Apoptosis Inducer

Ertabresib (Standard) (INCB-057643 (Standard)) is the analytical standard of Ertabresib (HY-111485). This product is intended for research and analytical applications. Ertabresib (INCB-057643) is an orally active BET protein inhibitor. Ertabresib blocks gene transcription by targeting the BET protein family, induces cell cycle arrest and apoptosis by downregulating proto-oncogenes such as c-MYC, and additionally reduces the expression of FOXP3 and PD-L1 to improve the immune microenvironment. It also exerts synergistic effects and overcomes drug resistance when combined with chemotherapy and XPO1 inhibitors. Ertabresib can be used in research related to high-grade B-cell lymphoma with MYC and BCL2 rearrangements, pancreatic cancer, pancreatitis, and metastatic castration-resistant prostate cancer.

Survivin-IN-1 (Compound II₃) is a potent Survivin (a member of the Inhibitor of Apoptosis Protein family) inhibitor with an IC₅₀ value of 8.1 μM against human lung cancer A549 cells and 9.0 μM against breast cancer MCF-7 cells. Survivin-IN-1 reduces Survivin protein levels and induces tumor cell apoptosis. Survivin-IN-1 is promising for research of malignant tumors such as lung cancer and breast cancer.

PS-1145 (Standard) is the analytical standard of PS-1145. This product is intended for research and analytical applications. PS-1145 is an IκB kinase (IKK) inhibitor with an IC50 of 88 nM.

Ramentaceone (7-Methyljuglon), a naphthoquinone that can be isolated from Drosera sp., inhibits PI3K activity. Ramentaceone (7-Methyljuglon) reduces the expression of the PI3K protein and inhibits the phosphorylation of the Akt protein in breast cancer cells. Ramentaceone (7-Methyljuglon) induces apoptosis.

VAS 3947 (Standard) is the analytical standard of VAS 3947 (HY-111447). This product is intended for research and analytical applications. VAS 3947, a specific NADPH oxidase (NOX) inhibitor, exerts a potent antiplatelet effect. VAS3947 induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins.

LYN-1604 dihydrochloride (Standard) is the analytical standard of LYN-1604 dihydrochloride (HY-101923B). This product is intended for research and analytical applications. LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).

Sapanisertib (INK-128; MLN0128; TAK-228) phosphate is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib phosphate directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib phosphate is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.

PETCM (Standard) is the analytical standard of PETCM (HY-103349). This product is intended for research and analytical applications. PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.

GW 5074 (Standard) is the analytical standard of GW 5074 (HY-10542). This product is intended for research and analytical applications. GW 5074 is a potent and selective c-Raf inhibitor with IC₅₀ of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.

Bendamustine (hydrochloride) (Standard) is the analytical standard of Bendamustine (hydrochloride). This product is intended for research and analytical applications. Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties.

SB 202190 (Standard) is the analytical standard of SB 202190. This product is intended for research and analytical applications. SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits. SB202190 induces autophagy.

Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib (HY-135317). Emavusertib mesylate is an orally active inhibitor for IRAK4 (IC₅₀=57 nM) and FLT3. Emavusertib mesylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib mesylate exhibits antitumor activity in mouse model.

PI-103 (Hydrochloride) (Standard) is the analytical standard of PI-103 (Hydrochloride). This product is intended for research and analytical applications. PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.

PDIC-NC is a STING agonist. PDIC-NC is cytotoxic to tumor cells and induces ROS explosion, apoptosis and autophagy. PDIC-NC has lung specific distribution and can be used in the study of lung cancer.

ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models.

CL-387785 (EKI-785; WAY-EKI 785) (Standard) is the analytical standard of CL-387785 (HY-10325). This product is intended for research and analytical applications. CL-387785 is an orally active EGFR inhibitor with an IC₅₀ of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC₅₀ of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease.

6-Hydroxycoumarin (Standard) is the analytical standard of 6-Hydroxycoumarin (HY-N6656). This product is intended for research and analytical applications. 6-Hydroxycoumarin is a plant-derived secondary metabolite of the coumarin class, possessing insecticidal, antitumor, and other biological activities. 6-Hydroxycoumarin targets the midgut tissue of the red imported fire ant (Solenopsis invicta), inhibits CYP450, induces elevated activities of GST, CarE, and SOD, disrupts mitochondrial ultrastructure, triggers apoptosis, and also impairs insect neuromuscular behavior. 6-Hydroxycoumarin exhibits photoallergic properties and serves as an intermediate for the synthesis of isoxazolyl and triazolyl derivatives. 6-Hydroxycoumarin is applicable to research related to red imported fire ant control.

TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC₅₀ of 5.90 μM) and the cell viability of p53 expressing A549R (IC₅₀ of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models.

Palomid 529 (Standard) is the analytical standard of Palomid 529. This product is intended for research and analytical applications. Palomid 529 is a potent inhibitor of mTORC1 and mTORC2 complexes.

Araloside A (Standard) (Chikusetsusaponin IV (Standard)), triterpenoid saponins, is an orally active component of Aralia elata. Araloside A (Standard) shows low-renin-inhibitory activity with an IC₅₀ of 77.4 μM. Araloside A (Standard) can inhibit cell proliferation and induce apoptosis. Araloside A (Standard) suppresses inflammatory cytokines IL-1β and IL-6 production. Araloside A (Standard) can be used for the researches of cancer, inflammation and cardiovascular disease, such as renal cell carcinoma and rheumatoid arthritis.