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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.

Cat. No.	Product Name	CAS No.	Information
H9074	Ser99 inhibitor NPB	2247491-97-8	Ser99 inhibitor NPB is a novel small molecule which inhibits BAD phosphorylation specifically at Ser99 has been shown to be effective in inducing apoptosis and reducing cell viability in various human cancer cell lines, as well as in inhibiting tumor growth in mammary carcinoma xenograft models.Ser99 inhibitor NPB was found to be the most potent with the IC50 of 6.5 μM.
H4223	YLT-11		YLT-11 (PLK4 inhibitor YLT11) is a novel potent, selective, ATP-competitive PLK4 inhibitor with IC50 of 22 nM, Kd of 5.2 nM; displays good selectivity over other PIMs and a panel of mitotic kinases, including JNK, TOPK, ERK, and so on; significantly decreases the viability of different subtypes of breast cancer cells with IC50 of 68-120 nM (MDA-MB-231, MDA-MB-468, BT549, and MCF-7 cells), also potently suppresses the DNA replication of cancer cells; significantly suppresses the tumor growth in human breast cancer xenograft models, orally active.
H4222	VS-II-173	1627962-21-3	VS-II-173 is a highly potent Pim1 and Pim3 inhibitor with IC50 of 70 and 20 nM respectively, and a potent and selective inducer of AML cell death (IC50=5.5 uM, Molm-13 cell); acts synergistically with the anthracycline daunorubicin, and additively with a number of other anti-cancer drugs; attenuates phosphorylation of Pim kinase substrates, shows towards cell lines harboring the FLT3-ITD mutation (Molm-13, FLT3-ITD heterozygous and MV4-11 FLT3-ITD homozygous) with EC50 of 2-3 uM; also induces cell death also in AML patient blasts, including blast carrying high-risk FLT3-ITD mutation.
H4221	TP-3654	1361951-15-6	A potent, selective, orally active second-generation PIM inhibitor with Ki of 5, 42 and 239 nM for Pim1, 2 and 3, respectively; exhibits submicromolar activity in UM-UC-3 bladder cancer cell line; displays favorabl hERG and CYP450 inhibition profiles compared with SGI-1776, reduces tumor growth in vivo xenografts.
H4220	TCS PIM-1 1	491871-58-0	A potent, selective, ATP-competitive Pim-1 kinase inhibitor with IC50 of 50 nM; displays >400-fold selectivity over Pim-2 and MEK1/2.
H4219	SGI-1776	1025065-69-3	SGI-1776 is a potent, selective, orally active Pim kinase inhibitor with IC50 of 7, 363 and 69 nM for Pim1, Pim2 and Pim3, respectively; exhibits promising selectivity against a panel of >300 kinases, shows inhibitory activity against two other kinases: Flt-3 (IC50=44 nM) and Haspin (IC50=34 nM); reduces cell viability of androgen-independent prostate cancer cell lines with IC50 of 2-4 uM, causes cell cycle arrest and caspase-dependent apoptosis in prostate cancer cells, marginally sensitizes prostate cancer cells to taxane-based therapeutics by inhibiting MDR1 activity and inducing apoptosis; shows efficacy in xenograft model bearing MV-4-11 tumors.
H4218	SEL24-B489 hydrochloride		SEL24-B489 (SEL24) is a potent, dual PIM and FLT3-ITD inhibitor with Kd of 2/2/3 nM for PIM1/2/3, Kd of 160/16 nM for FLT3-WT/FLT3-ITD, respectively; exhibits significantly broader on-target activity in AML cell lines (MV-4-11 GI50=20 nM) and primary AML blasts than selective FLT3-ITD or PIM inhibitors, decreases viability of AML cells with FLT3-TKD mutations associated with resistance to selective FLT3-ITD inhibitors; inhibits the growth of a broad panel of AML cell lines in xenograft models.
H4217	SEL24-B489	1616359-00-2	SEL24-B489 (SEL24) is a potent, dual PIM and FLT3-ITD inhibitor with Kd of 2/2/3 nM for PIM1/2/3, Kd of 160/16 nM for FLT3-WT/FLT3-ITD, respectively; exhibits significantly broader on-target activity in AML cell lines (MV-4-11 GI50=20 nM) and primary AML blasts than selective FLT3-ITD or PIM inhibitors, decreases viability of AML cells with FLT3-TKD mutations associated with resistance to selective FLT3-ITD inhibitors; inhibits the growth of a broad panel of AML cell lines in xenograft models.
H4216	Pim1/AKK1-IN-1	1093222-27-5	A potent, multikinase inhibitor with Kd of 35/53/75/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
H4215	Pim-IN-22m	1405126-60-4	Pim-IN-22m is a potent, selective Pim1/Pim2 inhibitor with IC50 of 24/95 pM respectively; potently inhibits the phosphorylation of BAD (s112) in a cell line that expresses high levels of all Pim isoforms, KMS-12-BM (IC50=28 nM).

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