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AB287116

PF-3758309

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MW 490.6 Da, Purity >98%. A potent small molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. It binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.

View Alternative Names

39 kDa protein kinase, 5 AMP activated protein kinase alpha 1catalytic subunit, 5 AMP activated protein kinase catalytic alpha 1 chain, 5' AMP activated protein kinase gamma 1 subunit, 5' AMP activated protein kinase subunit gamma 1, 5''-AMP-activated protein kinase subunit gamma-1, 5''-AMP-activated protein kinase subunit gamma-2, 5'-AMP-activated protein kinase catalytic subunit alpha-1, 90 kDa ribosomal protein S6 kinase 6, AAKG, AAKG1_HUMAN, AAKG2_HUMAN, AAPK1_HUMAN, ACACA kinase, AI194361, AI450832, AL024255, AMP activated protein kinase noncatalytic gamma 1 subunit, AMP-activate kinase alpha 1 subunit, AMP-activated protein kinase, catalytic, alpha -1, AMPK, AMPK 1, AMPK alpha 1, AMPK alpha 1 chain, AMPK gamma 1 chain, AMPK gamma1, AMPK gamma2, AMPK subunit alpha-1, AMPK subunit gamma-1, AMPK subunit gamma-2, AMPKa1, AMPKg, Acetyl-CoA carboxylase kinase, Alpha-PAK, BMK 1 kinase, BMK-1, BTF2 p80, Basic transcription factor 2 80 kDa subunit, Beta PAK, Big MAP kinase 1, C130083N04Rik, CAK, CAK 1, CDK-activating kinase, CDK-activating kinase 1, CDK7_HUMAN, CDKN1A, CDKN7, CMH6, COFS 2, CXPD, Cell division protein kinase 7, Cyclin-dependent kinase 7, DNA excision repair protein ERCC-2, DNA repair protein complementing XP-D cells, EC 2.7.11.1, EC 2.7.11.24, EM9, ERCC2_HUMAN, ERK-1, ERK-2, ERK-4, ERT 2, ERT1, Excision repair 2, Excision repair cross complementing rodent repair deficiency complementation, Excision repair cross complementing rodent repair deficiency, complementation group 2, Extracellular signal-regulated kinase 1, Extracellular signal-regulated kinase 2, Extracellular signal-regulated kinase 5, Gamma-PAK, H91620p, HCAK, HMG CoA reductase kinase, HMGCR kinase, HS44KDAP, HUMKER1A, Homolog of Xenopus MO15 Cdk activating kinase, Hydroxymethylglutaryl-CoA reductase kinase, Insulin-stimulated MAP2 kinase, KIAA1142, KIAA126, KS6A6_HUMAN, Kinase subunit of CAK, MAP kinase 1, MAP kinase 2, MAP kinase 3, MAP kinase 7, MAP kinase isoform p42, MAP kinase isoform p44, MAPK 1, MAPK 7, MGC102762, MGC126218, MGC126219, MGC33776, MGC57364, MGC8666, MK01_HUMAN, MK07_HUMAN, MO15, MO15, Xenopus, homolog of, MRX30, MRX47, Microtubule-associated protein 2 kinase, Mitogen-activated protein kinase 1, Mitogen-activated protein kinase 2, Mitogen-activated protein kinase 3, Mitogen-activated protein kinase 7, OPHN3, OTTHUMP00000045860, OTTHUMP00000045861, OTTHUMP00000045862, OTTHUMP00000045863, OTTHUMP00000065906, OTTHUMP00000065907, OTTHUMP00000161795, OTTHUMP00000161796, Oligophrenin 3, P21 (CDKN1A) activated kinase 2, P21 (CDKN1A) activated kinase 3, P21 protein (Cdc42/Rac) activated kinase 1, P21 protein (Cdc42/Rac) activated kinase 3, P21/Cdc42/Rac1 activated kinase 1 (yeast Ste20 related), P38, P39 Mo15, P41, P58, PAK alpha, PAK3beta, PAK65, PAK7, PAKgamma, PRKAA 1, PRKAG 1, PRKM 2, PRKM 3, PRKM 7, PRKM1, PROTEIN KINASE, MITOGEN-ACTIVATED, 7, Prkag2, Protein kinase AMP activated alpha 1 catalytic subunit, Protein kinase AMP activated gamma 1 non catalytic subunit, Protein kinase AMP activated gamma 2 non catalytic subunit, Ribosomal S6 kinase 4, Ribosomal protein S6 kinase 90kDa polypeptide 6, Ribosomal protein S6 kinase alpha-6, S6/H4 kinase, S6K-alpha-6, SNF1-like protein AMPK, SNF1A, STE20 homolog, yeast, STK-1, Serine threonine kinase Stk1, Serine/threonine protein kinase 1, Serine/threonine protein kinase MO15, Serine/threonine protein kinase PAK 2, Serine/threonine protein kinase PAK 3, Serine/threonine-protein kinase PAK 1, Serine/threonine-protein kinase PAK 4, Serine/threonine-protein kinase PAK 6, Serine/threonine-protein kinase PAK 7, TFIIH 80 kDa subunit, TFIIH Basal Transcription Factor Complex Helicase Subunit, TFIIH basal transcription factor complex 80 kDa subunit, TFIIH basal transcription factor complex helicase XPD subunit, TFIIH basal transcription factor complex kinase subunit, TFIIH basal transcription factor complex p80 subunit, TFIIH p80, Tau-protein kinase PRKAA1, WPWS, XPDC, Xeroderma pigmentosum complementary group D, Xeroderma pigmentosum group D-complementing protein, bPAK, cb116, cyclin-dependent kinase 7 (MO15 homolog, Xenopus laevis, cdk-activating kinase), erk1/2, hPAK3, hormone sensitive lipase kinase, im:7154392, kinase AMPK alpha1, p21 activated kinase 3, p21 protein (Cdc42/Rac)-activated kinase 2, p21-activated kinase 1, p21-activated kinase 2, p21-activated kinase 4, p21-activated kinase 5, p21-activated kinase 6, p21-activated kinase 7, p21/Cdc42/Rac1-activated kinase 1 (STE20 homolog, yeast), p41mapk, p42-MAPK, p44-ERK1, p44-MAPK, p65-PAK, p90-RSK 6, pp90RSK4, protein kinase, AMP-activated, noncatalytic gamma-1, protein tyrosine kinase ERK2, rps6ka6, wu:fa94c10

Key facts

CAS number

898044-15-0

Purity

>98%

Form

Solid

form

Molecular weight

490.6 Da

Molecular formula

C<sub>2</sub><sub>5</sub>H<sub>3</sub><sub>0</sub>N<sub>8</sub>OS

PubChem

25227462

Nature

Synthetic

Solubility

Soluble to in DMSO to 10 mM

Biochemical name

N-((1S)-2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-((2-methylthieno(3,2-d)pyrimidin-4-yl)amino)-4,6-dihydropyrrolo(3,4-C)pyrazole-5(1H)-carboxamide

Biological description

A potent small molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. It binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.

Canonical smiles

CC1=NC2=C(C(=N1)NC3=NNC4=C3CN(C4(C)C)C(=O)NC(CN(C)C)C5=CC=CC=C5)SC=C2

Isomeric smiles

CC1=NC2=C(C(=N1)NC3=NNC4=C3CN(C4(C)C)C(=O)N[C@H](CN(C)C)C5=CC=CC=C5)SC=C2

InChi

InChI=1S/C25H30N8OS/c1-15-26-18-11-12-35-20(18)23(27-15)29-22-17-13-33(25(2,3)21(17)30-31-22)24(34)28-19(14-32(4)5)16-9-7-6-8-10-16/h6-12,19H,13-14H2,1-5H3,(H,28,34)(H2,26,27,29,30,31)/t19-/m1/s1

InChiKey

AYCPARAPKDAOEN-LJQANCHMSA-N

IUPAC Name

N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide

Product details

This product is manufactured by BioVision, an Abcam company and was previously called B2634 PF-3758309. B2634-25 is the same size as the 25 mg size of ab287116.

Properties and storage information

Shipped at conditions
Blue Ice
Appropriate long-term storage conditions
-20°C
Storage information
Store in the dark
Handling instructions

Need more advice on solubility, usage and handling? Please visit our our product support page for more details.

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Toxic, refer to SDS for further information.

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Cyclin-dependent kinase 7 (Cdk7) xeroderma pigmentosum group D protein (XPD) p21 activated kinases 1 2 and 3 (PAK1 PAK2 PAK3) and AMP-activated protein kinase alpha 1 (AMPK alpha 1) are all proteins with specific roles in cellular processes. Cdk7 is a 40-50 kDa protein involved in cell cycle control and transcription regulation. It often functions in complex with other proteins. PAK family proteins like PAK1 PAK2 and PAK3 are serine/threonine kinases that modulate various signaling pathways with PAK1 being highly expressed in the brain and muscles. AMP-activated protein kinase (AMPK) alpha 1 is an important energy sensor that regulates cellular energy homeostasis and it is expressed in various tissues especially liver and muscle.
Biological function summary

These proteins have essential roles in their respective cellular contexts. Cdk7 associates with other cyclin-dependent kinases functioning in the transcription preinitiation complex and regulating the cell cycle. XPD participates in nucleotide excision repair due to its helicase activity important for correcting DNA damage. PAKs modulate cytoskeletal dynamics cell motility and apoptosis. AMPK alpha 1 serves as a metabolic switch responding to ATP levels and activating pathways for energy production. Both ERK1 (44 kDa) and ERK2 (42 kDa) also known as MAPK3 and MAPK1 respectively are involved in transmitting signals from the cell membrane to the nucleus playing a part in cell division and differentiation.

Pathways

These proteins integrate into complex networks. Cdk7 is part of the CAK (CDK-activating kinase) complex influencing the cyclin-CDK complex activity in cell cycle regulation. It also interacts with factors like TFIID in transcription. AMPK alpha 1 plays a significant role in the AMPK pathway which is critical for energy balance and interacts with mTOR signaling. PAK1 through PAK6 regulates the MAPK/ERK signaling pathway influencing cellular responses to growth signals. ERK1 and ERK2 belong to the MAPK pathway activated by MEK kinases affecting functions from proliferation to survival.

These proteins link to various pathologies. PAK1 consistently shows a connection with cancer progression due to its role in promoting cell motility and survival. Overexpression or mutations in Cdk7 are often observed in aggressive forms of cancer making it a potential therapeutic target. AMPK alpha 1 is linked to metabolic disorders such as obesity and type 2 diabetes due to its regulatory role in energy balance. ERK1 and ERK2 through aberrant activation have associations with cancer due to promoting abnormal cell cycles and proliferation. Understanding these proteins and their pathways helps in targeting diseases where they play a role.

Product protocols

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