drug resistance — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T3971	CASIN	Pirl1-related Compound 2	CDK , STAT , Ras
	CASIN (Pirl1-related Compound 2) is a specific inhibitor of GTPase Cdc42 (IC50: 2 uM).		CDK , STAT , Ras
T27617	Inz-1		P450
	Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC50s of 8.092 and 45.320 μM for yeast and human. Inz-1 reverses Fluconazole or other triazole antifungals’ resistance in the path...		P450
T2620	G-749	G749	Apoptosis , FLT , c-RET , TAM Receptor , Aurora Kinase
	G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.		Apoptosis , FLT , c-RET , TAM Receptor , Aurora Kinase
T16339	Norverapamil hydrochloride	(±)-Norverapamil hydrochloride,D591 hydrochloride	Calcium Channel , P-gp , Drug Metabolite
	Norverapamil hydrochloride (D591 hydrochloride) ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.		Calcium Channel , P-gp , Drug Metabolite
T15168	DRF-1042		Others
	DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 displays perfect anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.		Others
T6018	Zosuquidar trihydrochloride	Zosuquidar (LY335979) 3HCl,RS 33295-198 trihydrochloride,RS 33295-198 (D06387) 3HCl,Zosuquidar 3HCl,LY-335979 trihydrochloride	P-gp
	Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.		P-gp
T6287	Tariquidar	XR9576	P-gp
	Tariquidar (XR9576)(Kd=5.1 nM) is a specific and effective non-competitive inhibitor of P-glycoprotein. It can reverse drug resistance in MDR cell Lines.		P-gp
T3S2381	Perillene	3-Isohexenylfuran,Perillen	Others , Antibacterial
	Perillene (3-Isohexenylfuran) is an actiive constituent in the drug which promotes enterocinesia. Perillen demonstrates strong resistance activity against staphylococcus aureus and E.coli.		Others , Antibacterial
T7861	Flumatinib mesylate	HHGV678 mesylate	Bcr-Abl , PDGFR , c-Kit
	Flumatinib mesylate (HHGV678 mesylate) is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.		Bcr-Abl , PDGFR , c-Kit
T0002	Ethamsylate	Cyclonamine,Etamsylate,Dicynene,Aglumin	Prostaglandin Receptor
	Ethamsylate (Dicynene) usually is used as a hemostatic drug, which increases capillary endothelial resistance and platelet adhesion, and inhibits biosynthesis and action of prostaglandins.		Prostaglandin Receptor
T25770	116-9e	MAL-2-11B,MAL2-11B,MAL211B,MAL 2 11B,MAL2 11B	Virus Protease
	116-9e (MAL2-11B) is a potent Hsp70 co-chaperone DNAJA1 inhibitor with antiviral properties, inhibition of simian virus 40 (SV40) replication, inhibition of tumour antigen (TAg) endogenous ATPase activity, and TAg-mediat...		Virus Protease
T3335	Darunavir Ethanolate	UIC 94017,Darunavir Ethanolate,TMC114	HIV Protease
	Darunavir Ethanolate (UIC 94017) is an HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination...		HIV Protease
T1649	Tenofovir	PMPA,TDF,GS 1278	HBV , HIV Protease , Reverse Transcriptase
	Tenofovir (GS 1278) is an adenine analog REVERSE TRANSC-RIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B. It is used to treat HIV INFECTIONS and CHRONIC HEPATITIS B, in combination with other ANTIV...		HBV , HIV Protease , Reverse Transcriptase
T36375	Ralaniten triacetate
	Ralaniten triacetate (EPI-506) is a novel pro-drug of Ralaniten, functioning as an orally active inhibitor of the androgen receptor (AR) N-terminal domain (NTD). Its remarkable first-in-class status signifies its unique ...
T8488	GMB-475		Bcr-Abl
	GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL).resulting in ubiquitinati...		Bcr-Abl
T2324	Darunavir	TMC114	HIV Protease
	Darunavir (TMC114) is an HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other AN...		HIV Protease
T2328	Radotinib	IY-5511,Supect	Bcr-Abl
	Radotinib (IY-5511), and sometimes referred to by its investigational name IY5511, is a drug for the treatment of different types of Y, most notably Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) w...		Bcr-Abl
T1496	Amiodarone hydrochloride	Amiodar,Amiodarone HCl,Nexterone	Potassium Channel , Adrenergic Receptor , Autophagy
	Amiodarone hydrochloride (Amiodarone HCl) is an antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM C...		Potassium Channel , Adrenergic Receptor , Autophagy
T3895	Polyphyllin I		Apoptosis , Akt , JNK , PDK , mTOR , Autophagy
	Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D ha...		Apoptosis , Akt , JNK , PDK , mTOR , Autophagy
T4S1419	(±)-Praeruptorin A	Praeruptorin A,(-)-Praeruptorin A	p38 MAPK , Calcium Channel , Akt
	1. (±)-Praeruptorin A could exhibit its anti-osteoclastogenic activity by inhibiting p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca(2+) oscillation 2. Praeruptorin A has the potential to inhibit migration/fusion ...		p38 MAPK , Calcium Channel , Akt