PARP1/ERK IN-1 is a dual PARP1/ERK inhibitor, with a PARP1 IC50 of 0.9 nM and an ERK2 IC50 of 1.8 nM. PARP1/ERK IN-1 inhibits proliferation and migration of various cancer cell lines, and induces apoptosis and DNA damage. PARP1/ERK IN-1 suppresses tumor growth in mouse models of colorectal cancer, and reduces the expression of Ki‑67, BRCA1 and Rad51. PARP1/ERK IN-1 can be used in the research of colorectal cancer, triple-negative breast cancer and pancreatic cancer.

MAP3K14-IN-1 (Compound 173) is a MAP3K14 (NIK kinase) inhibitor with an IC50 of 1.8 nM. MAP3K14-IN-1 inhibits the autophosphorylation of MAP3K14 kinase. MAP3K14-IN-1 reduces the level of phosphorylated IKKα in cancer cells. MAP3K14-IN-1 inhibits the proliferation of multiple myeloma cells. MAP3K14-IN-1 can be used in research related to multiple myeloma.

LY 300168 (GYKI 53655) is a non-competitive, blood-brain-barrier permeable AMPA receptor antagonist. LY 300168 attenuates hippocampal injury. LY 300168 blocks the sound-induced clonic and tonic convulsions.

ERRγ-IN-1 is a ERRγ inhibitor with an IC50 of 0.040 μM. ERRγ-IN-1 activates MAPK (p44/p42) and inhibits the activity of ERRγ. ERRγ-IN-1 significantly increases iodine uptake in anaplastic thyroid carcinoma xenografts and suppresses tumor growth in nude mice. ERRγ-IN-1 is applicable for the research of anaplastic thyroid carcinoma.

FG-0041 (FG0041) is a small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 of 2 uM for collagen prolyl hydroxylase.

Davotifan (Compound A17) is a bicyclic compound. Davotifan is an inhibitor of HIF-2α. Davotifan can be studied in research for HIF-2α-related cancer.

Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1).

ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases.

Octyl-α-ketoglutarate (1-Octyl 2-oxopentanedioate) is a stable, cell-permeable form of α-ketoglutarate which accumulates rapidly in HEK293 cells with a dysfunctional tricarboxylic acid (TCA) cycle, stimulating prolyl hydroxylase (PHD) activity. In addition, Octyl-α-ketoglutarate competitively blocks succinate- or fumarate-mediated inhibition of PHD.

LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model.

JPHM-2-167 (Compound 11) is a selective PHD (prolyl hydroxylase domain enzyme) inhibitor. JPHM-2-167 inhibits PHD2, PHD3 with IC50s of 0.253 μM and 3.95 μM, respectively. JPHM-2-167 can be used for chronic kidney disease .

DDO-3055 is an orally active PHD2 inhibitor that can be used in the research of anemia associated with chronic kidney disease.

1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH).

HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing.

MO-2097 is a small molecule hnRNPA2B1-binding compound (ITC KD=43.1 uM) that suppresses hnRNPA2B1-induced HIF-1α protein expression under hypoxic and mimetic hypoxia.

ER-400583-00 is a small-molecule HIF-1α inhibitor, inhibits the induction of HIF-1 reporter activity in response to hypoxia with IC50 of 7.9 nM.

PX-478 is an inhibitor of HIF-1a with an IC50 of 20-30μM enhances radiosensitivity of prostate carcinoma cells.

Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay). PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells. PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d.

PT2385 is an orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha, with potential antineoplastic activity.

Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.

KC7F2 is a potent HIF-1 pathway inhibitor and that its potential as a cancer therapy agent warrants further study.

Hypoxia-inducible factor prolyl hydroxylase inhibitor

FG-4592 is an HIF αprolyl hydroxylase inhibitor, stabilizes HIF-2 and induces EPO production.

Daprodustat(GSK1278863) isa HIF-prolyl hydroxylase inhibitor.

2-methoxyestradiol (2ME2; NSC-659853) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 ± 0.11 μM for the inhibition of BPAEC migration.

Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.

Zifcasiran is a hypoxia-inducible factor (HIF) synthesis reducer. Zifcasiran shows antitumor activities and can be used in advanced renal cell carcinoma research.

Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects.

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.

BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor.