1. JAK/STAT Signaling
  2. Pim
  3. PIM1-IN-1

PIM1-IN-1 

Cat. No.: HY-111552
Handling Instructions

PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.

For research use only. We do not sell to patients.

PIM1-IN-1 Chemical Structure

PIM1-IN-1 Chemical Structure

CAS No. : 1417630-95-5

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Description

PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity[1].

IC50 & Target[1]

PIM1

7 nM (IC50)

PIM3

70 nM (IC50)

PIM2

5530 nM (IC50)

In Vitro

PIM1-IN-1 (Compound 42) exhibits antiproliferative activity, with GI50 of 1.48 µM for melanoma cell line SKMEL-19. PIM1-IN-1 has significant synergistic effect combined with different antitumoral agents in different tumor cell lines[1].
PIM1-IN-1 (2.5, 5, or 10 µM, 24 hours) induces apoptosis in SKMEL19 cells[1].

Apoptosis Analysis[1]

Cell Line: SKMEL19 cells
Concentration: 2.5, 5, or 10 µM
Incubation Time: 24 hours
Result: Regulated cell cycle, induced cell apopsis in SKMEL19 cells.
In Vivo

PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice[1].

Molecular Weight

474.56

Formula

C₂₅H₃₀N₈O₂

CAS No.

1417630-95-5

SMILES

COCCN1C2=C(C3=NN=C(C4=NC5=C(NCC6CCNCC6)C=CC=C5C=C4)N3N=C2)OCC1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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PIM1-IN-1
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