Hyaluronan-IN-1
Based on 1 Customer Validation
Hyaluronan-IN-1 (Pep-1) is a Hyaluronan inhibitor with a Kd value of 1.65 μM. Hyaluronan-IN-1 blocks CD44-dependent cell adhesion. Hyaluronan-IN-1 inhibits cell adhesion to hyaluronan substrates. Hyaluronan-IN-1 suppresses the development of contact hypersensitivity in mice by blocking the homing process of inflammatory cells to the skin. Hyaluronan-IN-1 also inhibits responses during the sensitization phase. Hyaluronan-IN-1 reduces lung metastasis of melanoma and prolongs the survival of mice. Hyaluronan-IN-1 can be used in research related to contact hypersensitivity, chronic skin inflammation, and melanoma.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 299157-43-0
- Formula: C64H94N20O16
- Molecular Weight:1399.56
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Hyaluronan-IN-1 (125 μg/mL; 72 h) does not directly affect the proliferation or the expression of proliferation marker genes in small intestinal organoids derived from wild-type (WT) C57BL/6 mice[1].
Hyaluronan-IN-1 (125I-labeled peptide; 50 μg/mL; 1 h) specifically binds to immobilized HA in a dose-dependent manner via HA-coated paramagnetic bead binding assay, with an apparent affinity constant Kd of 1.65 μM[2].
Hyaluronan-IN-1 (0-500 μg/mL; 2 h) inhibits the binding of soluble HA to BW5147 thymoma cells in a dose-dependent manner, with an inhibition rate of approximately 75% observed at the concentration of 500 μg/mL[2].
Hyaluronan-IN-1 (500 μg/mL; 1 h) potently inhibits CD44-dependent adhesion of B16-F10 melanoma cells to HA-coated substrates[3].
Hyaluronan-IN-1 (500 μg/mL; 1 h) potently inhibits the adhesion of RPMI 7591 melanoma cells to HA-coated substrates[3].
Hyaluronan-IN-1 (500 μg/mL; 1 h) potently inhibits the adhesion of B16-BL6 melanoma cells to HA-coated substrates[3].
Hyaluronan-IN-1 (0-250 μg/mL; 24 h) does not alter the proliferation of B16-F10 melanoma cells in vitro[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:WT C57BL/6 mouse small intestinal enteroids
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Concentration:125 μg/mL
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Incubation Time:72 h
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Result:Showed no effect on enteroid growth measured by MTT incorporation in either stem cell-supporting or differentiation-supporting conditions.
Showed no effect on the mRNA expression of proliferation markers Ki-67 or Cyclin-D1, with no significant differences compared to control enteroids.
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Cell Line:B16-F10 melanoma cells
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Concentration:0-250 μg/mL
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Incubation Time:24 h
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Result:Had no effect on [3H]thymidine uptake at any tested concentration, indicating no impact on in vitro cell proliferation.
Hyaluronan-IN-1 (40 mg/kg; i.p.; every other day; 7 days) reduces crypt fission, impairs Lgr5+ stem cell proliferation, suppresses crypt base epithelial proliferation, increases apoptosis, and reduces Paneth cell numbers in wild-type and CD44-/- postnatal mice, but not in TLR4-/- mice, indicating dependence on TLR4 signaling for these postnatal intestinal development effects[1].
Hyaluronan-IN-1 (13.3-40 µg/ear; s.c.; single or two injections; 1-3 days pre-DNFB exposure) inhibits hapten-triggered Langerhans cell migration from the murine epidermis in a dose- and time-dependent manner, with complete inhibition achieved via two 40 µg/ear injections 24 h and 1 h before DNFB exposure[2].
Hyaluronan-IN-1 (40 µg/ear/injection; s.c.; two injections; 24 h and 1 h before sensitization) locally and temporally suppresses the sensitization phase of murine contact hypersensitivity responses, with no induction of long-term unresponsiveness[2].
Hyaluronan-IN-1 (40 µg/ear-1 mg/animal; s.c., i.v., topical; single or two injections; 1-24 h before challenge) inhibits the elicitation phase of acute murine contact hypersensitivity responses, reducing ear swelling, edema, and leukocyte infiltration[2].
Hyaluronan-IN-1 (40 µg/ear/injection; s.c.; injections on days 0, 1, 3, and 5) significantly inhibits murine chronic dermatitis induced by repeated hapten applications[2].
Hyaluronan-IN-1 (500 μg/mouse; i.v.; single co-injection) significantly reduces B16-F10 melanoma lung metastasis incidence and prolongs survival in female C57BL/6 mice, with a 35.1% survival rate at 48 days post-tumor inoculation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, wild-type, CD44-/-, TLR4-/-, 3 weeks old at study start)[1]
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Dosage:40 mg/kg
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Administration:i.p.; twice a week; 5 weeks
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Result:Reduced small intestinal length, reduced colonic length, decreased jejunal villus height, decreased jejunal crypt depth, decreased colonic crypt depth, reduced number of BrdU-positive epithelial cells per proximal jejunum crypt section, reduced number of BrdU-positive epithelial cells per distal colon crypt section, and lowered average body weight by 10% compared to controls in wild-type mice.
Reduced small intestinal length, reduced colonic length, decreased jejunal villus height, decreased jejunal crypt depth, decreased colonic crypt depth, reduced number of BrdU-positive epithelial cells per proximal jejunum crypt section, reduced number of BrdU-positive epithelial cells per distal colon crypt section, and lowered average body weight by 8% compared to controls in CD44-/- mice.
Showed no significant effects on small intestinal length, colonic length, villus height, crypt depth, BrdU-positive cell counts, or body weight compared to controls in TLR4-/- mice.
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Animal Model:Lgr5/EGFP C57BL/6J (wild-type, CD44-/-, TLR4-/-, 7 days old at study start)[1]
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Dosage:40 mg/kg
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Administration:i.p.; every other day; 7 days
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Result:Reduced small intestinal crypt fission frequency, reduced colonic crypt fission frequency, decreased percentage of Lgr5+/BrdU+ epithelial cells in nonfissioning crypts, reduced positional epithelial proliferation at crypt base positions 1-4, increased positional apoptosis at crypt positions 1-7, and reduced Paneth cell number per crypt section in wild-type mice.
Reduced small intestinal crypt fission frequency, reduced colonic crypt fission frequency, decreased percentage of Lgr5+/BrdU+ epithelial cells in nonfissioning crypts, reduced positional epithelial proliferation at crypt base positions 1-4, showed no significant effect on apoptosis, and showed no significant effect on Paneth cell number in CD44-/- mice.
Showed no significant effects on crypt fission frequency, Lgr5+ stem cell proliferation, positional epithelial proliferation, apoptosis, or Paneth cell number compared to controls in TLR4-/- mice.
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Animal Model:BALB/c (female, 6-8 weeks old)[2]
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Dosage:40 µg/ear/injection (complete inhibition); 13.3 µg/ear (partial inhibition); 40 µg/ear (single injection, complete inhibition at 1-2 days pre-DNFB, no inhibition at 3 days pre-DNFB)
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Administration:s.c.; two injections at 24 h and 1 h before DNFB application; single injection at 24 h, 1 day, 2 days, or 3 days before DNFB application
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Result:Prevented DNFB-triggered Langerhans cell migration almost completely (≥80% inhibition across seven independent experiments) with two 40 µg/ear/injection doses.
Caused partial inhibition of DNFB-triggered Langerhans cell migration with a single 13.3 µg/ear dose.
Caused more prominent inhibition of DNFB-triggered Langerhans cell migration with a single 40 µg/ear dose.
Blocked DNFB-triggered Langerhans cell migration completely with a single 40 µg/ear dose administered 1 or 2 days before DNFB application.
Lost inhibitory activity for DNFB-triggered Langerhans cell migration with a single 40 µg/ear dose administered 3 days before DNFB application.
Showed equivalent inhibitory activity to its His→Ala mutant.
Abrogated inhibitory activity in its Trp→Ala mutant form.
Did not affect Langerhans cell densities in the absence of DNFB.
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Animal Model:BALB/c (female, 6-8 weeks old)[2]
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Dosage:40 µg/ear/injection
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Administration:s.c.; two injections at 24 h and 1 h before sensitization
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Result:Significantly reduced ear swelling responses to DNFB when sensitized with DNFB on the peptide-injected left ear.
Showed comparable ear swelling responses to OX (sensitized on the abdomen) relative to control peptide-treated mice.
Significantly reduced swelling responses to OX when sensitized with OX on the left ear.
Showed comparable swelling responses to DNFB (sensitized on the abdomen) relative to control peptide-treated mice.
Showed similar swelling responses to control peptide-treated mice when resensitized and rechallenged with DNFB, indicating no long-term unresponsiveness.
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Animal Model:BALB/c (female, 6-8 weeks old)[2]
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Dosage:40 µg/ear/injection (s.c.); 1 mg/animal (i.v.); 40 µg/ear (topical)
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Administration:s.c.; two injections at 24 h and 1 h before challenge; i.v.; single injection 1 h before challenge; topical; single application 1 h before challenge after acetone skin barrier disruption
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Result:Caused a significant reduction in ear swelling compared to PBS, control peptide, or Pep-2-treated mice via subcutaneous administration.
Caused significant reductions in ear swelling relative to control peptide-treated mice via intravenous and topical administration.
Reduced skin edema and leukocyte infiltration compared to controls, with statistically significant decreases in measured ear thickness and infiltrating leukocyte counts.
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Animal Model:BALB/c (female, 6-8 weeks old)[2]
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Dosage:40 µg/ear/injection
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Administration:s.c.; injections on days 0, 1, 3, and 5
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Result:Significantly reduced ear swelling at every time point tested compared to control peptide-treated mice, with progressive suppression of the chronic inflammatory response.
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Animal Model:C57BL/6 (female, 6-8 weeks old)[3]
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Dosage:500 μg/mouse (co-injection); 40 μg/mouse (days 3 and 6 post-inoculation)
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Administration:s.c.; single co-injection; two additional injections on days 3 and 6
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Result:Had no significant effect on local tumor growth at the inoculation sites, with tumor size measurements comparable to control groups.
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Animal Model:C57BL/6 (female, 6-8 weeks old)[3]
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Dosage:500 μg/mouse
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Administration:i.v.; single co-injection
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Result:Reduced the number of lung metastatic lesions with statistical significance (P < 0.05) compared to control groups.
Prolonged survival significantly (P < 0.01), with a median survival time of 32 days, compared to 26 days for the control peptide group and 25 days for the PBS group.
Achieved a 35.1% survival rate (13 of 37 mice) at 48 days post-inoculation, while all PBS-treated mice died by day 28 and only 2 of 30 control peptide-treated mice survived.
Resulted in no macroscopically discernible lung metastatic lesions in surviving mice.
Chemical Information
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CAS No. 299157-43-0
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Appearance Solid
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Molecular Weight 1399.56
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Formula C64H94N20O16
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Color White to off-white
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Sequence
Gly-Ala-His-Trp-Gln-Phe-Asn-Ala-Leu-Thr-Val-Arg
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Sequence Shortening
GAHWQFNALTVR
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Riehl TE, et al. CD44 and TLR4 mediate hyaluronic acid regulation of Lgr5+ stem cell proliferation, crypt fission, and intestinal growth in postnatal and adult mice. Am J Physiol Gastrointest Liver Physiol. 2015;309(11):G874-G887. [Content Brief]
[2]. Mummert ME, et al. Development of a peptide inhibitor of hyaluronan-mediated leukocyte trafficking. J Exp Med. 2000;192(6):769-779. [Content Brief]
[3]. Mummert ME, et al. Functional roles of hyaluronan in B16-F10 melanoma growth and experimental metastasis in mice. Mol Cancer Ther. 2003 Mar;2(3):295-300. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hyaluronan-IN-1 Related Classifications
HY-P5352 Related Classifications
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