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Cat. No. Product name CAS No.
DC60559 PT-179 Featured

PT-179 is a new orthogonal immunomodulatory drug (IMiD) derivative that binds CRBN but does not induce degradation of off-target proteins. PT-179 potently degrades proteins fused to SD40 at either the N or C terminus.

DC60460 SJ3149 Featured

SJ3149 is a uniquely potent and selective CK1α degrader with DC50 of 3.7 nM. SJ3149 shows high activity across a range of acute leukemia (AL) cell lines derived from different hematologic neoplasms, such as B-cell and T-cell acute lymphoblastic leukemia. SJ3149 activity shows a strong correlation with wild-type TP53 expression.SJ3149 (SJ-3149) is uniquely potent and selective CK1α degrader with DC50 of 3.7 nM and Dmax 95% in MOLM-13 cells, potently inhibits the viability of MOLM-13 cells with IC50 of 13 nM. SJ 3149 shows a broad antiproliferative profile on a panel of AML and ALL cell lines with IC50 values in a single digit nanomolar range, and even sub-nanomolar activity. SJ-3149 also potently inhibited the viability of multiple cell lines derived from solid tumors, including breast, soft tissue, and tumors of the male and female reproductive system, with several cell lines being inhibited more potently than MOLM-13. SJ3149 also inhibits several TP53-altered cell lines, such as BT-20 and KU812.

DC60444 FX-909 Featured

FX-909(FX 909) is a first-in-class inverse agonist of the peroxisome proliferator-activated receptor gamma (PPARG) lineage transcription factor with EC50 of 1 nM and shows >2000-fold selectivity for PPARG over PPARA/PPARD - acting through a mechanism that promotes a repressive conformation of PPARG.

DC70648 NH-23-C2 Featured

NH-23-C2 (Caspase-2 inhibitor NH-23-C2) is a potent, selective and cell-permeable endogenous caspase-2 inhibitor, does not block caspase-3 or caspase-8.NH-23-C2 displays off-reactivity with cysteine and threonine proteases (cathepsins B, L, V, S).HCT116 cells were preincubated with NH-23-C2 inhibitor, MDM-2 cleavage was inhibited in a concentration-dependent manner (IC50 =3.11 μM).NH-23-C2 selectively block caspase-2 activity and caspase-2-mediated MDM-2 cleavage.

DC70620 MS934 Featured

MS934 (MS-934) is a VHL-recruiting MEK1/2 degrader (PROTAC) with HT29 DC50 of 18/9 nM for MEK1/2 degradation, respectively.MS934 is more potent at inhibiting the growth of HT-29, SK-MEL-28, H3122, and SUDHL1 cells. MS934 also displays good plasma exposure in mice.

DC70375 E722-2648 Featured

E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.E722-2648 (Compound C-1) inhibited β-catenin/BCL9 complexes at concentrations as low as 1 uM in BCL9-dependent CRC cell lines, Colo320 and HCT116.E722-2648 (Compound C-1) inhibited the expression of bona fide downstream Wnt/β-catenin target genes, AXIN2 and CD44, in the β-catenin/BCL9-dependent CRC cell lines.E722-2648 (Compound C-1) disrupted cholesterol homeostasis via increased cholesterol esterification and lipid droplet accumulation.E722-2648 (Compound C-1) demonstrated antitumorigenic activity in CRC cell lines and xenograft mouse models.

DC70010 98N12-5 Featured

98N12-5 is an ionizable cationic lipid. It has been used in combination with other lipids in the generation of lipid nanoparticles (LNPs). LNPs containing 98N12-5 and encapsulating proprotein convertase subtilisin kexin type 9 (PCSK9) siRNA selectively accumulate in the liver and reduce total serum cholesterol levels in mice and rats and serum LDL levels in cynomolgus monkeys.

DC59010 C14-4 (C14-494,Lipid B-4,Lipid B4) Featured

C14-4 (C14-494,Lipid B-4,Lipid B4) is a novel ionizable lipid with the highest T-cell transfection efficiency and low cytotoxicity.The C14-4 ionizable lipid has been explored for CAR-T therapy.To screen the excellent formulations for mRNA delivery, a lipid library of 24 ionizable lipids was constructed to make iLNPs, which were used to deliver luciferase mRNA into Jurkat cells.[115] The optimal iLNPs formulation was C14-4 iLNPs (C14-4 ionizable lipid, DOPE, chol, and PEG at a molar ratio of 35%, 16%, 46.5%, and 2.5%) (Figure 6c). The optimal dose of luciferase mRNA for C14-4 iLNPs was 30 ng. Compared with electroporated CAR T cells, the CAR T cells engineered via C14-4 iLNPs showed potent cancer-killing activity when they were cocultured with Nalm-6 acute lymphoblastic leukemia cells. To obtain a safer and more effective CAR mRNA delivery vehicle, the orthogonal design provided 256 potential formulations, and 16 representative iLNPs formulations were evaluated.Through evaluating the safety, delivery efficiency, and transfection efficiency of 16 iLNPs, the formulation B10 (C14-4 ionizable lipid, DOPE, chol, PEG at a molar ratio of 40%, 30%, 25%, and 2.5%) was screened out as the optimal performing formulation. The luciferase expression based on B10 formulation was increased threefold than the initial formulation. Reducing the accumulation and clearance of iLNPs in the liver can increase the expression of CAR mRNA in T cells, further improving the therapeutic effect of CAR-T. Studies have shown that cholesterol analogs can alter the mechanisms of intracellular circulation and enhance the delivery of mRNA, which may be related to the reduced recognition of iLNPs by the Niemann Pick C1 (NPC1) enzyme.The addition of a hydroxyl group to various locations in the cholesterol molecule can alter the binding kinetics between the modified cholesterol and NPC1, and reduced NPC1 recognition of cholesterol. The results showed that replacement of 25% and 50% 7 α-hydroxycholesterol for cholesterol in iLNPs improved mRNA delivery to primary human T cells in vitro by 1.8-fold and twofold, respectively.C14-4 is one of the ionizable lipids to efficiently deliver mRNA to Jurkat cells or primary human T cells. It will effectively promote the development of mRNA delivery by iLNPs for CAR-T therapy.

DC57046 ATX-100 Featured

ATX-100 is an ionizable cationic lipid (pKa = 6.38).1,2 It has been used in the generation of lipid nanoparticles (LNPs) for the delivery of siRNA. Intravenous administration of LNPs containing ATX-100 and encapsulating Factor VII siRNA decrease Factor VII blood levels in mice.2

DC53045 STM2457 Featured

STM2457 is in stock, and we can ship it immeidately. STM2457 is a potent inhibitor of METTL3/METTL14 catalytic activity with IC50 of 16.9 nM, Kd of 1.4 nM, respectively. STM2457 is highly specific for METTL3 and shows significant anti-leukaemic effect.