Bcl-2 Family Inhibitor

Bcl-2-IN-15 (Compound 13d)) is a Bcl-2 inhibitor (IC₅₀: 363 nM). Bcl-2-IN-15 inhibits the proliferation ofNCI leukemia cancer cell line.

MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer.

Bcl-2-IN-19 (compound 27) is a potent Bcl-2 inhibitor for targeting breast cancer.

Bcl-2-IN-24 (Compound 11g) is an efficient and selective Bcl-2 inhibitor with a K_d value of 11.3 μM. Bcl-2-IN-24 exhibits anti-proliferative activity against HCT-116 cells and A549 cells. Bcl-2-IN-24 effectively inhibits the colony-forming ability of tumor cells and induces cell apoptosis. Bcl-2-IN-24 can be used for research on colon cancer and lung cancer.

Beclanorsen is an antisense oligonucleotide targeted to the mRNA of the Bcl-2 oncoprotein.

XSJ81 is an orally active anti-cancer agent. XSJ81 significantly inhibits the proliferation of ampullary carcinoma (AC) DPC-X3 cells with an IC₅₀ of 0.655 μM. XSJ81 inhibits the colony formation, arrests cell cycle at the G2/M phase and inhibits the migration in DPC-X3 cells. XSJ81 induces DNA damage and apoptosis in DPC-X3 cells. XSJ81 demonstrates significant anti-tumor efficacy in mice bearing DPC-X3 xenografts. XSJ81 can be used for the study of ampullary carcinoma.

Bfl-1-IN-7 is an orally active and selective Bfl-1 inhibitor with an IC₅₀ value of 0.015 μM. Bfl-1-IN-7 activates caspase 3/7, and when combined with the Mcl-1 inhibitor AZD5991 (HY-101533), it reduces the viability of lymphoma cells. Bfl-1-IN-7 can be used in lymphoma-related studies.

BAX Human Pre-designed siRNA Set A contains three designed siRNAs for BAX gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Antitumor agent-217 is a dual mitochondria-targeted anticancer agent. Antitumor agent-217 exhibits potent and selective antiproliferative activity against bladder cancer cell line J82 (IC₅₀ = 6.3 μM), and inhibits colony formation and migration of J82 cells. Antitumor agent-217 accumulates in mitochondria, alters mitochondrial morphology, reduces ATP production, increases ROS generation and decreases mitochondrial membrane potential. Antitumor agent-217 induces apoptosis (Apoptosis) and ferroptosis (Ferroptosis) in bladder cancer cells. Antitumor agent-217 can be used for the research of bladder cancer.

Spicamycin, an adenine nucleoside antibiotic with antifungal and antitumor activities. Spicamycin is also a potent inducer of differentiation of myeloid leukemia cells. Spicamycin induces apoptosis in NB4 cells via down-regulation of Bcl-2 expression and modulation of PML protein.

VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC₅₀: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells.

Bcl-2-IN-3 (Compound 10) is a Bcl-2 inhibitor. Bcl-2-IN-3 can be used for the research of cancer.

BI-3812 (Standard) is the analytical standard of BI-3812 (HY-111381). This product is intended for research and analytical applications. BI-3812, a chemical probe, is a highly efficient BCL6 inhibitor that is capable of suppressing the BTB domain of BCL6, with an IC₅₀ value of ≤ 3 nM, exhibiting antitumor activity.

BP1002 is an antisense oligonucleotide targeting BCL-2. BP1002 silences BCL-2 expression by targeting the translation initiation site of Bcl-2 mRNA. Its backbone carries ethoxy modifications, which confer nuclease resistance, reduce off-target effects, and lower toxicity. BP1002 prolongs survival in non-Hodgkin's lymphoma xenograft models. BP1002 can be used in studies of acute myeloid leukemia, aggressive non-Hodgkin's lymphoma, and Venetoclax (HY-15531)-resistant hematological malignancies.

FI-700 is an orally active FLT3 inhibitor with an IC₅₀ of 20 nM. FI-700 induces G1 phase cell cycle arrest by inhibiting autophosphorylation of mutant FLT3 and the downstream STAT5/MAPK pathway. FI-700 triggers the mitochondrial apoptosis pathway by downregulating anti-apoptotic proteins Mcl-1 and Bcl-XL, altering the conformation of Bax, and activating caspase-3. FI-700 can be used in research related to acute myeloid leukemia.

Dihydrokaempferol (Standard) is the analytical standard of Dihydrokaempferol. This product is intended for research and analytical applications. Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic agents.

ASO-4625 is a 20-nucleotide gapmer antisense oligonucleotide with a full phosphorothioate backbone and 2'-O-(2-methoxy) ethyl ribose modifications, which targets BCL2 mRNA and BCL2L1 mRNA. ASO-4625 downregulates Bcl-2 expression via an RNase H-dependent antisense mechanism with 100% complementarity, and downregulates Bcl-xL expression via the same mechanism with three mismatches. ASO-4625 induces Apoptosis and acts as a chemosensitizer. ASO-4625 does not significantly modulate the expression of Bcl-W, survivin, Akt, or p53 mRNA. ASO-4625 can be used in studies of breast cancer and non-small cell lung cancer.

WAY-605337 (MLS-0073383) is a Bcl-B inhibitor, which can be used for structural modification and optimization of scaffolds.

Glufosfamide (Standard) is the analytical standard of Glufosfamide. This product is intended for research and analytical applications. Glufosfamide is a glucose-conjugated alkylating cytotoxic agent and a derivative of Ifosfamide (HY-17419). Glufosfamide induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in cancer cells. Glufosfamide shows great anti-tumor activity in MiaPaCa-2-RFP mouse model. Glufosfamide can be used for the study of hepatocellular carcinoma, prostate cancer and pancreatic carcinoma.

Maritoclax (Standard) is the analytical standard of Maritoclax. This product is intended for research and analytical applications. Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).