cc-4

ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide and it is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1].

CC-401 is a specific inhibitor of JNK (Ki: 25-50nM).

CC-401 Hydrochloride (CC401 HCl) is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor (Ki of 25 to 50 nM.)with potential antineoplastic activity.

GCC-4401C methanesulfonate is a factor Xa inhibitor similar to rivaroxaban that is currently under development for venous thromboembolic disease (VTE).

GCC-4401C free base is a factor Xa inhibitor similar to rivaroxaban that is currently under development for venous thromboembolic disease (VTE).

High affinity and subtype selective α6β2 and α4β2 partial agonist (Ki values are 12 and 26nM for rat α6β2 and α4β2 receptors respectively). Has low affinity for α3β4 and α7 receptors (Ki values are 4.8 and 13 μM for human α3β4 and rat α7 receptors respectively). Stimulates dopamine release from striatal slices in vitro. Attenuates nicotine-induced self-administration and conditional place preference in rats. Sala et al (2013) CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking c Br.J.Pharmacol. 168 835 PMID:22957729 |Riganti et al (2005) Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells. Br.J.Pharmacol. 146 1096 PMID:16273122 |Carbonnelle et al (2003) Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes. Eur.J.Pharmacol. 471 85 PMID:12818695

STF-31 is an inhibitor of glucose transporter 1 (GLUT1) with IC50 of 1 μM.

Pomalidomide (CC-4047) is an anti-angiogenic and immunomodulatory agent. Pomalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN) and is commonly used in the synthesis of PROTAC products.

STF-62247 is TGN inhibitor with IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively.

(S,R,S)-AHPC-C4-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 28) is a synthesized E3 ligase ligand-linker conjugate comprising the (S,R,S)-AHPC-based VHL ligand and a linker.

(S,R,S)-AHPC-C4-NH2 dihydrochloride is a chemically derived E3 ligase ligand-linker conjugate that includes the (S,R,S)-AHPC VHL ligand and a linker specifically engineered for EED-Targeted PROTAC[1].

(S,R,S)-AHPC-C4-NH2 is a custom-synthesized conjugate consisting of an E3 ligase ligand-linker, combining a VHL ligand based on (S,R,S)-AHPC with a linker specifically designed for EED-targeted PROTAC[1].

High affinity JNK inhibitor (Ki values are 25-50 nM). Inhibits JNK via competitive binding of the ATP-binding site of active, phosphorylated JNK. Exhibits > 40-fold selectivity for JNK over p38, ERK, IKK2, protein kinase C, Lck and ZAP70. Hepatoprotective. Also inhibits HCMV replication. Uehara et al (2004) c-Jun N-terminal kinase mediates hepatic injury after rat liver transplantation. Transplantation. 78 324 PMID:15316358 |Uehara et al (2005) JNK mediates hepatic ischemia reperfusion injury. J.Hepatol. 42 850 PMID:15885356 |Ma et al (2007) A pathogenic role for c-Jun amino-terminal kinase signaling in renal fibrosis and tubular cell apoptosis. J.Am.Soc.Nephrol. 18 472 PMID:17202416 |Ma et al (2009) Blockade of the c-Jun amino terminal kinase prevents crescent formation and halts established anti-GBM glomerulonephritis in the rat. Lab.Invest. 89 470 PMID:19188913 |Zhang et al (2015) The c-Jun N-terminal kinase inhibitor SP600125 inhibits human cytomegalovirus replication. J.Med.Virol. 87 2135 PMID:26058558 |Vasilevskaya et al (2015) Inhibition of JNK sensitizes hypoxic colon cancer cells to DNA-damaging agents. Clin.Cancer.Res. 21 4143 PMID:26023085

ARCC 4 negative control is a negative control for ARCC 4. Binds androgen receptors (AR) without inducing degradation.

MM41 is a human telomeric and gene promoter DNA quadruplex stabilizer with an IC50 of <10 nM against the MIA PaCa-2 pancreatic cancer cell line.

Metitepine is a serotonin receptor antagonist in the CNS used as an antipsychotic.

CD4 (81-92) is a peptide that was previously found to inhibit gp120 binding, HIV-1 infectivity, and syncytium formation.

JNJ-39729209 is a TRPV1 antagonist.

Mobocertinib (tak788) is a potent inhibitor of epidermal growth factor receptor (EGFR) and an antineoplastic agent

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

CathepsinG, human neutrophils (CTSH; ACC4), is a serine protease found in polymorphonuclear neutrophils (PMN), playing a role in the inflammatory response.

C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).

Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor that reduces the production of pro-inflammatory mediators and cytokines. Dovramilast is used in the study of Mycobacterium tuberculosis infections and lupus erythematosus.

Apremilast (CC-10004) (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities.