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haematological malignancies

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By Targets:	Apoptosis (2) Btk (3) Casein Kinase (4) PI3K (4) PKA (1) Platelet-activating Factor Receptor (PAFR) (1)
By Research Areas:	Cancer (9) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (1)

9

Inhibitors & Agonists

1

Inhibitory Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

KT5720 3 Publications Verification	PKA	Neurological Disease Cancer
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC₅₀=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 ⁺ concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .

Umbralisib 3 Publications Verification TGR-1202; RP5264	PI3K Casein Kinase	Cancer
Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC₅₀ of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach .

Umbralisib hydrochloride 3 Publications Verification TGR-1202 hydrochloride; RP5264 hydrochloride	PI3K Casein Kinase	Cancer
Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC₅₀ of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach .

Umbralisib sulfate TGR-1202 sulfate; RP-5264 sulfate	PI3K Casein Kinase	Cancer
Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC₅₀ of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach .

Umbralisib tosylate TGR-1202 tosylate; RP5264 tosylate	PI3K Casein Kinase	Cancer
Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC₅₀ of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach .

Ibrutinib-MPEA	Btk	Cancer
Ibrutinib-MPEA (Compound 20) is ibrutinib derivative. Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) that has been used to treat haematological malignancies .

SDZ-62-434	Platelet-activating Factor Receptor (PAFR)	Metabolic Disease
SDZ-62-434 is a platelet-activating factor (PAF) antagonist. SDZ-62-434 has antiproliferative activity in human solid and haematological malignancies .

Tirabrutinib hydrochloride 3 Publications Verification ONO-4059 hydrochloride; GS-4059 hydrochloride	Btk Apoptosis	Inflammation/Immunology Cancer
Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC₅₀ of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies .

Tirabrutinib 3 Publications Verification ONO-4059; GS-4059	Btk Apoptosis	Inflammation/Immunology Cancer
Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC₅₀ of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies .

Cat. No.	Product Name	Target	Research Area

ATG-031 1 Publications Verification	Inhibitory Antibodies	Cancer
ATG-031 is a humanised anti-CD24 monoclonal antibody. ATG-031 effectively stimulates macrophage-mediated phagocytosis and induces cancer cell destruction by blocking the "don't eat me" signals that characterize the growth of many cancers. ATG-031 can be used in the study of haematological malignancies as well as solid tumours.

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