penetrant — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T15275	Fenobam		GluR
	Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric mo...		GluR
T9346	CVN424		GPR
	CVN424 is a selective and novel GPR6 Inverse agonist effective in models of Parkinson Disease.		GPR
T9466	RTICBM-189		Others
	RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectivel...		Others
T9697	ASK1-IN-1		ASK
	ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.		ASK
T9452	PW0787		GPR
	PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM).		GPR
T4081	MPTP hydrochloride	MPTP-hydrochloride	Apoptosis , Dopamine Receptor
	MPTP hydrochloride is a precursor of MPP+, a dopamine neurotoxin with blood-brain barrier permeability. MPTP hydrochloride is toxic to dopaminergic neurons, which can lead to Parkinson's disease, and is widely used in th...		Apoptosis , Dopamine Receptor
T12998	SR10067		Others , Autophagy
	SR10067 is a potent, selective and brain penetrant agonist of Rev-Erbα/β(IC50 of 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively),has anxiolytic activity.		Others , Autophagy
T7388	GSK805		ROR
	GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA bindi...		ROR
T21747	VU0483605		GluR
	VU0483605 is an effective and selective positive allosteric modulator of mGluR1 with EC50s of 390 and 356 nM for human and rat, respectively.		GluR
T8554	KCC-07		DNA Alkylator/Crosslinker
	KCC-07 is a selective, potent and brain-penetrant inhibitor of methyl-CpG-binding domain protein 2(MBD2) with anticancer activity. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenes...		DNA Alkylator/Crosslinker
T16849	SB-222200		Neurokinin receptor
	SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).		Neurokinin receptor
T9786	Lu AF27139		P2X Receptor
	Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases st...		P2X Receptor
T3707	GNE-3511	GNE3511	DNA Alkylation , MAPK
	GNE-3511 is a potent and selective dual leucine zipper kinase inhibitors.		DNA Alkylation , MAPK
T6031	GNE0877	GNE 0877,GNE-0877	LRRK2
	GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM).		LRRK2
T7100	PLX5622	PLX-5622	c-Fms , CSF-1R
	PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor.		c-Fms , CSF-1R
T27620	IP7e	IP 7e,IP-7e,isoxazolo-pyridinone 7e	Others
	IP7e (isoxazolo-pyridinone 7e) is a Nurr1 activator with an EC50 value of 3.9 nM.		Others
T0492	Dimethyl fumarate	DMF	Reactive Oxygen Species , HIV Protease , Nrf2 , Endogenous Metabolite , Autophagy
	Dimethyl fumarate (DMF), a fumarate derivative, is used as antiinflammatory and immunomodulatory agent.
T21793	CGP 35348		GABA Receptor
	CGP 35348 is a selective antagonist of GABAB receptor (EC50 = 34 μM). CGP 35348 can be used in studies of neuromuscular coordination and spatial learning after neonatal brain damage in albino mice.		GABA Receptor
T21652	RN-1 dihydrochloride		Histone Demethylase , MAO
	RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).		Histone Demethylase , MAO
T6504	Flupirtine maleate	Katadolon maleate	Potassium Channel , NMDAR , iGluR
	Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.		Potassium Channel , NMDAR , iGluR