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MedKoo Cat#: 523116 | Name: PF-06260933 HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PF-06260933 dihydrochloride is a MAP4K4 (HGK) inhibitor (IC50 = 140 nM). It also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). PF-06260933 dihydrochloride has been shown to improves fasting hyperglycemia in mice. (

Chemical Structure

PF-06260933 HCl
CAS#1883548-86-4 (2HCl)

Theoretical Analysis

MedKoo Cat#: 523116

Name: PF-06260933 HCl

CAS#: 1883548-86-4 (2HCl)

Chemical Formula: C16H15Cl3N4

Exact Mass: 0.0000

Molecular Weight: 369.67

Elemental Analysis: C, 51.99; H, 4.09; Cl, 28.77; N, 15.16

Price and Availability

Size Price Availability Quantity
5mg USD 195.00
25mg USD 575.00
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Related CAS #
1883548-86-4 (2HCl) 1811510-56-1 (free base) 2118243-34-6 (HCl)
Synonym
PF-06260933 dihydrochloride; PF06260933 HCl; PF06260933; PF 06260933; PF-06260933; PF6260933; PF 6260933; PF-6260933;
IUPAC/Chemical Name
5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine dihydrochloride
InChi Key
VRQXEOPUAQLBQI-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H13ClN4.2ClH/c17-13-4-1-10(2-5-13)14-7-12(9-21-16(14)19)11-3-6-15(18)20-8-11;;/h1-9H,(H2,18,20)(H2,19,21);2*1H
SMILES Code
NC1=CC=C(C2=CC(C3=CC=C(Cl)C=C3)=C(N)N=C2)C=N1.[H]Cl.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PF-06260933 dihydrochloride is a MAP4K4 (HGK) inhibitor (IC50 = 140 nM).
In vitro activity:
To optimize the hydrogen bond with Asp115, compound 16 (PF-06260933) was prepared, as modeling indicated that the NH2 group of the newly introduced aminopyridine group interacts with Asp115 in a similar fashion as the phenol OH in 13. Compound 16 (PF-6260933) was very potent against the enzyme with a very good ligand efficiency (LE = 0.57) and was the most potent analogue in the cell assay. Indeed, compound 16 showed a kinase activity IC50 (tested at Km) of 15 and 8 nM for TNIK and MINK, respectively. Reference: ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. https://pubmed.ncbi.nlm.nih.gov/26617966/
In vivo activity:
The model mice were assigned to four groups: MAP4K4 recombinant protein, scramble small interfering RNA, and MAP4K4 small interfering RNA were delivered by intracerebroventricular injection, while PF-06260933, a small-molecule inhibitor of MAP4K4, was administrated orally. Furthermore, administration of the MAP4K4 inhibitor PF-06260933 reduced blood-brain barrier damage in mice, promoted the recovery of neurological function, and reduced p-p65 and MMP9 protein expression. Reference: Neural Regen Res. 2021 Feb;16(2):325-332. https://pubmed.ncbi.nlm.nih.gov/32859792/
Solvent mg/mL mM comments
Solubility
DMSO 7.4 20.00
Water 37.0 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 369.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Zou Z, Dong YS, Liu DD, Li G, Hao GZ, Gao X, Pan PY, Liang GB. MAP4K4 induces early blood-brain barrier damage in a murine subarachnoid hemorrhage model. Neural Regen Res. 2021 Feb;16(2):325-332. doi: 10.4103/1673-5374.290904. PMID: 32859792; PMCID: PMC7896238. 2. Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Carlo AA, Conrad R, Cortes C, Dow RL, Dowling MS, El-Kattan A, Ford K, Guimarães CR, Hepworth D, Jiao W, LaPerle J, Liu S, Londregan A, Loria PM, Mathiowetz AM, Munchhof M, Orr ST, Petersen DN, Price DA, Skoura A, Smith AC, Wang J. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. doi: 10.1021/acsmedchemlett.5b00215. PMID: 26617966; PMCID: PMC4645242.
In vitro protocol:
1. Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Carlo AA, Conrad R, Cortes C, Dow RL, Dowling MS, El-Kattan A, Ford K, Guimarães CR, Hepworth D, Jiao W, LaPerle J, Liu S, Londregan A, Loria PM, Mathiowetz AM, Munchhof M, Orr ST, Petersen DN, Price DA, Skoura A, Smith AC, Wang J. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. doi: 10.1021/acsmedchemlett.5b00215. PMID: 26617966; PMCID: PMC4645242.
In vivo protocol:
1. Zou Z, Dong YS, Liu DD, Li G, Hao GZ, Gao X, Pan PY, Liang GB. MAP4K4 induces early blood-brain barrier damage in a murine subarachnoid hemorrhage model. Neural Regen Res. 2021 Feb;16(2):325-332. doi: 10.4103/1673-5374.290904. PMID: 32859792; PMCID: PMC7896238. 2. Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Carlo AA, Conrad R, Cortes C, Dow RL, Dowling MS, El-Kattan A, Ford K, Guimarães CR, Hepworth D, Jiao W, LaPerle J, Liu S, Londregan A, Loria PM, Mathiowetz AM, Munchhof M, Orr ST, Petersen DN, Price DA, Skoura A, Smith AC, Wang J. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. doi: 10.1021/acsmedchemlett.5b00215. PMID: 26617966; PMCID: PMC4645242.
1: Yang J, Zheng XG, Wu YL, Wang AP, Wang CH, Chen WX, Zhong S, Yang H. Intestinal epithelial cell-derived exosomes package microRNA-23a-3p alleviate gut damage after ischemia/reperfusion via targeting MAP4K4. Biomed Pharmacother. 2022 May;149:112810. doi: 10.1016/j.biopha.2022.112810. Epub 2022 Mar 15. PMID: 35303564. 2: Nam GS, Kim S, Kwon YS, Kim MK, Nam KS. A new function for MAP4K4 inhibitors during platelet aggregation and platelet-mediated clot retraction. Biochem Pharmacol. 2021 Jun;188:114519. doi: 10.1016/j.bcp.2021.114519. Epub 2021 Mar 15. PMID: 33737052. 3: Zou Z, Dong YS, Liu DD, Li G, Hao GZ, Gao X, Pan PY, Liang GB. MAP4K4 induces early blood-brain barrier damage in a murine subarachnoid hemorrhage model. Neural Regen Res. 2021 Feb;16(2):325-332. doi: 10.4103/1673-5374.290904. PMID: 32859792; PMCID: PMC7896238. 4: Roth Flach RJ, Skoura A, Matevossian A, Danai LV, Zheng W, Cortes C, Bhattacharya SK, Aouadi M, Hagan N, Yawe JC, Vangala P, Menendez LG, Cooper MP, Fitzgibbons TP, Buckbinder L, Czech MP. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis. Nat Commun. 2015 Dec 21;6:8995. doi: 10.1038/ncomms9995. PMID: 26688060; PMCID: PMC4703891. 5: Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Carlo AA, Conrad R, Cortes C, Dow RL, Dowling MS, El-Kattan A, Ford K, Guimarães CR, Hepworth D, Jiao W, LaPerle J, Liu S, Londregan A, Loria PM, Mathiowetz AM, Munchhof M, Orr ST, Petersen DN, Price DA, Skoura A, Smith AC, Wang J. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. doi: 10.1021/acsmedchemlett.5b00215. PMID: 26617966; PMCID: PMC4645242.

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