DC Chemicals

Cas No.:	1505452-64-1
Chemical Name:	TCMDC-136879
Formula:	C₂₅H₂₅N₃O
M.Wt:	383.5

Cat. No.	Product name	Field of application
DC72999	CK-2-63	CK-2-63 is a potent first-in-class M. tuberculosis cytochrome bd (cyt bd) inhibitor, demonstrates growth suppression of M. tuberculosis H37Rv with IC50 of 3.7 uM.
DC72295	SpdSyn binder-1	SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparum spermidine synthase. SpdSyn binder-1 can be used for the research of malaria.
DC70609	MMV030084	MMV030084 (MMV-030084) is a potent, specific P. falciparum cGMP-dependent protein kinase (PKG) inhibitor (Kdapp=9-16 nM), inhibits invasion of P. berghei ANKA parasites into HepG2 liver cells with IC50 of 199 nM.MMV030084 potently inhibits hepatocyte invasion by Plasmodium sporozoites, merozoite egress from asexual blood stage schizonts, and male gamete exflagellation, shows potent activity against liver, asexual, and sexual blood stage development.MMV030084 showed an IC50 of 109 nM against the drug-sensitive 3D7-A10 line, and an IC50 of 120 nM against multidrug-resistant Dd2-B2 parasites in a 72-h growth inhibition assay against Pf ABS parasites.MMV030084 inhibited male gamete exflagellation at an IC50 of 141 nM when gametocytes were stimulated to develop into male gametes.MMV030084 is a promising Plasmodium PKG-targeting chemotype.
DC70101	INE963	INE963 (INE-963) is a potent and fast-acting blood-stage antimalarial, demonstrates potent cellular activity against Pf 3D7 with EC50 of 6 nM in Pf growth inhibition assay.
DC70091	GSK3186899	GSK 3186899 (GSK-3186899, DDD853651) is a novel specific inhibitor of parasite cdc-2-related kinase 12 (CRK12), shows activity against L. donovani in intra-macrophage assay with EC50 value of 1.4 uM, and shows good selectivity against mammalian THP-1 host cells (EC50> 50 uM).
DC70064	Parabulin	Parabulin is a novel potent, parasite-specific tubulin inhibitor, inhibits growth of parasites while displaying no effects on human cells.
DC48830	GSK3494245	GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties.
DC47399	MMV674850	MMV674850 is potent against asexual stage parasites at 2.7 and 4.5 nM and preferentially targets early-stage gametocytes (early-stage gametocyte: IC50 4.5 ± 3.6 nM; late-stage gametocyte: IC50 28.7 ± 0.2 nM).
DC47398	MMV666810	MMV666810, a 2-aminopyrazine similar to MMV390048, is potent against asexual parasites at 5.94 nM, but against gametocytes, it has a 3.3-fold selectivity to late-stage gametocytes compared to earlier stages (early-stage gametocyte: IC50 603 ± 88 nM; late-stage gametocyte: IC50 179 ± 8 nM).
DC46818	ACT-451840	ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.