RO-275|CAS 2648837-04-9|DC Chemicals

Cas No.:	2648837-04-9
Chemical Name:	RO-275
Formula:	C₁₈H₁₄ClN₅O
M.Wt:	351.79

Cat. No.	Product name	Field of application
DC81075	Mps1/TTK-IN-1	Mps1/TTK-IN-1 (Compound cpd-5), a derivative of NMS-P715, is a Mps1 kinase inhibitor with an IC50 of 9.2 nM and a Kd of 1.6 nM. Mps1/TTK-IN-1 specifically targets the ATP-binding pocket of the Mps1 kinase. Mps1/TTK-IN-1 maintains inhibitory activity against Mps1 drug-resistant mutants (C604Y, C604W) with IC50 values of 170 and 19 nM and Kd values of 471 and 349 nM. Mps1/TTK-IN-1 can block the phosphorylation of kinetochore protein KNL1 mediated by Mps1, interfere with the spindle assembly checkpoint function, prevent the correct separation of chromosomes, and thereby inhibit the mitosis and proliferation of tumor cells.
DC73619	Org 34167	Org 34167 HCl salt is a broad-spectrum inhibitor of HCN channels with IC50 of 23.4, 8.2 and 9.2 uM for HCN1, HCN2 and HCN4 channels, respectively, slowing activation and causing a hyperpolarising shift in voltage-dependence of activation.
DC73618	NUCC-0200590	NUCC-0200590 is a small-molecule inhibitor of the TRIP8b-HCN interaction with IC50 of 7.0 uM in AlphaScreen assays, effectively disrupts the TRIP8b-HCN interaction in vitro and in vivo.
DC70477	EC18 HCN inhibitor	EC18 HCN inhibitor is a HCN channel inhibitor. EC18 acts as a potent HCN4 inhibitor in a human iPSC-derived sinus node model with proven HCN4 expression. EC18 is an attractive pharmacological tool, enabling HCN channel-modulation studies with some specificity for HCN4 (EC50 [HCN4] = 3.98 ± 1.16 µM) over HCN1 (EC50 = 21.00 ± 3.98 µM) and HCN2 (EC50 = 19.35 ± 4.48 µM). EC18 abolishes HCN4 triggered pace making in a human iPSC (hiPSC) pacemaker model.
DC81807	α-Obscurine derivative-1	α-Obscurine derivative-1 (Compound 7) is a α-Obscurine derivative. α-Obscurine derivative-1 inhibits CaV3.1 ion channel current with an IC50 of 0.19 μM. α-Obscurine derivative-1 can be used in the research of neurological disorders.
DC81354	PROTAC EZH2 Degrader-16	PROTAC EZH2 Degrader-16 (compound 51) is a PROTAC protein degrader targeting EZH2 with an IC50 of 13.74 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-16 exerts antiproliferative activity against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-16 can be used for the research of diffuse large B-cell lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).
DC81352	PROTAC EZH2 Degrader-14	PROTAC EZH2 Degrader-14 is an EZH2 PROTAC degrader, with an IC50 of 18.21 μM against diffuse large B-cell lymphoma cells, and exhibits no antiproliferative activity against non-target cells at concentrations up to 30.00 μM. PROTAC EZH2 Degrader-14 can be used in studies related to diffuse large B-cell lymphoma. (Pink: Histone Methyltransferase ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).
DC81064	MMP-9-IN-13	MMP-9-IN-13 (Example 1) is a selective inhibitor of human MMP9 with an IC50 value of 0.02 nM. MMP-9-IN-13 can be used in the research of ocular surface.
DC80977	LUF7996	LUF7996 is a CCR2 PROTAC Degrader degrading CCR2 with DC50 = 2.6 μM. LUF7996 demonstrates engagement of both and the E3 ligase cereblon and displays sustain and concentration-dependent degradation of CCR2. LUF7996 reliance on the lysosomal pathway to induce CCR2 degradation. LUF7996 efficiently inhibits monocyte migration in virto. (Pink: CCR2 ligand ; Blue: Cereblon ligand ; Black: linker).
DC80551	DM243	DM243 is an EPAC1 activator and STAT3 modulator with an pIC50 of 4.769. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells, with no activation of EPAC2 or PKA. DM243 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing α-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts.