| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
DiZPK hydrochloride targets protein-protein interaction interfaces in living cells. Upon photoactivation, it covalently crosslinks interacting proteins, enabling the capture of direct binding partners. The primary molecular target is the engineered site within the bait protein where DiZPK has been genetically incorporated. Unlike small molecule inhibitors that block active sites, DiZPK functions as an environmental sensor that labels any protein within close proximity (within ~3-5 Angstrom) to the diazirine upon UV exposure.
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| ln Vitro |
As a photocrosslinker for detecting direct protein-protein interactions in living prokaryotic and eukaryotic cells, DiZPK hydrochloride is a structural analog of pyrrolysine (Pyl)[1].
In vitro experiments with DiZPK hydrochloride involve its incorporation into proteins expressed in E. coli or mammalian cells using orthogonal aminoacyl-tRNA synthetase/tRNA pairs. Western blotting analysis reveals UV-dependent crosslinking products that migrate at higher molecular weights. The compound has been shown to selectively crosslink interacting protein pairs, such as between a bait protein and its known binding partner. No cytotoxicity has been reported at working concentrations (typically 1-100 microM). |
| ln Vivo |
No in vivo animal studies have been reported with DiZPK hydrochloride as an administered compound. Its use is limited to cell culture or bacterial systems where genetic incorporation is feasible. Because the compound must be site-specifically incorporated via an engineered tRNA/tRNA synthetase pair, whole-animal applications are challenging. However, conceptually similar photocrosslinkers have been used in C. elegans or Drosophila, though DiZPK specifically has not.
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| Enzyme Assay |
For a standard photocrosslinking experiment, proteins of interest are expressed in cells grown in media supplemented with 1 mM DiZPK hydrochloride. After 12-24 hours of expression, cells are lysed, and lysates are irradiated at 365 nm with a UV lamp (intensity ~1.2 J/cm2) on ice for 10-20 minutes. Crosslinked products are then analyzed by SDS-PAGE and Western blotting. Unirradiated controls are essential to confirm UV dependence. For validation, crosslinking can be competed with excess free amino acid or disrupted by mutations.
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| Cell Assay |
Typical protocol for DiZPK hydrochloride: HEK293T or HeLa cells are transfected with plasmids encoding an orthogonal pyrrolysyl-tRNA synthetase (PylRS) and a UAG stop codon-containing target gene. Cells are cultured in DMEM with 10% FBS and penicillin/streptomycin, and 1 mM DiZPK is added to the medium 12-24 hours post-transfection. After 24-48 hours, cells are washed with PBS, harvested, lysed in RIPA buffer with protease inhibitors, and irradiated or not irradiated at 365 nm. Samples are separated by 4-12% gradient SDS-PAGE and analyzed by immunoblotting.
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| Animal Protocol |
No animal experiments have been conducted with DiZPK hydrochloride as a directly administered compound. Its specialized genetic incorporation mechanism limits its use to cell-based systems. However, conceptually similar photocrosslinkers have been used in Drosophila melanogaster for mapping PPIs, requiring tissue-specific expression of the orthogonal tRNA/tRNA synthetase pair. Such studies typically involve crossing transgenic fly lines followed by UV irradiation of dissected tissues or whole larvae. No such data are available for DiZPK.
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| ADME/Pharmacokinetics |
No pharmacokinetic data are available for DiZPK hydrochloride. As a tool compound for in vitro research, it is not intended for systemic administration. Based on its structure (molecular weight 321.8 g/mol, logP estimated ~0-1 due to polar groups), it would likely have low oral bioavailability and rapid clearance if administered. No studies on absorption, distribution, metabolism, excretion, or half-life have been reported. The compound is soluble in water (≥10 mg/mL) and is typically stored as a powder at -20degC protected from light.
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| Toxicity/Toxicokinetics |
Aminoglycoside-like compounds have known nephrotoxicity, but DiZPK hydrochloride as a research chemical has not undergone formal toxicological evaluation. Based on its structural similarity to lysine, acute toxicity is expected to be low. It is not classified as a carcinogen or mutagen. However, the photoactivated diazirine species is reactive and could theoretically cause DNA damage if UV-irradiated in the presence of cells. Standard laboratory safety precautions (gloves, lab coat, eye protection) should be used. Avoid inhalation or skin contact.
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| References |
[1]. Zhang M, et al. A genetically incorporated crosslinker reveals chaperone cooperation in acid resistance. Nat Chem Biol. 2011 Sep 4;7(10):671-7.
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| Additional Infomation |
DiZPK hydrochloride is not a drug; it is a chemical biology tool exclusively for research use. It has no clinical trial history, regulatory approval, or therapeutic indications. Unlike other photocrosslinkers (e.g., benzophenones or azides), DiZPK is smaller and produces a shorter crosslinking radius, offering higher spatial resolution for mapping interaction interfaces. The diazirine group is photochemically activated at 365 nm, which is less damaging to cells than 254 nm UV. The compound is often provided with orthogonal PylRS/tRNA vectors for direct implementation.
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| Exact Mass |
321.157
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|---|---|
| CAS # |
2349295-23-2
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| Related CAS # |
DiZPK;1337883-32-5
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| PubChem CID |
134694958
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
21
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| Complexity |
366
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1(N=N1)CCCNC(=O)NCCCC[C@@H](C(=O)O)N.Cl
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| InChi Key |
SMAFSXMDCAPICY-FVGYRXGTSA-N
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| InChi Code |
InChI=1S/C12H23N5O3.ClH/c1-12(16-17-12)6-4-8-15-11(20)14-7-3-2-5-9(13)10(18)19;/h9H,2-8,13H2,1H3,(H,18,19)(H2,14,15,20);1H/t9-;/m0./s1
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| Chemical Name |
(2S)-2-amino-6-[3-(3-methyldiazirin-3-yl)propylcarbamoylamino]hexanoic acid;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 8.33 mg/mL (25.89 mM)
DMSO: < 1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (6.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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