Signaling Pathway

Pim

Pim

Related Products

PDF File 0.26MB

Pim kinases are a small family of serine/threonine kinases regulating several signaling pathways that are fundamental to cancer development and progression. They were first recognized as pro-viral integration sites for the Moloney Murine Leukemia virus. Pim kinases possess a hinge region which creates a unique binding pocket for ATP. Absence of a regulatory domain means that these proteins are constitutively active once transcribed. Pim kinases are critical downstream effectors of the ABL (ableson), JAK2 (janus kinase 2), and Flt-3 (FMS related tyrosine kinase 1) oncogenes and are required by them to drive tumorigenesis. Recent investigations have established that the Pim kinases function as effective inhibitors of apoptosis and when overexpressed, produce resistance to the mTOR (mammalian target of rapamycin) inhibitor, rapamycin . Overexpression of the PIM kinases has been reported in several hematological and solid tumors (PIM 1), myeloma, lymphoma, leukemia (PIM 2) and adenocarcinomas (PIM 3). As such, the Pim kinases are a very attractive target for pharmacological inhibition in cancer therapy. Novel small molecule inhibitors of the human Pim kinases have been designed and are currently undergoing preclinical evaluation.

Pim Inhibitors & Modulators (14)

Product Name Catalog No. Brief Description
(1S,3R,5R)-PIM447 dihydrochloride

HY-19322C

(1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.

(Z)-SMI-4a

HY-16576A

(Z)-SMI-4a is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM for Pim-1 compared to an IC50 of 100 nM for Pim-2 and with little or no activity against a panel of 50 other kinases tested.

AZD1208

HY-15604

AZD1208 is a novel, orally bioavailable, highly selective PIM kinases inhibitor with single nanomolar potency against all three PIM kinases and is currently undergoing Phase I testing and dose escalation studies in AML.

CX-6258

HY-18095

CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.

CX-6258 hydrochloride hydrate

HY-18095A

CX-6258 hydrochloride hydrate is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.

GDC-0339

HY-16976

GDC-0339 is a Pim kinase inhibitor with IC50 of 43.6 nM for BaF3 PIM1.

M-110

HY-12830

M-110 is a novel and highly selective inhibitor of PIM kinases; inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 uM, with no activity on normal human peripheral blood mononuclear cells up to 40 uM.

PIM-447 dihydrochloride

HY-19322B

PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.

Pim1 AKK1-IN-1

HY-10371

PIM/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively; also inhibits MPSK1 and TNIK.

PIM447

HY-19322

PIM447 is novel pan-PIM kinase inhibitor, including  Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.

SGI-1776

HY-13287

SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM; 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin.

TCS PIM-1 1

HY-18086

TCS PIM-1 1(sc-204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).

TCS-PIM-1-4a

HY-16576

TCS-PIM-1-4a is a Pim inhibitor that blocks mTORC1 activity via activation of AMPK; kills a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 μM).

TP-3654

HY-101126

TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.