hematopoietic

16,16-Dimethyl prostaglandin E2 is an orally active vertebrate Hematopoietic stem cells homeostasis critical regulator. It can act through EP2/EP4 and has an interaction with the Wnt pathway.

DB1976 dihydrochloride (DB1976 2HCl) , a transcription factor PU.1 inhibitor with potential anti-inflammatory activity, slowed down inflammation and fibrosis and improved glucose homeostasis and dyslipidemia in mice in in vivo experiments.DB1976 dihydrochloride promotes apoptosis and may be used in studies of metabolic dysfunction and non-alcoholic steatohepatitis.

Rezafungin acetate (Biafungin acetate) is a echinocandin with antimicrobial activity that inhibits 1,3-β-D-glucan synthase. It can be used for research on invasive fungal diseases in hematopoietic and bone marrow transplant recipients.

CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpressed CDK6.

HQL-79 is a selective and orally active human hematopoietic prostaglandin D synthase (H-PGDS) inhibitor. It inhibits the synthesis of PGD2 and acts as an anti-allergic agent (Kd: 0.8 μM and IC50: 6 μM). It also shows no obvious effect on COX-1, COX-2, m-P

PYZD-4409 is a selective UBA1 inhibitor with an IC50 of 20 μM. PYZD-4409 induces cell death in malignant cells and is preferentially cytotoxic to malignant cells over normal hematopoietic cells.

HPGDS inhibitor 1 is a novel and selective inhibitor for Hematopoietic Prostaglandin D Synthase (HPGDS) with an IC50 Value of 0.7 nM.

SGD-1882 (PBD dimer) is a cytotoxic conjugate that is a target for mouse and human hematopoietic stem cells (HSC) and acute myeloid leukemia cells.

TETi76 is an orally active inhibitor from the TET family, demonstrating IC50 values of 1.5, 9.4, and 8.8 μM against TET1, TET2, and TET3, respectively. The compound competitively binds to the active sites of TET enzymes, reducing cytosine hydroxymethylation and restricting clonal growth in mutated TET2 in vitro and in vivo, without affecting the growth of normal hematopoietic progenitor cells. TETi76 is utilized in leukemia research.

HPK1-IN-52 is an effective orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor, displaying anti-tumor activity with an IC50 value of 10.4 nM.

Burixafor (also known as TG-0054) is an orally available inhibitor of the CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell mobilization activities. By binding to the CXCR4 chemokine receptor, Burixafor blocks the binding and subsequent activation of stromal cell-derived factor-1 (SDF-1 or CXCL12) with the CXCR4 receptor, potentially facilitating the mobilization of hematopoietic stem and progenitor cells from the bone marrow into the bloodstream. Note: Elemental analysis shows that this compound is a salt containing 3 HBr and 3 water molecules.

PF-07265028 is an HPK1 inhibitor with an IC50 of 17 nM. Pharmacokinetic studies in mice and monkeys indicate that PF-07265028 exhibits moderate clearance, terminal half-life, volume of distribution, and oral bioavailability. It targets, binds, and inhibits Hpk1 activity, blocking Hpk1-mediated signaling pathways to prevent immune suppression mediated by Hpk1, including the inhibition of T-cell receptor (TCR) signaling, effector T-cell suppression, aberrant cytokine expression, and the elimination of the immunosuppressive tumor microenvironment (TME). This action can activate a cytotoxic T lymphocyte (CTL)-mediated immune response against tumor cells. Hpk1 is primarily expressed in hematopoietic cells and acts as a negative regulator of TCR signaling and T and B cell activation.

HPK1-IN-54 (Compound 16) is a potent inhibitor of HPK1 (hematopoietic progenitor kinase 1), enhancing T cell activation and proliferation by blocking HPK1 activity to exert antitumor effects. It has an IC50 of 2.67 nM for HPK1, showing excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 exhibits moderate in vivo clearance and reasonable oral exposure in both mice and rats. Additionally, in the CT26 mouse colon cancer model, HPK1-IN-54 demonstrates significant antitumor activity and shows a synergistic effect when combined with anti-PD-1 therapy. HPK1-IN-54 holds promise for research in the field of immunology.

HPK1-IN-55 (compound 19) is a selective and orally active inhibitor of hematopoietic progenitor kinase 1 (HPK1) with an IC50 of less than 0.51 nM. It exhibits exceptional kinase selectivity, being over 637 times more selective for HPK1 compared to GCK kinase and over 1022 times compared to LCK. HPK1-IN-55 possesses anti-cancer properties.

CRX 527 is a TLR4 ligand and serves as an adjuvant for peptide cancer vaccines, enhancing anti-tumor immune responses. CRX 527 also induces hematopoietic stem cell (HSC) differentiation, increasing the proportion and number of LSK cells, and promotes their differentiation into macrophages. This activation bolsters immune defense and protects intestinal epithelium from radiation damage.