Apoptosis

Ch282-5, an orally active inhibitor targeting the Bcl-2 protein, promotes mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. It demonstrates antiproliferative effects on colorectal cancer cells, effective both in vitro and in vivo, while also inhibiting metastasis. Further, Ch282-5 augments Oxaliplatin-induced autophagy (Autophagy) by downregulating Mcl-1 protein and raising platelet count, which helps mitigate the adverse effects of Navitoclax.

PD-L1/VISTA-IN-2 (Compound S8) is an orally active dual inhibitor targeting PD-L1 and VISTA, with an IC50 of 1.4 μM for PD-L1 and a KD of 2.1 μM for VISTA. This compound can activate the tumor immune microenvironment, exerting anticancer effects.

JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2.

L-Ascorbic acid sodium salt (Vitamin C sodium salt) is a more bioavailable form of vitamin C that is an alternative to taking ascorbic acid as a supplement.

ISRIB is a potent and selective PERK inhibitor.

Antineoplaston A10 (NSC-648539) is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker. The mechanism of action of irbesartan is as an Angiotensin 2 Receptor Antagonist.

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Human soluble DPP4. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Human soluble DPP4. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Human soluble DPP4, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Human soluble DPP4 in the samples is then determined by comparing the OD of the samples to the standard curve.

BTM-3566 triggers ISR via OMA1, induces apoptosis in cancer cells, and is used to research DLBCL.

AChE-IN-81 (compound 22) is a reversible, selective inhibitor of AChE with an 80.0% inhibition rate and an IC50 of 3.7 μM. It binds to AChE with an affinity (Kd) of 5.37 μM. AChE-IN-81 effectively reduces apoptosis in zebrafish brain cells and shows potential neuroprotective activity in an H2O2-induced SH-SY5Y cell damage model.

Ro 41-5253 is a RARα antagonist with antitumor activity that inhibits the proliferation of ZR-75.1 estrogen receptor-positive breast cancer cells.

Niacin is a water-soluble B vitamin with antihyperlipidemic effects, found in food and converted to niacinamide for coenzyme activity.

Applications Protected Curcumin (C838500). A natural phenolic compound. Potent anti-tumor agent having anti-inflammatory and anti-oxidant properties. Induces apoptosis in cancer cells and inhibits phorbol ester-induced protein kinase C (PKC) activity. Reported to inhibit production of inflammatory cytokines by peripheral blood monocytes and alveolar macrophages. Potent inhibitor of EGFR tyrosine kinase and IκB kinase. Inhibits inducible nitric oxide synthase (iNOS), cycloxygenase and lipoxygenase. Easily penetrates into the cytoplasm of cells, accumulating in membranous structures such as plasma membrane, endoplasmic reticulum and nuclear envelope. References Srinivasan, et al.: J. Pharm. Pharmacol., 5, 448 (1953), Tu, B., et al.: J .Cell Biol., 164, 341 (2004), Xu, G., et al.: Biochemistry, 44, 9817 (2005), Johnson, J., et al.: Cancer Lett., 255, 170 (2007),

Pyridinium bisretinoid A2E (A2E) TFA, a fluorophore derived from retinal pigment epithelium (RPE) lipofuscin, initiates blue-light-induced apoptosis, mediates

Pladienolide B, a macrolide from Streptomyces, inhibits spliceosome's SF3B1, causing necrosis and antitumor effects for leukemia and lymphoid studies.

GPNA hydrochloride inhibits Gln transporter ASCT2, induces apoptosis in A549 cells, blocks SNAT1/2/4/5 & LAT1/2 transporters, and is a GGT substrate.

PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1/3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1/IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)

Minnelide is a prodrug of triptolide,and shows potent antitumor activity in a number of tumor types.

CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.