- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S1453||Tipifarnib||<1 mg/mL||14 mg/mL||<1 mg/mL|
|S2797||Lonafarnib||<1 mg/mL||127 mg/mL||127 mg/mL|
|S2799||Daporinad (FK866, APO866)||<1 mg/mL||<1 mg/mL||78 mg/mL|
|S2674||A922500||<1 mg/mL||86 mg/mL||<1 mg/mL|
|S8056||Lomeguatrib||<1 mg/mL||65 mg/mL||<1 mg/mL|
|S5336||Hecogenin||<1 mg/mL||<1 mg/mL||<1 mg/mL|
|S5449||3-Methoxybenzamide||-1 mg/mL||30 mg/mL||-1 mg/mL|
|S4989||AOA hemihydrochloride||-1 mg/mL||21 mg/mL||-1 mg/mL|
|S3945||L-Cycloserine||20 mg/mL||8 mg/mL||-1 mg/mL|
|S8608||Adenosine Dialdehyde (ADOX)||3 mg/mL||19 mg/mL||<1 mg/mL|
|S3658||O6-Benzylguanine||<1 mg/mL||48 mg/mL||12 mg/mL|
|S7466||GGTI 298 TFA salt||<1 mg/mL||100 mg/mL||100 mg/mL|
|S8244||Etomoxir (Na salt)||64 mg/mL||64 mg/mL||13 mg/mL|
|S4021||Tolcapone||<1 mg/mL||55 mg/mL||55 mg/mL|
|S4589||Amodiaquine dihydrochloride dihydrate||29 mg/mL||92 mg/mL||<1 mg/mL|
|S4743||Wogonin||<1 mg/mL||56 mg/mL||3 mg/mL|
|S7467||LB42708||<1 mg/mL||100 mg/mL||86 mg/mL|
|S4280||Meclofenoxate (Centrophenoxine) HCl||58 mg/mL||58 mg/mL||58 mg/mL|
|S7192||PF-04620110||<1 mg/mL||49 mg/mL||<1 mg/mL|
|S7465||FTI 277 HCl||17 mg/mL||96 mg/mL||14 mg/mL|
- Transferase Inhibitors (20)
- New Transferase Products
|Catalog No.||Information||Product Use Citations||Product Validations|
Tipifarnib (R115777) is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Phase 3.
Effect of the inhibition of mutated RAS on thyroid cancer cell response to gefitinib . C-643 (RAS mutated thyroid cancer cells) and BC-PAP (wild type RAS thyroid cancer cells) were seeded in 96-well plates and incubated with increasing doses of gefitinib (Gef.; 0.5, 1.0 , and 5.0 uM), the RAS inhibitor tipifarnib (0.1, 1.0 and 10 uM) or both for 48 hours. Cell viability was then measured by the MTT assay.
Lonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.
Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.
Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2.
Bar graph showing the effect of the PBEF inhibitor FK866 on PLB-induced autophagy in PC-3 cells. Data are presented as the mean ± SD of three independent experiments. *P<0.05; **P<0.01; and ***P<0.001 by one-way ANOVA.
A922500 is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.
Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM.
Characterization of melanoma cell lines upon MGMT status. A, representative examples of dose-response curves for MGMT+ and MGMT− cells treated with temozolomide (TMZ) with or without lomeguatrib (LOM). Graphs show the average GI50 for temozolomide in the presence or absence of lomeguatrib (B).
Hecogenin, a steroid saponin isolated from Agave sisalana, is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM.
3-Methoxybenzamide is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT)
Aminooxyacetic acid is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism.
L-Cycloserine is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity.
Adenosine Dialdehyde (ADOX) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM.
O6-Benzylguanine (O6-BG) is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.
GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis.
Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane.
CPT1A inhibitor counteracted the protective effect of BBR against PA-induced lipid accumulation and apoptosis in HK-2 cells. HK-2 cells were pretreated with or without 40 μmol/L Etomoxir for 24 h, and then treated with 12.5 μmol/L BBR in the presence or absence of 450 μmol/L PA for 24 h. Intracellular lipid content was detected by Oil Red O staining (400×) (A) .
Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.
Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase with estimated Ki of 18.6 nM. It is also used as an antimalarial and anti-inflammatory agent.
Wogonin, a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; Also inhibits N-acetyltransferase.
Effect of Wogonin on the translocation and transcriptional activity of NFATc1. U2OS cells stably transfected with EGFP-NFATc1, RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. The IN Cell™ Analyzer 1000 was used to observe the translocation of NFATc1. (A) DMSO was used as a control. RANKL (100 ng/ml) significantly stimulated the translocation of NFATc1; Wogonin (5 mM) significantly decreased the translocation of NFATc1 induced by RANKL (magnification, x200). (B) Statistics showed that Wogonin could decrease the translocation of NFATc1 into the nucleus induced by RANKL in a concentration-dependent manner. RAW264.7 cells were transfected with pGL3-promoter-NFATc1-RE, and then RANKL (100 ng/ml) and different concentrations of Wogonin (5.0, 1.0, 0.1 and 0.0 mM) were added and incubated for 24 h. (C) RANKL significantly increased the transcriptional activity of NFATc1 and Wogonin decreased the transcriptional activity of NFATc1 induced by RANKL in a concentration-dependent manner. n=3; *P<0.05 and ***P<0.001 compared with the RANKL group. NAFTc1, nuclear factor of activated T cells c1; EGFP, enhanced green fluorescent protein; DMSO, dimethylsulfoxide, RANKL, receptor activator of nuclear factor κB ligand; RE, response element.
LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively.
Meclofenoxate (Centrophenoxine) HCl is an anti-aging drug used to treat the symptoms of senile dementia and Alzheimer's disease, and also inhibits the activity of cholinephosphotransferase.
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I.