Bcl-2 Inhibitor

Gossypol acetic acid ((±)-Gossypol-acetic acid) binds to Bcl-xL protein and Bcl-2 protein with K_is of 0.5-0.6 μM and 0.2-0.3 mM, respectively.

GM-90257 is a microtubule acetylation inhibitor. GM-90257 binds directly to α-tubulin. GM-90257 prevents the recruitment of α-tubulin acetyltransferase 1 (αTAT1) to the K40 residue in α-tubulin. GM-90257 causes Apoptosis, downregulates BCl-2, and activates JNK and PARP. GM-90257 has anticancer activity against breast cancer.

Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.

Ganoderma Lucidum/Reishi Extract is a Ganoderma lucidum extract. Ganoderma Lucidum/Reishi Extract reduces the expression of c-Myc, BCL-2, BCL-XL, TERT, PDGFB, eIF4G, Survivin, β-catenin, and eIF4E. Ganoderma Lucidum/Reishi Extract downregulates the gene expression of MMP-9. Ganoderma Lucidum/Reishi Extract upregulates the expression of IL8. Ganoderma Lucidum/Reishi Extract is applicable to the research of inflammatory breast cancer. Ganoderma Lucidum is used in the research of various diseases, such as allergy, arthritis, hypertension, neurasthenia, inflammation, and cancer.

S55746 (BCL201) is a potent, orally active and selective BCL-2 inhibitor, with a K_i of 1.3 nM and a K_d of 3.9 nM. S55746 (BCL201) has antitumor activity with low toxicity.

IGF2BP1-IN-1, a Cucurbitacin B (HY-N0416) derivative, is a potent IGF2BP1 inhibitor (K_D = 2.88 nM). IGF2BP1-IN-1 binds directly to IGF2BP1, thereby inducing tumor cell cycle arrest, increasing apoptosis, and reducing autophagy. IGF2BP1-IN-1 can be used in research on NSLSC, colon, breast, liver, ovarian, pancreatic, and cervical cancers.

PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC₅₀, 4.94 μM; DC₅₀, 3.0 μM) and Mcl-1 (IC₅₀, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.

Poly-L-lysine hydrobromide (MW 30000-70000) is a water-soluble synthetic polypeptide. Poly-L-lysine hydrobromide (MW 30000-70000) downregulates Bcl-2 and upregulates Bax and p53 proteins. Poly-L-lysine hydrobromide (MW 30000-70000) promotes Apoptosis and reduces VEGF expression. Poly-L-lysine hydrobromide (MW 30000-70000) shows anticancer activity against a variety of tumors. Poly-L-lysine hydrobromide (MW 30000-70000) can also be used as a coating material.

PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC₅₀ of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC₅₀ of 0.54 μM.

TW-37 is a potent Bcl-2 inhibitor with K_i values of 260, 290 and 1110 nM for Mcl-1, Bcl-2 and Bcl-xL, respectively.

(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with K_is of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.

Sorafenib (Standard) (Bay 43-9006 (Standard)) is the analytical standard of Sorafenib (HY-10201). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

Sabutoclax is a potent and effective Bcl-2 Family (Bcl-2, Bcl-XL, Mcl-1, Bfl-1) inhibitor with IC₅₀s of 0.32 μM, 0.31 μM, 0.20 μM, and 0.62 μM, respectively. Sabutoclax increases Bax, Bim, PUMA and survivin expression.

Daphnoretin (Dephnoretin; Thymelol) is a protein kinase C (PKC) activator that inhibits the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and exhibits antiviral activity. Daphnoretin exerts its antitumor effects by inhibiting the activation of the PI3K/AKT signaling pathway and triggers the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and activation of the NLRP3 inflammasome. Daphnoretin regulates the differentiation and maturation of dendritic cells, inhibits their immunostimulatory function by downregulating the phosphorylation level of JNK, and thus exerts a protective effect in skin graft rejection.

Secoxyloganin is an orally effective iridoid derivative. Secoxyloganin can be isolated from the flower buds of L. japonica. Secoxyloganin induces Apoptosis by inhibiting the expression of Bcl-2. Secoxyloganin potently inhibits the proliferation of breast cancer cells, while exerting weak activity against normal mammary epithelial cells. Secoxyloganin inhibits the decrease in tail vein blood flow associated with allergic reactions.

BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a K_i of 2.4±0.2 μM in FP assay. BH3I-1 has a K_d of 5.3 μM against the p53/MDM2 pair.

MCL-1/BCL-2-IN-2 is a Mcl-1 and Bcl-2 inhibitor with IC₅₀ values of 5.4 and 7.66 μM. MCL-1/BCL-2-IN-2 is applicable to the research of Mcl-1-dependent cancers.

(S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.

3-Methylxanthine is a blood-brain barrier-permeable cyclic GMP phosphodiesterase inhibitor, with an IC₅₀ of 920 μM against guinea pig cyclic GMP phosphodiesterase. 3-Methylxanthine relaxes the spontaneous tension of isolated guinea pig tracheal smooth muscle preparations. Through a DRD1-dependent pathway, 3-Methylxanthine upregulates the expression of γH2AX and activated caspase-3, downregulates the expression of Bcl-2, and enhances Cisplatin-induced apoptosis (apoptosis) in ovarian cancer cells both in vitro and in vivo. 3-Methylxanthine induces clonic convulsions in the central nervous system. 3-Methylxanthine is the major metabolite of Theophylline (HY-B0809). 3-Methylxanthine can be used in studies related to ovarian cancer and neurotoxic convulsions.

HA14-1 is a Bcl-2/Bcl-X_L antagonist. HA14-1 binds the designated pocket on Bcl-2 with the IC₅₀ of ≈9 μM in competing with the Bcl-2 binding of Flu-BakBH3, and inhibits its function.