Ionizable Lipid Products

IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.

Santacruzamate A is a potent and selective histone deacetylase inhibitor.

BML-210 is a novel HDAC inhibitor, and its mechanism of action has not been characterized.

M344 (D 237) is an inhibitor of histone deacetylase (IC50=100 nM) and an inducer of terminal cell fifferentiation.

SC66 is a novel Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.

HPOB is a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 56 nM, >30 fold less potent against other HDACs.target: HDAC6 [1]IC 50: 56nM [1]In vitro: HPOB causes growth inhibition of normal and transformed cells but does not induce cell death. HPOB enhances the effectiveness of DNA-damaging anticancer drugs in transformed cells but not normal cells. [1] Neuroprotective effect of HPOB demonstrated the crucial role of HDAC6 inhibition in reducing Cort-induced apoptosis in PC12 cells. Pre-treatment with HPOB remarkably reduces Cort-induced cytotoxicity and confirms the anti-apoptotic effect of HPOB via the caspase-3 activity assay and H33342/PI and TUNEL double staining. [2]In vivo: on corticosterone (Cort)-induced apoptosis and explors the possible mechanism of action of HPOB in rat adrenal pheochromocytoma (PC12) cells, which possesses typical neuron features and expresses high levels of glucocorticoid receptors. [2]

GSK583 is a highly potent and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM.

WIKI4 is a potent inhibitor of Wnt/β-catenin signaling (EC50 ~ 75 nM); inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM).

Tivantinib is a novel and highly selective c-Met tyrosine kinase inhibitor with Ki of 355 nM.

TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a Ki value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC50s of 18 and 63 nM as well as monkey PHD2 with an IC50 value of 22 nM[1].

CPI-169 racemate is the racemate form of CPI-169, which is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2); decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines. IC50 value: < 1 nM (catalytic activity of PRC2); 70 nM (Cellular EC50) in vitro: CPI-169, a representative compound from that effort, inhibits the catalytic activity of PRC2 with an IC50 of < 1nM, decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines. Importantly, compound treatment triggers a sequence of downstream functional consequences of EZH2 inhibition whereby apoptosis is not induced before ten days of continuous target engagement . in vivo: Administered subcutaneously at 200 mpk twice daily (BID), CPI-169 is well tolerated in mice with no observed toxic effect or body weight loss. In the present study we show that CPI-169 treatment led to tumor growth inhibition (TGI) of an EZH2 mutant KARPAS-422 DLBCL xenograft. The TGI is proportional to the dose administered and to the reduction of the pharmacodynamic marker H3K27me3. The highest dose, 200 mpk, BID led to complete tumor regression. Since CHOP (cyclophosphamide, doxorubicin, vincristine and prednisone) is the standard treatment of advanced DLBCL, we were interested in combining a suboptimal dose of CPI-169 (100 mpk, BID) with a single dose of CHOP in the KARPAS-422 model. After a week of combinatorial treatment the tumors rapidly regressed and became unpalpable. Four weeks after the last dose only a single mouse presented a palpable tumor.

PAMP-12(human, porcine) is a major component of immunoreactive (ir)-PAMP, is processed from the adrenomedullin precursor, is a potent hypotensive peptide and participates in cardiovascular control.

CSP1 is a potent and selective ComD1 receptor agonist, with an IC50 of 10.3 nM. CSP1 is a major variants of competence-stimulating peptide (CSP), and it can regulate genetic transformation of S. pneumonia by modulating quorum sensing (QS). CSP1 can act as an antibacterial agent.

Fmoc-Val-Cit-PAB-PNP is a peptide prodrug linker, is a linker for antibody-drug-conjugation (ADC).

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

BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.

YH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agent.YH239-EE inhibits the growth of OCI-AML-3 cells with wild type p53 by inhibiting the p53-MDM2 interaction. YH239-EE induces cell cycle arrest and causes potent cell apoptosis via activation of p53 and downstream targets in four AML cells (OCI-AML-3 and MOLM-13 with wt p53, NB4 with p53 mutation, and HL60 with p53 deletion).

AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.

Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.

ALK2-IN-1 is a activin receptor-like kinase-2 (ALK2) inhibitor extracted from patent WO2017181117A1, Compound 876, has an IC50 of <10 nM[1].