APL-5125|CAS 2830619-57-1|DC Chemicals

Cas No.:	2830619-57-1
Chemical Name:	APL-5125
Formula:	C₂₇H₂₄F₅N₃O₅
M.Wt:	565.49
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Cat. No.	Product name	Field of application
DC74445	FL-1607	FL-1607, a novel Fam20C inhibitor, has shown remarkable anti-proliferative effects in triple-negative breast cancer (TNBC) cells. This compound induces apoptosis and significantly reduces the migration ability of MDA-MB-468 cells, underscoring its potential as a promising therapeutic agent for TNBC treatment.
DC8146	PF-5006739	PF-5006739 is a potent inhibitor of casein kinases 1 delta (CK1δ) and 1 epsilon (CK1ε)
DC11251	Casein Kinase inhibitor A86	CKIα inhibitor A86 is a groundbreaking pan-specific inhibitor targeting Casein Kinase I (CSNK1), with a remarkable binding affinity (Kd=1-10 nM) and a specific Kd of 9.8 nM for CKIα. Beyond its primary activity, this compound also demonstrates dual inhibitory effects on the transcriptional kinases CDK7 and CDK9. Notably, it exhibits minimal to no inhibition against CDK8, CDK13, CDK11a, CDK11b, and CDK19, highlighting its selective pharmacological profile.
DC11250	Casein Kinase inhibitor A51	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.
DC11950	SR-2890	A potent, highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 4 nM for CK1δ.
DC79853	IOR-160	IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research.
DC79742	MU1742-amide-C6-acid	MU1742-amide-C6-acid is a CK1δ/ε inhibitor. MU1742-amide-C6-acid can be used for synthesis of PROTAC AH081.
DC79429	APL-5125	APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer.
DC79358	AH081	AH081 (Compound 38) is a CK1δ/ε PROTAC degrader. AH081 is the negative control compound of AH078. AH081 has inhibitory but no degradation activity for CK1δ/ε by using an inactive stereoisomer of the VHL ligand.
DC78683	KDX1381	KDX1381 is a bivalent CK2α inhibitor (IC50: 17 nM, KD: 54 nM). KDX1381 has antitumor activity in mouse 786-O and A375 tumor xenograft models. KDX1381 combined with VEGFR inhibitors or DNA damaging agents enhances antitumor efficacy in mouse hepatocellular carcinoma and glioma models.