TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity[1].
4'-Bromo-resveratrol is a potent and dual inhibitor Sirtuin-1 and Sirtuin-3. 4'-Bromo-resveratrol inhibits melanoma cell growth through mitochondrial metabolic reprogramming. 4'-Bromo-resveratrol imparts antiproliferative effects in melanoma cells through a metabolic reprogramming and affecting the cell cycle and apoptosis signaling[1].
PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer[1].
DHX9-IN-1 is an inhibitor of ATP-dependent RNA helicase A (DHX9), with the IC50 of 9.45 nM that has antitumor activity[1].
7,15-Dihydroxy-4,4,14-trimethyl-3,11-dioxochol-8-en-24-oic acid is one of the ganoderma triterpenoids which have been recognised as an important bioactive ingredient in Ganoderma Lucidum Karst. and can be used for the research of various etiologies[1][2].
Cdc7-IN-19 (compound 1-1) is a potent CDC7 inhibitor with an IC50 of 1.49 nM[1].
LGnRH-III, lamprey, an isoform of GnRH isolated from the sea lamprey, is a weak GnRH agonist with antitumor activities[1][2].
Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity[1][2][3].
Zilurgisertib is a selective ALK 2 inhibitor for treating diseases such as cancer.
RLY-2608 is a first-in-class allosteric mutant-selective inhibitor of PI3Ka[1].
Istiratumab (M-6495) is bispecific monoclonal antibody targeting IGF-1R and ErbB3. Istiratumab induces IGF-1R and ErbB3 receptor degradation through the proteasome pathway Istiratumab can be used for research of cancers[1][2][3].
W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway[1].
YAP-TEAD-IN-3 (compound 155) is a YAP/TAZ-TEAD inhibitor. YAP-TEAD-IN-3 inhibits Avi-humanTEAD4217-434 with an IC50 value of 9 nM. YAP-TEAD-IN-3 also inhibits NCI-H2052 with an GI50 of 0.048 μM (cell proliferation)，and an IC50 of 0.048 μM (YAP reporter gene expression)，respsectively[1].
Mal-PEG24-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Metoprolol fumarate (CGP 2175C) is an orally active, selective β1-adrenoceptor antagonist. Metoprolol fumarate shows anti-inflammation, antitumor and anti-angiogenic properties[1][2][3].
Fmoc-PEG4-GGFG-CH2-O-CH2-Cbz is a cleavable ADC linker containing 4 units of PEG, which can be used to synthesize active antibody conjugation molecules (ADC)[1].
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research[1].
HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has inhibitory activity against pre-miR-21 RNA. HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has the potential for the research of neoplastic disease such as cancer and especially cancers expressing miR-21 (extracted from patent WO2021087084A1, compound 25)[1].
ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4)[1].
Inuviscolide is an apoptosis inducer. Inuviscolide can induce of G2/M arrest in human melanoma cell lines. Inuviscolide exhibits antineoplastic and anti-inflammatory activities[1][2][3].
EGFR-IN-54 (Compound 3c) is a potent EGFR inhibitor with an IC50 of 1.623 µM. EGFR-IN-54 shows cytotoxic activity against cancer cell lines[1].
HaloPROTAC-E is a novel HaloPROTAC potent degrader, inducing reversible degradation of two endosomally localized proteins, SGK3 and VPS34, with a DC50 of 3-10 nM, remarkably selective inducing only degradation of the Halo tagged endogenous VPS34 complex (VPS34, VPS15, Beclin1, and ATG14).
Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
3'-Demethylnobiletin, a derivative of Nobiletin, is a polymethoxyflavonoid in citrus fruits[1]. Nobiletin exhibits anticancer activity and inhibits tumor angiogenesis by regulating Src, FAK, and STAT3 signaling[2].
Methylnitronitrosoguanidine (MNNG) is an alkylating agent with toxic and mutagenic effects[1].
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells[1][2][3].
SCAL-266 is a potent mitochondrial complex I (CI) inhibitor with IC50 of 0.83 μM. SCAL-266 blocks mitochondrial function, inhibits OCR, induces ROS production, and reduces MMP. SCAL-266 displays a considerable antiproliferation effect against oxidative phosphorylation (OXPHOS)-dependent cancer cells[1].
DUBs-IN-2 is a potent deubiquitinase inhibitor with an IC50 of 0.28 μM for USP8.
J1-1 is an inhibitor of ICMT with an IC50 of 1.0 μM and has anticancer activity[1].
5-(2,3,5-Tri-O-benzyl-beta-D-ribofuranosyl)-3-methyl-2-benzyloxypyridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].