Ionizable Lipid Products

Emixustat hydrochloride strongly inhibits 11-cis-retinol production with IC50 values of 232 ± 3 nM.Emixustat hydrochloride is a novel visual cycle modulator, in healthy volunteers. Oral Emixustat was safe and well tolerated when administered once daily for 14 days with minimal systemic adverse events reported. Evaluation of emixustat in subjects with geographic atrophy associated with dry age-related macular degeneration.[2]

PF-562271 (besylate) is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase with IC50 of 1.5 nM and 13 nM, and has > 100-fold selectivity against other protein kinases, except for some CDKs.

TRIF agonist AV-C is a novel TRIF pathway agonist that activates innate and interferon-associated responses, strongly inhibits replication of ZIKV, CHIKV, and DENV (IC90~5 uM); activates IFNAR-mediated transcription and translation of antiviral effector genes, AV-C-mediated, IRF3-dependent innate activation occurs independently of adaptor proteins IPS-1/MAVS and STING but requires TRIF.

KX2-391 is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation

Casein Kinase inhibitor A51 (CKIα inhibitor A51) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=0.5-20 nM, CKIα Kd=5.3 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19; target both CDK7 and CDK9 with low nM Kd values; induces leukemia cell apoptosis at <160 nM, in correlation to the capacity to stabilize p53; shows high and selective sensitivity against leukemic CFUs in colony-forming unit (CFU) assay, without effect on normal hematopoietic CFUs; blocking CKIα together with CDK7 and/or CDK9 synergistically stabilize p53, deprive leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, induce apoptosis, abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1; demonstrates therapeutic efficacy with preserved hematopoiesis and leukemia cure potential in AML mouse models.

Mobocertinib is a potent epidermal growth factor receptor (EGFR) inhibitor and an antineoplastic agent, extracted from patent WO2019222093A1, compound A[1][2].

LJ 001 ((LJ-001, LJ001) is a broad-spectrum antiviral agent targeting entry of enveloped viruses, including influenza A, filoviruses, poxviruses, arenaviruses, bunyaviruses, paramyxoviruses, flaviviruses, and HIV-1; specifically intercalates into viral membranes, irreversibly inactivates virions while leaving functionally intact envelope proteins, and inhibits viral entry at a step after virus binding but before virus-cell fusion; specifically inhibits virus-cell but not cell-cell fusion

LY3023414 potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. LY3023414 potently inhibits mTORC1/2 at low nanomolar concentrations.

MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation[1].

BMS-813160 is the first dual CCR2/CCR5 antagonist to enter clinical development for cardiovascular.

Prodigiosin (Prodigiosine) is a secondary metabolite of Symbiotic bacteria, with anti-fungal and anti-cancer activity[1][2].

Enzastaurin is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.

I-BRD9 is the first selective cellular chemical probe for BRD9 (pIC50=7.3).IC50 value: 7.3 (pIC50) [1]Target: BRD9in vitro: I-BRD9 is a selective cell active chemical probe for bromodomain containing protein 9 inhibition. I-BRD9, the first selective cellular chemical probe for bromodomain-containing protein 9 (BRD9). I-BRD9 is identified through structure-based design, leading to greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways and to the best of our knowledge, represents the first selective tool compound available to elucidate the cellular phenotype of BRD9 bromodomain inhibition.

TAK-243 is a potent and selective ubiquitin-like modifier activating enzyme 1 (UBA1) inhibitor.

STING agonist-3 is a selective small-molecule STING agonist. STING agonist-3 is a non-nucleotide STING agonist which has durable anti-tumor effect and tremendous potential to improve treatment of cancer[1].

Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).

Furimazine is an imidazopyrazinone substrate. NanoLuc (Nluc) paired with Furimazine produced 2.5 million-fold brighter luminescence in mammalian cells relative to Oluc-19 with Coelenterazine.

NVP-CGM097 is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.

GDC-0032 is a potent, next-generation β iso Form-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. IC50 Value: 0.29 nM/0.12 nM /0.97 nM(PI3Kα/δ/γ) Target: PI3K in vitro: GDC-0032 is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ iso Forms, with 30 fold less inhibition of the PI3K β iso Form relative to the PI3Kα iso Form. Preclinical data show that GDC-0032 has increased activity against PI3Kα iso Form (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM. in vivo: GDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t1/2 of 40 hours. The combination of GDC-0032 enhances activity of fulvestrant resulting in tumor regressions and tumor growth delay (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 with tamoxifen enhances the efficacy of tamoxifen in vivo (102%TGI For GDC-0032) .For the detailed information of GDC-0032, the solubility of GDC-0032 in water, the solubility of GDC-0032 in DMSO, the solubility of GDC-0032 in PBS buffer, the animal experiment (test) of GDC-0032, the cell expriment (test) of GDC-0032, the in vivo, in vitro and clinical trial test of GDC-0032, the EC50, IC50,and Affinity of GDC-0032, Please contact DC Chemicals.