cc 4

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

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

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.

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).

AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor used for asthma research.

CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).

7,4'-Dihydroxyflavone (4',7-Dihydroxyflavone) can induce transcription of nodulation (nod) genes in Rhizobium meliloti. It has inhibitory activities against COX-2.

Mogamulizumab (KW-0761) is a monoclonal antibody targeting T cell CC chemokine receptor 4. It exhibits anticancer activity by eliminating tumor cells through antibody-dependent cytotoxicity (ADCC) and can be used in the study of cancer, adult T-cell leukemia lymphoma (ATLL), and cutaneous T-cell lymphoma (CTCL).

Apremilast D5 (CC-10004 D5) is a deuterium-labeled Apremilast. Apremilast is an orally available inhibitor of PDE-4 (IC50: 74 nM). Apremilast inhibits TNF-α release by lipopolysaccharide (IC50: 104 nM).

KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chemokine, stromal cell-derived factor 1alpha, to CXCR4 specifically and subsequent signal transduction. KRH-1636 prevented monoclonal antibodies from binding to CXCR4 without down-modulation of the coreceptor. KRH-1636 seems to be a promising agent for the treatment of HIV-1 infection.

CCR4 Antagonist 4 (Compound 22) is a potent and selective antagonist of the CC chemokine receptor-4 (CCR4), displaying an IC50 value of 0.02 μM. It also inhibits MDC-mediated chemotaxis and Ca2+ mobilization, with IC50 values of 0.007 μM and 0.003 μM, respectively. This compound is utilized in research on allergic inflammation [1].

Antiparasitic agent-4 (compound 4q) exhibits high antiparasitic activity with an IC50 of 8.51 μM for Leishmania infantum (L. infantum) and an IC50 of 2.20 μM for Trypanosoma cruzi (T. cruzi). It is also cytotoxic against HepG2 cells with a CC50 of 18.97 μM [1].

CC-90005 is a potent, selective, and orally active inhibitor of protein kinase C-θ (PKC-θ) with an IC50 of 8 nM, demonstrating strong selectivity over PKC-δ (IC50=4440 nM). Additionally, CC-90005 can inhibit T cell activation by IL-2 expression[1].

GSK2239633 is a potent CC-chemokine receptor 4 antagonist with pIC50 of 7.9. The CC-chemokine receptor 4 (CCR4) is thought potentially to play a critical role in asthma pathogenesis due to its ability to recruit type 2 T-helper lymphocytes to the inflamed airways. Therefore, CCR4 provides an excellent target for anti-inflammatory therapy.

Sodium thiosulfate (Pentahydrate) is an antioxidant and antifungal. Sodium thiosulfate protects against cisplatin-induced hearing loss in children and is not associated with serious adverse events attributed to its use[3]. The addition of sodium thiosulfate, administered 6 hours after cisplatin chemotherapy, resulted in a lower incidence of cisplatin-induced hearing loss among children with standard-risk hepatoblastoma, without jeopardizing overall or event-free survival[4]. Calciphylaxis is a potentially fatal disorder of abnormal calcium deposition. Treatment is multifaceted, and improved outcomes have been demonstrated with intravenous sodium thiosulfate; however, the use of this medication can be limited by its adverse effects[5]. TST (topical sodium thiosulfate) appears to be a relatively well-tolerated adjuvant treatment for CC(calcinosis cutis)[6]. The combined treatment of sodium thiosulfate, pamidronate and calcitomimetics has been effective and safe for the treatment of calciphylaxis, inducing complete remission[7].

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist with IC50 values of 180 nM and 24 nM for CCR2 inhibition and MCP-1-induced chemotaxis inhibition, respectively.

CCR4 antagonist 2 (Compound 31) is a novel, potent, orally bioavailable small molecule antagonist of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+ flux and [chemotaxis] CTX at 40 nM and 70 nM, respectively.

Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a Btk kinase activity inhibitor with an IC50 of less than 0.5 nM and a Kinact Ki of 7.69×10^4 M^-1s^-1.

AF-399/42018025 is a CC chemokine receptor 4 (CCR4) antagonist.

CC-1088 is an analog of thalidomide with potential antineoplastic activity that belongs to the functional class of agents called selective cytokine inhibitory drugs (SelCIDs). SelCIDs inhibit phosphodiesterase-4 (PDE 4), an enzyme involved in tumor necrosis factor alpha (TNF alpha) production. CC-1088 inhibits production of the cytokines vascular endothelial growth factor (VEGF) (a pro-angiogenic factor) and interleukin-6 (IL-6).

FtsZ-IN-4, an orally active inhibitor of FtsZ (filamenting temperature-sensitive mutant Z), demonstrates remarkable antibacterial activity and favorable pharmaceutical properties. With low cytotoxicity (CC 50 >20 μg mL) [1], FtsZ-IN-4 exhibits promising potential for therapeutic applications.

GSK2239633A is an allosteric antagonist of CC-chemokine receptor 4 (CCR4) with a pIC50 of 7.96 for the binding of [125I]-TARC to human CCR4.

Apremilast, (+/-)-, is a small molecule inhibitor of phosphodiesterase 4 (PDE4) with oral activity. It is used to treat psoriatic arthritis.

(Rac)-Apremilast D5 is a deuterium-labeled version of the enantiomer (R)-Apremilast, also known as (R)-CC-10004, which itself is one specific form of Apremilast.

(R)-Apremilast ((R)-CC-10004), the enantiomer of Apremilast, is one of the isoindoline derivatives.