gp-4

PGP-4008 is a selective and potent P-glycoprotein (Pgp) inhibitor that inhibits tumor growth by co-administration with Doxorubicin.

CGP-42112 acetate is a potent angiotensin receptor AT2 agonist that inhibits the increase in protein kinase A activity produced by LPS.

P-gp inhibitor 4 is a selective P-glycoprotein modulator with an EC 50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells .

CGP-42112 is an agonist of the Angiotensin-II subtype 2 receptor (AT2 R).

CGP-42454A is a bio-active chemical.

CGP-47292 is a metabolite of the novel antiepileptic compound CGP 33,101.

CGP-49823 is a non-peptide tachykinin NK1 receptor antagonist.

CGP-42456A - Benazepril Related Compound A, it is an Impurity. Benazepril is a prodrug which is metabolized by the liver into its active form benazeprilat via cleavage of the drug's ester group. Benazepril and Benazeprilat inhibit angiotensin-converting enzyme (ACE) in human subjects and animals. Benazeprilat has much greater ACE inhibitory activity than does Benazepril. It is indicated for the treatment of hypertension.

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

Diclofenac sodium (GP 45840) is a non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.

Tamarixetin (4'-O-Methyl Quercetin) is a natural flavonoid derivative of quercetin that exhibits anti-inflammatory and antioxidative effects, offering protection against cardiac hypertrophy.

PF-06273340 is an effective, Selective, and Peripherally Restricted Pan-Trk inhibitor (IC50: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflux transporters P-gp (ER = 35.7) and BCRP (ER = 4.0) and has moderate passive permeability (RRCK Papp = 5.4 × 10 6 cm s 1).

Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and a potent chemosensitizer that enhances the number of DNA double-strand breaks induced by Doxorubicin. It serves as an effective multidrug resistance (MDR) inhibitor, demonstrating inhibitory activity against P-glycoprotein (P-gp) mediated drug efflux. Multi-target kinase inhibitor 4 can be encapsulated in PEG-coated lipid nanoparticles.

3',4',5',5,7-Pentamethoxyflavone is a naturally occurring brassinosteroid compound from the Rutaceae family that exhibits cancer cell resistance by inhibiting the Nrf2 pathway to overcome chemotherapeutically active molecules.

BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the efflux pump P-glycoprotein (P-gp) but co-application of BAAA with a P-gp inhibitor, such as verapamil , inhibits BAA efflux.2BAAA-DA has been used to isolate human hematopoietic progenitor cells, which have high ALDH activity, andviaflow cytometry to sort cancer stem cells that contain high levels of ALDH.1,3BAA used in cells can be excited at 488 nm and displays an emission maximum of 512 nm.4 1.Storms, R.W., Trujillo, A.P., Springer, J.B., et al.Isolation of primitive human hematopoietic progenitors on the basis of aldehyde dehydrogenase activityProceedings of the National Academy of Sciences of the United States of America96(16)9118-9123(1999) 2.Smith, C.A., Colvin, M., Storms, R.W., et al.BODIPY aminoacetaldehyde diethyl acetal08010501.81-15(2010) 3.Leng, Z., Yang, Z., Li, L., et al.A reliable method for the sorting and identification of ALDHhigh cancer stem cells by flow cytometryExp. Ther. Med.(2017) 4.Pomper, M.G., Wang, H., Minn, I., et al.Red fluorescent aldehyde dehydrogenase (ALDH) substrate(2015)

Cilengitide is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.

EBOV-IN-4 (compound 12), a benzothiazepine, acts as a potent inhibitor against the Ebola virus (EBOV), displaying 64.9% inhibitory activity against EBOV-GP-pseudotype virus (pEBOV) at a concentration of 10 μM. It is, however, inactive against ASFV [1].

GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.

(+ -)-Verapamil hydrochloride-d7 is a deuterated compound of (+ -)-Verapamil hydrochloride. (+ -)-Verapamil hydrochloride has a CAS number of 152-11-4. Verapamil hydrochloride is a calcium channel blocker that is a class IV anti-arrhythmia agent.

Cefditoren-d3 is a deuterated compound of Cefditoren. Cefditoren has a CAS number of 104146-53-4. Cefditoren sodium is a cephalosporin antibiotic potentially for the treatment of bacterial infection. The expression levels of Mrp2, Bcrp, Oat2 mRNA were markedly increased, while P-gp and Oct1 mRNA were decreased. In concordance with RT-PCR results, Mrp2 expression level increased by Western blotting.

Verapamil-d7 Hydrochloride is a deuterated compound of Verapamil Hydrochloride. Verapamil Hydrochloride has a CAS number of 152-11-4. Verapamil hydrochloride is a calcium channel blocker that is a class IV anti-arrhythmia agent.

Dihydroevocarpine (1-methyl-2-tridecylquinolin-4-one) induces AML cytotoxicity, apoptosis and G0 G1 blockade, and inhibits tumor growth by inhibiting mTORC1 2 activity and the mTOR pathway in an acute myeloid leukemia (AML) xenograft model.