Autophagy Inducer

Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and EGFR/HER1 (IC₅₀=500 nM).

Veliparib (dihydrochloride) (Standard) is the analytical standard of Veliparib (dihydrochloride) (HY-10130). This product is intended for research and analytical applications. Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.

Lapatinib-d₇ (GW572016-d₇) is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

Pazopanib (Standard) is the analytical standard of Pazopanib. This product is intended for research and analytical applications. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC₅₀s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

N-Desmethyl clomipramine-d₆ (Desmethylclomipramine-d₆; Norclomipramine-d₆) is the deuterated-labeled N-Desmethyl clomipramine (HY-12388). N-Desmethyl clomipramine (Desmethylclomipramine; Norclomipramine) is the orally active major active metabolite of the tricyclic antidepressant Clomipramine (HY-B0457A), possessing multiple activities including anti-inflammatory, antioxidant, antibacterial, and antiparasitic effects. N-Desmethyl clomipramine blocks autophagosome-lysosome fusion, leading to the accumulation of LC3-II, p62, ATG7, WIPI2, and ATG5-12, reactivates the p53/p21 pathway, induces apoptosis through C-PARP and C-CAS3, and inhibits the proliferation, migration, and invasion of renal cancer cells. N-Desmethyl clomipramine inhibits LdTOPIA, inducing R-loop accumulation in the nucleus of Leishmania, ultimately causing parasite death. N-Desmethyl clomipramine can be used for research on depression, metastatic renal cell carcinoma, and leishmaniasis.

Efavirenz-d₅ (DMP 266-d₅) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a K_i of 2.93 nM and exhibits an IC₉₅ of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture. Efavirenz-d₅ is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cilostazol-d₂ (OPC 13013-d₂) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM.

Linagliptin-d₅ (BI 1356-d₅) is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC₅₀ of 1 nM.

Dacinostat (Standard) is the analytical standard of Dacinostat. This product is intended for research and analytical applications. Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.

C646 (Standard) is the analytical standard of C646 (HY-13823). This product is intended for research and analytical applications. C646 is a selective and competitive histone acetyltransferase p300 inhibitor with K_i of 400 nM, and is less potent for other acetyltransferases.

Cabazitaxel (Standard) is the analytical standard of Cabazitaxel. This product is intended for research and analytical applications. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.

Panobinostat lactate (Standard) is the analytical standard of Panobinostat lactate (HY-10224A). This product is intended for research and analytical applications. Panobinostat lactate is a potent and orally active non-selective HDAC inhibitor. Panobinostat lactate has antineoplastic activities. Panobinostat lactate effectively disrupts HIV latency. Panobinostat lactate induces cell apoptosis and autophagy. Panobinostat lactate can be used for the study of refractory or relapsed multiple myeloma.

Milciclib (Standard) is the analytical standard of Milciclib. This product is intended for research and analytical applications. Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.

Tioxolone (Standard) is the analytical standard of Tioxolone. This product is intended for research and analytical applications. Tioxolone is an inhibitor for the carbonic anhydrase. Tioxolone exhibits anti-leishmanial, antitumor, and anti-inflammatory activities. Tioxolone can be used in research of acne and psoriasis.

AZD 6482 (Standard) is the analytical standard of AZD 6482 (HY-10344). This product is intended for research and analytical applications. AZD 6482 (KIN-193) is a potent and selective p110β inhibitor with an IC₅₀ of 0.69 nM.

Isomahanine, carbazole alkaloid, is an antioxidative agent. Isomahanine has DPPH radical scavenging activity with an IC₅₀ value of 24 μM.

Rilmenidine (Standard) is the analytical standard of Rilmenidine. This product is intended for research and analytical applications. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.

Mocetinostat (Standard) is the analytical standard of Mocetinostat. This product is intended for research and analytical applications. Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.

Thalidomide 4'-oxyacetamide-C1-PEG3-C3-amine hydrochloride is a functionalized cereblon ligand for PROTAC research and development with terminal amine ready for conjugation to a target protein ligand.

Laduviglusib (monohydrochloride) (Standard) is the analytical standard of Laduviglusib (monohydrochloride). This product is intended for research and analytical applications. Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy.